Andrographolide sulfonate(AS)is a sulfonated derivative of andrographolide extracted from Andrographis paniculata(Burm.f.)Nees,and has been approved for several decades in China.The present study aimed to investigate ...Andrographolide sulfonate(AS)is a sulfonated derivative of andrographolide extracted from Andrographis paniculata(Burm.f.)Nees,and has been approved for several decades in China.The present study aimed to investigate the novel therapeutic application and possible mechanisms of AS in the treatment of rheumatoid arthritis.Results indicated that administration of AS by injection or gavage significantly reduced the paw swelling,improved body weights,and attenuated pathological changes in joints of rats with adjuvant-induced arthritis.Additionally,the levels of tumor necrosis factor-alpha(TNF-α),interleukin-6(IL-6),and IL-1β in the serum and ankle joints were reduced.Bioinformatics analysis,along with the spleen index and measurements of IL-17 and IL-10 levels,suggested a potential relationship between AS and Th17 cells under arthritic conditions.In vitro,AS was shown to block Th17 cell differentiation,as evidenced by the reduced percentages of CD4^(+)IL-17A^(+)T cells and decreased expression levels of RORγt,IL-17A,IL-17F,IL-21,and IL-22,without affecting the cell viability and apoptosis.This effect was attributed to the limited glycolysis,as indicated by metabolomics analysis,reduced glucose uptake,and p H measurements.Further investigation revealed that AS might bind to hexokinase2(HK2)to down-regulate the protein levels of HK2 but not glyceraldehyde-3-phosphate dehydrogenase(GAPDH)or pyruvate kinase M2(PKM2),and overexpression of HK2 reversed the inhibition of AS on Th17 cell differentiation.Furthermore,AS impaired the activation of phosphatidylinositol 3-kinase(PI3K)/protein kinase B(AKT)signals in vivo and in vitro,which was abolished by the addition of lactate.In conclusion,AS significantly improved adjuvant-induced arthritis(AIA)in rats by inhibiting glycolysis-mediated activation of PI3K/AKT to restrain Th17 cell differentiation.展开更多
Acute lung injury(ALI)is a severe inflammatory condition with a high mortality rate,often precipitated by sepsis.The pathophysiology of ALI involves complex mechanisms,including inflammation,oxidative stress,and ferro...Acute lung injury(ALI)is a severe inflammatory condition with a high mortality rate,often precipitated by sepsis.The pathophysiology of ALI involves complex mechanisms,including inflammation,oxidative stress,and ferroptosis,a novel form of regulated cell death.This study explores the therapeutic potential of andrographolide(AG),a bioactive compound derived from Andrographis,in mitigating Lipopolysaccharide(LPS)-induced inflammation and ferroptosis.Our research employed in vitro experiments with RAW264.7 macrophage cells and in vivo studies using a murine model of LPS-induced ALI.The results indicate that AG significantly suppresses the production of pro-inflammatory cytokines and inhibits ferroptosis in LPS-stimulated RAW264.7 cells.In vivo,AG treatment markedly reduces lung edema,decreases inflammatory cell infiltration,and mitigates ferroptosis in lung tissues of LPS-induced ALI mice.These protective effects are mediated via the modulation of the Toll-like receptor 4(TLR4)/Kelch-like ECH-associated protein 1(Keap1)/Nuclear factor erythroid 2-related factor 2(Nrf2)signaling pathway.Molecular docking simulations identified the binding sites of AG on the TLR4 protein(Kd value:-33.5 kcal·mol^(-1)),and these interactions were further corroborated by Cellular Thermal Shift Assay(CETSA)and SPR assays.Collectively,our findings demonstrate that AG exerts potent anti-inflammatory and anti-ferroptosis effects in LPS-induced ALI by targeting TLR4 and modulating the Keap1/Nrf2 pathway.This study underscores AG's potential as a therapeutic agent for ALI and provides new insights into its underlying mechanisms of action.展开更多
The rise of emerging infectious diseases has become notably prominent due to ecological changes and mutations in pathogens.The respiratory illness outbreak caused by the COVID-19 pandemic has spread globally.Natural p...The rise of emerging infectious diseases has become notably prominent due to ecological changes and mutations in pathogens.The respiratory illness outbreak caused by the COVID-19 pandemic has spread globally.Natural products contain numerous structures and biological activities,offering ample options for discovering new antiviral drugs with unique targets and mechanisms.Andrographis paniculata has been utilized in Indian Ayurvedic,Swedish,Traditional Thai,and Chinese medicine to alleviate coughs,colds,and influenza symptoms.Early-stage laboratory studies indicate that this herbal extract may reduce inflammation and fever,and boost the body's natural defenses against viruses,potentially leading to symptom relief.This review aims to systematically present clinical trial data about antiviral herbal formulations derived from Andrographis paniculata,delineating the antiviral effects of both natural and synthetic derivatives,along with in silico analyses.展开更多
This paper reviews the purification process,content determination methods and pharmacological action of Andrographolide,aiming to provide new ideas for the subsequent study of Andrographolide and its related drug deve...This paper reviews the purification process,content determination methods and pharmacological action of Andrographolide,aiming to provide new ideas for the subsequent study of Andrographolide and its related drug development and application.展开更多
Objective: To study the effects of andrographolide on immune functions and the immune mechanism in clinical therapy.Methods: The amounts of IFN-α,IFN-γ, TNF-α, IL-8 in the peripheral blood mononuclear cells (PBMC) ...Objective: To study the effects of andrographolide on immune functions and the immune mechanism in clinical therapy.Methods: The amounts of IFN-α,IFN-γ, TNF-α, IL-8 in the peripheral blood mononuclear cells (PBMC) culture supernatants dealt with by different concentrations of LianBiZhi (LBZ) injection, the effective component of which is andrographolide, were detected by biological activity test or ELISA in vitro. The effects of LBZ injection on macrophage phagocytotic function and natural killer cells cytotoxicity were examined by means of macrophage to phagocytize cock erythrocyte and measurement of lactate dehydrogenase (LDH) activity released from the damaged cells, respectively.Results: The LBZ injection could not only enhance the phagocytosis activity of peritoneal macrophage from guinea pig to phagocytosis cock erythrocytes, but also augment the cytotoxicity mediated by natural killer cells from PBMCs.Conclusion: Andrographolide is an immunostimulant agent which can modulate both antigen specific and nonspecific immune function by means of its natural killer cells, macrophage and cytokines.展开更多
A new andrographolide metabolite 1 was isolated from human urine samples after oral administration. The structure was determined to be 3-carbonylandrographolide-19-O-β-D-glu- curonide on the basis of chemical evidenc...A new andrographolide metabolite 1 was isolated from human urine samples after oral administration. The structure was determined to be 3-carbonylandrographolide-19-O-β-D-glu- curonide on the basis of chemical evidences and spectral analysis, especially by 2D-NMR techni- ques.展开更多
The NF-kB transcription factors modulate the expression of tissue factor （TF）, E-selectin （CD62E） and vascular cell adhesion molecule-1 （VCAM-1）, which are essential for thrombosis and inflammation. We have prev...The NF-kB transcription factors modulate the expression of tissue factor （TF）, E-selectin （CD62E） and vascular cell adhesion molecule-1 （VCAM-1）, which are essential for thrombosis and inflammation. We have previously shown that andrographolide （Andro） covalently modifies the reduced cysteine^62 of p50-a major subunit of NF-kB transcription factors, thus blocking the binding of NF-kB transcription factors to the promoters of their target genes, preventing NF-kB activation and inhibiting inflammation in vitro and in vivo. Here we report that Andro, but not its inactive structural analog 4H-Andro, significantly suppressed the proliferation of arterial neointima （-60% reduction） in a murine model of arterial restenosis. Consistently, p50^-/- mice manifested attenuated neointimal hyperplasia upon arterial ligation. Notably, the same dosage of Andro did not further reduce neointimal formation in p50^-/- mice, which implicates the specificity of Andro on p50 for treating experimental arterial restenosis. The upregulation of NF-kB target genes, including TF, E-selectin and VCAM-1, and the increased deposition of leukocytes （mainly CD68^＋ macrophages） were clearly detected within the injured arterial walls, all of which were significantly abolished by treatment with Andro or genetic deletion of p50. The expression ofTF, E-selectin and VCAM-I was also markedly upregulated in the patient sample of thrombotic vasculitis, indicating the clinical relevance of NF-kB activation in the pathogeneses of occlusive arterial diseases. Our data thus indicate that, by the downregulation of the NF-kB target genes that are critical in thrombosis and inflammation, specific inhibitors of p50, such as Andro, may be therapeutically valuable for preventing and treating thrombotic arterial diseases, including neointimal hyperplasia in arterial restenosis.展开更多
Andrographolide (AG) is the characteristic constituent of Andrographis paniculata, of the Acanthaceae family. This plant is a well-known Asian medicinal plant that is widely used in India, China, and Thailand. A monog...Andrographolide (AG) is the characteristic constituent of Andrographis paniculata, of the Acanthaceae family. This plant is a well-known Asian medicinal plant that is widely used in India, China, and Thailand. A monograph of Herba Andrographidis (Chuanxinlian) is included in the Chinese Pharmacopoeia, which reports that this decoction can “remove heat, counteract toxicity, and reduce swellings.” The numerous potential activities of AG range from anti-inflammatory to anti-diabetic action, from neuroprotection to antitumor activity, and from hepatoprotective to anti-obesity properties. However, AG has low bioavailability and poor water solubility, which can limit its distribution and accumulation in the body after administration. In addition, AG is not stable in gastrointestinal alkaline and acidic environments, and has been reported to have a very short half-life. Among the diverse strategies that have been adopted to increase AG water solubility and permeability, the technological approach is the most useful way to develop appropriate delivery systems. This review reports on published studies related to microparticles (MPs) and nanoparticles (NPs) loaded with AG. MPs based on polylactic-glycolic acid (PLGA), alginic acid, and glucan derivatives have been developed for parenteral oral and pulmonary administration, respectively. NPs include vesicles (both liposomes and niosomes);polymeric NPs (based on polyvinyl alcohol, polymerized phenylboronic acid, PLGA, human serum albumin, poly ethylcyanoacrylate, and polymeric micelles);solid lipid NPs;microemulsions and nanoemulsions;gold NPs;nanocrystals;and nanosuspensions. Improved bioavailability, target-tissue distribution, and efficacy of AG loaded in the described drug delivery systems have been reported.展开更多
Tumor necrosis factor-related apoptosis-inducing ligand （TRAIL） is a promising agent for anticancer therapy. The identification of small molecules that can establish the sensitivity of prostate cancer （PCa） cells ...Tumor necrosis factor-related apoptosis-inducing ligand （TRAIL） is a promising agent for anticancer therapy. The identification of small molecules that can establish the sensitivity of prostate cancer （PCa） cells to TRAIL-induced apoptosis is crucial for the targeted treatment of PCa. PC3, DU145, JAC-1, TsuPrl, and LNCaP cells were treated with Andrographolide （Andro） and TRAIL, and the apoptosis was measured using the Annexin V/PI double staining method. Real time-polymerase chain reaction （PCR） and Western blot analysis were performed to measure the expression levels of target molecules. RNA interference technique was used to down-regulate the expression of the target protein. We established a nude mouse xenograft model of PCa, which was used to measure the caspase-3 activity in the tumor cells using flow cytometry. In this research study, our results demonstrated that Andro preferentially increased the sensitivity of PCa cells to TRAIL-induced apoptosis at subtoxic concentrations, and the regulation mechanism was related to the up-regulation of DR4. In addition, it also increased the p53 expression and led to the generation of reactive oxygen species （ROS） in the cells. Further research revealed that the DR4 inhibition, p53 expression, and ROS generation can significantly reduce the apoptosis induced by the combination of TRAIL and Andro in PCa cells. In conclusion, Andro increases the sensitivity of PCa cells to TRAIL-induced apoptosis through the generation of ROS and up-regulation of p53 and then promotes PCa cell apoptosis associated with the activation of DR4.展开更多
Andrographolide is a labdane diterpenoid extracted and purified from the aerial parts of plants belonging to genus Andrographis(Acanthaceae).The research has shown the plant based compound is low cytotoxic,having anti...Andrographolide is a labdane diterpenoid extracted and purified from the aerial parts of plants belonging to genus Andrographis(Acanthaceae).The research has shown the plant based compound is low cytotoxic,having antimicrobial,anti-cancer,antiviral and anti-parasitic effects.Andrographolide both prevent spread as well as transmission of virus to neighboring cells by interfering with different cell signaling pathways.In addition to its medicinal value,plant has been found having nutritional value.Therefore being cost effective,easy availability and having nutritional value as a natural supplement,can be used to improve the quality of life in countries having low standard of living.Due to the limited number of effective vaccines,the plant-based antiviral drugs have provided considerable hope for fighting against the viral infections.The plant-derived compound when produced in large quantities is cost effective with low cytotoxic effects.However,much deep insight research at the molecular level is needed to develop the molecules against the viral infection.This paper aims to highlight the antiviral role of Andrographolide that can made significant contributions toward the improvement of human health and will also summarize the current status and future strategies concerning the therapeutic applications of Andrographolide to combat different viral disease in humans.展开更多
Porcine reproductive and respiratory syndrome virus(PRRSV) continues to cause significant economic loss worldwide and remains a serious threat to the pork industry. Currently, vaccination strategies provide limited pr...Porcine reproductive and respiratory syndrome virus(PRRSV) continues to cause significant economic loss worldwide and remains a serious threat to the pork industry. Currently, vaccination strategies provide limited protection against PRRSV infection, and consequently, new antiviral strategies are urgently required. Andrographolide(Andro) and its derivative potassium dehydrographolide succinate(PDS) have been used clinically in China and other Asian countries as therapies for inflammation-related diseases, including bacterial and viral infections, for decades. Here, we demonstrate that Andro and PDS exhibit robust activity against PRRSV replication in Marc-145 cells and primary porcine alveolar macrophages(PAMs). The two compounds exhibited broad-spectrum inhibitory activities in vitro against clinically circulating type 2 PRRSV GD-HD, XH-GD, and NADC30-like HNhx strains in China. The EC_(50)values of Andro against three tested PRRSV strain infections in Marc-145 cells ranged from 11.7 to 15.3 lmol/L, with selectivity indexes ranging from 8.3 to10.8, while the EC_(50)values of PDS ranged from 57.1 to 85.4 lmol/L, with selectivity indexes ranging from 344 to 515.Mechanistically, the anti-PRRSV activity of the two compounds is closely associated with their potent suppression on NFj B activation and enhanced oxidative stress induced by PRRSV infection. Further mechanistic investigations revealed that PDS, but not Andro, is able to directly interact with PRRSV particles. Taken together, our findings suggest that Andro and PDS are promising PRRSV inhibitors in vitro and deserves further in vivo studies in swine.展开更多
Atherosclerotic cardiovascular disease(ASCVD)frequently results in sudden death and poses a serious threat to public health worldwide.The drugs approved for the prevention and treatment of ASCVD are usually used in co...Atherosclerotic cardiovascular disease(ASCVD)frequently results in sudden death and poses a serious threat to public health worldwide.The drugs approved for the prevention and treatment of ASCVD are usually used in combination but are inefficient owing to their side effects and single therapeutic targets.Therefore,the use of natural products in developing drugs for the prevention and treatment of ASCVD has received great scholarly attention.Andrographolide(AG)is a diterpenoid lactone compound extracted from Andrographis paniculata.In addition to its use in conditions such as sore throat,AG can be used to prevent and treat ASCVD.It is different from drugs that are commonly used in the prevention and treatment of ASCVD and can not only treat obesity,diabetes,hyperlipidaemia and ASCVD but also inhibit the pathological process of atherosclerosis(AS)including lipid accumulation,inflammation,oxidative stress and cellular abnormalities by regulating various targets and pathways.However,the pharmacological mechanisms of AG underlying the prevention and treatment of ASCVD have not been corroborated,which may hinder its clinical development and application.Therefore,this review summarizes the physiological and pathological mechanisms underlying the development of ASCVD and the in vivo and in vitro pharmacological effects of AG on the relative risk factors of AS and ASCVD.The findings support the use of the old pharmacological compound(‘old bottle’)as a novel drug(‘novel wine’)for the prevention and treatment of ASCVD.Additionally,this review summarizes studies on the availability as well as pharmaceutical and pharmacokinetic properties of AG,aiming to provide more information regarding the clinical application and further research and development of AG.展开更多
Current formulation development strongly relies on trial-and-error experiments in the laboratory by pharmaceutical scientists,which is time-consuming,high cost and waste materials.This research aims to integrate vario...Current formulation development strongly relies on trial-and-error experiments in the laboratory by pharmaceutical scientists,which is time-consuming,high cost and waste materials.This research aims to integrate various computational tools,including machine learning,molecular dynamic simulation and physiologically based absorption modeling(PBAM),to enhance andrographolide(AG)/cyclodextrins(CDs)formulation design.The light GBM prediction model we built before was utilized to predict AG/CDs inclusion's binding free energy.AG/γ-CD inclusion complexes showed the strongest binding affinity,which was experimentally validated by the phase solubility study.The molecular dynamic simulation was used to investigate the inclusion mechanism between AG andγ-CD,which was experimentally characterized by DSC,FTIR and NMR techniques.PBAM was applied to simulate the in vivo behavior of the formulations,which were validated by cell and animal experiments.Cell experiments revealed that the presence of D-α-Tocopherol polyethylene glycol succinate(TPGS)significantly increased the intracellular uptake of AG in MDCKMDR1 cells and the absorptive transport of AG in MDCK-MDR1 monolayers.The relative bioavailability of the AG-CD-TPGS ternary system in rats was increased to 2.6-fold and 1.59-fold compared with crude AG and commercial dropping pills,respectively.In conclusion,this is the first time to integrate various computational tools to develop a new AG-CD-TPGS ternary formulation with significant improvement of aqueous solubility,dissolution rate and bioavailability.The integrated computational tool is a novel and robust methodology to facilitate pharmaceutical formulation design.展开更多
Atrial fibrillation(AF)is the most prevalent cardiac arrhythmia seen in clinical settings,which has been associated with substantial rates of mortality and morbidity.However,clinically available drugs have limited eff...Atrial fibrillation(AF)is the most prevalent cardiac arrhythmia seen in clinical settings,which has been associated with substantial rates of mortality and morbidity.However,clinically available drugs have limited efficacy and adverse effects.We aimed to investigate the mechanisms of action of andrographolide(Andr)with respect to AF.We used network pharmacology approaches to investigate the possible therapeutic effect of Andr.To define the role of Andr in AF,HL-1 cells were pro-treated with Andr for 1 h before rapid electronic stimulation(RES)and rabbits were pro-treated for 1 d before rapid atrial pacing(RAP).Apoptosis,myofibril degradation,oxidative stress,and inflammation were determined.RNA sequencing(RNA-seq)was performed to investigate the relevant mechanism.Andr treatment attenuated RAP-induced atrial electrophysiological changes,inflammation,oxidative damage,and apoptosis both in vivo and in vitro.RNA-seq indicated that oxidative phosphorylation played an important role.Transmission electron microscopy and adenosine triphosphate(ATP)content assay respectively validated the morphological and functional changes in mitochondria.The translocation of nuclear factor erythroid 2-related factor 2(Nrf2)to the nucleus and the molecular docking suggested that Andr might exert a therapeutic effect by influencing the Keap1-Nrf2 complex.In conclusions,this study revealed that Andr is a potential preventive therapeutic drug toward AF via activating the translocation of Nrf2 to the nucleus and the upregulation of heme oxygenase-1(HO-1)to promote mitochondrial bioenergetics.展开更多
Macrophages play a crucial role in initiating,maintaining,and resolving inflammation through the phenotypic shift,inducing or inhibiting the production of inflammatory cytokines.Therefore,macrophages are potential tar...Macrophages play a crucial role in initiating,maintaining,and resolving inflammation through the phenotypic shift,inducing or inhibiting the production of inflammatory cytokines.Therefore,macrophages are potential targets for treating inflammatory diseases.Andrographolide(AND)is a potent anti-inflammatory drug that can reduce pro-inflammatory cytokines and suppress NF-κB/MAPK pathway in activated macrophages.Although AND has many medicinal properties,its lower water solubility and first-pass effect in the liver have hindered its clinical application.In this context,by using a metal phenolic network as a stabilizer,we designed and prepared highly stabilized AND nanocrystals(AND-MPN Ns)with high drug loading capacity to facilitate the clinical application of AND.Our findings showed that AND-MPN Ns could be used to enhance the anti-inflammation in-vitro via macrophage polarization,reducing proinflammatory cytokines IL-6 and TNF-α,and suppressing the NF-κB signaling pathway activation.The results demonstrated the potential of AND-MPN Ns to combat inflammatory diseases effectively.展开更多
Andrographis paniculata Nees has been extensively used for traditional medicine and help against fever dysentery, diarrhoea, inflammation, and sore throat. In this study, andrographolide, the main component of this pl...Andrographis paniculata Nees has been extensively used for traditional medicine and help against fever dysentery, diarrhoea, inflammation, and sore throat. In this study, andrographolide, the main component of this plant was extracted from the leaves of A. paniculata using supercritical carbon dioxide. The operating pressures were varied from 7.50 to 20MPa, the temperatures were varied from 30℃ to 60℃, and the flow rates were varied from 0.5 to 4ml.min^-1. The best extraction condition occurred at 10MPa, 40℃, and a flow rate of 2ml.min^-1 for a 3g sample of A. paniculata ground-dried leaves. The measured extraction rate was found to be about 0.0174g of andrographolide per gram of andrographolide present in the leaves per hour of operation. The future studies must focus on the interaction between the various operating parameters such as temperature, pressure, and flow rate of supercritical carbon dioxide.展开更多
A series of Andro derivatives were described and evaluated for their anti-HIV activity in vitro. Compound 10 and 16b, of which TI were 〉 10, had some anti-HIV-1 activity in vitro. Therein, compound 10 which was the b...A series of Andro derivatives were described and evaluated for their anti-HIV activity in vitro. Compound 10 and 16b, of which TI were 〉 10, had some anti-HIV-1 activity in vitro. Therein, compound 10 which was the best potent compound, could serve as a new lead for further development of anti-AIDS agents.展开更多
One-sixth of the currently known natural products containα,β-unsaturated carbonyl groups.Our previous studies reported a rare C-sulfonate metabolic pathway.Sulfonate groups were linked to theβ-carbon ofα,β-unsatu...One-sixth of the currently known natural products containα,β-unsaturated carbonyl groups.Our previous studies reported a rare C-sulfonate metabolic pathway.Sulfonate groups were linked to theβ-carbon ofα,β-unsaturated carbonyl-based natural compounds through this pathway.However,the mechanism of this type of metabolism is still not fully understood,especially whether it is formed through enzyme-mediated biotransformation or direct sulfite addition.In this work,the enzyme-mediated and non-enzymatic pathways were studied.First,the sulfite content in rat intestine was determined by LC-MS/MS.The results showed that the amount of sulfite in rat intestinal contents was from 41.5 to 383μg·g^(-1),whereas the amount of sulfite in rat feed was lower than the lower limit of quantitation(20μg·g^(-1)).Second,the reaction kinetics of sulfite-andrographolide reactions in phosphate buffer solutions(pH 6-8)was studied.The half-lives of andrographolide ranged from minutes to hours.This was suggested that the C-sulfonate reaction of andrographolide was very fast.Third,the C-sulfonate metabolites of andrographolide were both detected when andrographolide and L-cysteine-S-conjugate andrographolide were incubated with the rat small intestine contents or sulfite,indicating that the sulfite amount in rat intestine contents was high enough to react with andrographolide,which assisted a significant portion of andrographolide metabolism.Finally,the comparison of andrographolide metabolite profiles among liver homogenate(with NADPH),liver S9(with NADPH),small intestine contents homogenate(with no NADPH),and sulfite solution incubations showed that the C-sulfonate metabolites were predominantly generated in the intestinal tract by non-enzymatic pathway.In summary,sulfite can serve as a substrate for C-sulfonate metabolism,and these results identified non-enzymatically nucleophilic addition as the potential mechanism for C-sulfonate metabolism of compounds containingα,β-unsaturated carbonyl moiety.展开更多
An inclusion complex of b-cyclodextrin with andrographolide (Andro) was prepared by using a convenient method of microwave irradiation. The structure of the inclusion complex was determined by the 1H NMR, 2D NMR spect...An inclusion complex of b-cyclodextrin with andrographolide (Andro) was prepared by using a convenient method of microwave irradiation. The structure of the inclusion complex was determined by the 1H NMR, 2D NMR spectroscopy as well as the elemental analysis.展开更多
Andrographolide total ester sulfonate（ATES） injection is one of the products of traditional Chinese medicine（TCM） currently used against viral infection in China.ATES injection was approved for manufacturing and m...Andrographolide total ester sulfonate（ATES） injection is one of the products of traditional Chinese medicine（TCM） currently used against viral infection in China.ATES injection was approved for manufacturing and marketing in January 2002.It is indicated for acute respiratory infections,tonsillitis,chronic obstructive pulmonary disease,influenza,foot and mouth disease,bronchiolitis,herpangina,mumps,infectious mononucleosis and psychosis.However,its usage also carries risk.We investigated the use of ATES at the Wuhan Union Hospital from January 2014 to December 2014 and evaluated its real-world clinical application using the hospital centralized monitoring method.A total of 848 cases were enrolled in this study.In these cases,it was mainly used for postoperative anti-inflammation and treating upper respiratory infection,pneumonia and bronchitis.Among them,39.86% were contraindicated.Irregular medication of adults and children accounted for 1.91% and 23.38%,respectively.Improper choice of solvent accounted for 3.18%.The choice of intravenous drip versus aerosol inhalation was reasonable.A case of adverse events（AEs） was observed in the monitoring period,and the incidence of adverse drug reaction（ADR） of ATES injection was 0.12%.ATES injection in our hospital is relatively safe with a low incidence of adverse reactions.The study assesses the clinical usage and adverse reactions of ATES injection,and provides suggestions for rational use in clinical practice.展开更多
基金supported by the project of Central Funds Guiding the Local Science and Technology Development(No.20212ZDD02010)。
文摘Andrographolide sulfonate(AS)is a sulfonated derivative of andrographolide extracted from Andrographis paniculata(Burm.f.)Nees,and has been approved for several decades in China.The present study aimed to investigate the novel therapeutic application and possible mechanisms of AS in the treatment of rheumatoid arthritis.Results indicated that administration of AS by injection or gavage significantly reduced the paw swelling,improved body weights,and attenuated pathological changes in joints of rats with adjuvant-induced arthritis.Additionally,the levels of tumor necrosis factor-alpha(TNF-α),interleukin-6(IL-6),and IL-1β in the serum and ankle joints were reduced.Bioinformatics analysis,along with the spleen index and measurements of IL-17 and IL-10 levels,suggested a potential relationship between AS and Th17 cells under arthritic conditions.In vitro,AS was shown to block Th17 cell differentiation,as evidenced by the reduced percentages of CD4^(+)IL-17A^(+)T cells and decreased expression levels of RORγt,IL-17A,IL-17F,IL-21,and IL-22,without affecting the cell viability and apoptosis.This effect was attributed to the limited glycolysis,as indicated by metabolomics analysis,reduced glucose uptake,and p H measurements.Further investigation revealed that AS might bind to hexokinase2(HK2)to down-regulate the protein levels of HK2 but not glyceraldehyde-3-phosphate dehydrogenase(GAPDH)or pyruvate kinase M2(PKM2),and overexpression of HK2 reversed the inhibition of AS on Th17 cell differentiation.Furthermore,AS impaired the activation of phosphatidylinositol 3-kinase(PI3K)/protein kinase B(AKT)signals in vivo and in vitro,which was abolished by the addition of lactate.In conclusion,AS significantly improved adjuvant-induced arthritis(AIA)in rats by inhibiting glycolysis-mediated activation of PI3K/AKT to restrain Th17 cell differentiation.
基金supported by China-ASEAN International Innovative Center for Health Industry of Traditional Chinese Medicine(No.AD20297142)Guangxi Collaborative Innovation Center for Scientific Achievements Transformation and Applicationon Traditional Chinese Medicine(No.05020058)。
文摘Acute lung injury(ALI)is a severe inflammatory condition with a high mortality rate,often precipitated by sepsis.The pathophysiology of ALI involves complex mechanisms,including inflammation,oxidative stress,and ferroptosis,a novel form of regulated cell death.This study explores the therapeutic potential of andrographolide(AG),a bioactive compound derived from Andrographis,in mitigating Lipopolysaccharide(LPS)-induced inflammation and ferroptosis.Our research employed in vitro experiments with RAW264.7 macrophage cells and in vivo studies using a murine model of LPS-induced ALI.The results indicate that AG significantly suppresses the production of pro-inflammatory cytokines and inhibits ferroptosis in LPS-stimulated RAW264.7 cells.In vivo,AG treatment markedly reduces lung edema,decreases inflammatory cell infiltration,and mitigates ferroptosis in lung tissues of LPS-induced ALI mice.These protective effects are mediated via the modulation of the Toll-like receptor 4(TLR4)/Kelch-like ECH-associated protein 1(Keap1)/Nuclear factor erythroid 2-related factor 2(Nrf2)signaling pathway.Molecular docking simulations identified the binding sites of AG on the TLR4 protein(Kd value:-33.5 kcal·mol^(-1)),and these interactions were further corroborated by Cellular Thermal Shift Assay(CETSA)and SPR assays.Collectively,our findings demonstrate that AG exerts potent anti-inflammatory and anti-ferroptosis effects in LPS-induced ALI by targeting TLR4 and modulating the Keap1/Nrf2 pathway.This study underscores AG's potential as a therapeutic agent for ALI and provides new insights into its underlying mechanisms of action.
文摘The rise of emerging infectious diseases has become notably prominent due to ecological changes and mutations in pathogens.The respiratory illness outbreak caused by the COVID-19 pandemic has spread globally.Natural products contain numerous structures and biological activities,offering ample options for discovering new antiviral drugs with unique targets and mechanisms.Andrographis paniculata has been utilized in Indian Ayurvedic,Swedish,Traditional Thai,and Chinese medicine to alleviate coughs,colds,and influenza symptoms.Early-stage laboratory studies indicate that this herbal extract may reduce inflammation and fever,and boost the body's natural defenses against viruses,potentially leading to symptom relief.This review aims to systematically present clinical trial data about antiviral herbal formulations derived from Andrographis paniculata,delineating the antiviral effects of both natural and synthetic derivatives,along with in silico analyses.
基金Supported by Heilongjiang Province Key Research and Development Plan Guid-ance Project(GZ20220039),Central Support for Local Universities Reform and Development Fund Talent Training Project(2020GSP16).
文摘This paper reviews the purification process,content determination methods and pharmacological action of Andrographolide,aiming to provide new ideas for the subsequent study of Andrographolide and its related drug development and application.
文摘Objective: To study the effects of andrographolide on immune functions and the immune mechanism in clinical therapy.Methods: The amounts of IFN-α,IFN-γ, TNF-α, IL-8 in the peripheral blood mononuclear cells (PBMC) culture supernatants dealt with by different concentrations of LianBiZhi (LBZ) injection, the effective component of which is andrographolide, were detected by biological activity test or ELISA in vitro. The effects of LBZ injection on macrophage phagocytotic function and natural killer cells cytotoxicity were examined by means of macrophage to phagocytize cock erythrocyte and measurement of lactate dehydrogenase (LDH) activity released from the damaged cells, respectively.Results: The LBZ injection could not only enhance the phagocytosis activity of peritoneal macrophage from guinea pig to phagocytosis cock erythrocytes, but also augment the cytotoxicity mediated by natural killer cells from PBMCs.Conclusion: Andrographolide is an immunostimulant agent which can modulate both antigen specific and nonspecific immune function by means of its natural killer cells, macrophage and cytokines.
文摘A new andrographolide metabolite 1 was isolated from human urine samples after oral administration. The structure was determined to be 3-carbonylandrographolide-19-O-β-D-glu- curonide on the basis of chemical evidences and spectral analysis, especially by 2D-NMR techni- ques.
基金This work was supported by grants from the National Natural Science Foundation of China （30370694, 30421005, 30623003, 30400245 and 30630036）, the Ministry of Science and Technology of China （2002CB513006, 2006CB943902 and 2006AA02Z 169）, the Chinese Acad- emy of Sciences （KSCX2-YW-R-67 and KJCX2-YW-H08） and the Shanghai Municipal Commission for Science and Technology （04JC14078, 06DZ22032, 055407035 and 058014578）.
文摘The NF-kB transcription factors modulate the expression of tissue factor （TF）, E-selectin （CD62E） and vascular cell adhesion molecule-1 （VCAM-1）, which are essential for thrombosis and inflammation. We have previously shown that andrographolide （Andro） covalently modifies the reduced cysteine^62 of p50-a major subunit of NF-kB transcription factors, thus blocking the binding of NF-kB transcription factors to the promoters of their target genes, preventing NF-kB activation and inhibiting inflammation in vitro and in vivo. Here we report that Andro, but not its inactive structural analog 4H-Andro, significantly suppressed the proliferation of arterial neointima （-60% reduction） in a murine model of arterial restenosis. Consistently, p50^-/- mice manifested attenuated neointimal hyperplasia upon arterial ligation. Notably, the same dosage of Andro did not further reduce neointimal formation in p50^-/- mice, which implicates the specificity of Andro on p50 for treating experimental arterial restenosis. The upregulation of NF-kB target genes, including TF, E-selectin and VCAM-1, and the increased deposition of leukocytes （mainly CD68^＋ macrophages） were clearly detected within the injured arterial walls, all of which were significantly abolished by treatment with Andro or genetic deletion of p50. The expression ofTF, E-selectin and VCAM-I was also markedly upregulated in the patient sample of thrombotic vasculitis, indicating the clinical relevance of NF-kB activation in the pathogeneses of occlusive arterial diseases. Our data thus indicate that, by the downregulation of the NF-kB target genes that are critical in thrombosis and inflammation, specific inhibitors of p50, such as Andro, may be therapeutically valuable for preventing and treating thrombotic arterial diseases, including neointimal hyperplasia in arterial restenosis.
基金the Fondazione Cassa Risparmio di Firenze for kindly supporting this review study
文摘Andrographolide (AG) is the characteristic constituent of Andrographis paniculata, of the Acanthaceae family. This plant is a well-known Asian medicinal plant that is widely used in India, China, and Thailand. A monograph of Herba Andrographidis (Chuanxinlian) is included in the Chinese Pharmacopoeia, which reports that this decoction can “remove heat, counteract toxicity, and reduce swellings.” The numerous potential activities of AG range from anti-inflammatory to anti-diabetic action, from neuroprotection to antitumor activity, and from hepatoprotective to anti-obesity properties. However, AG has low bioavailability and poor water solubility, which can limit its distribution and accumulation in the body after administration. In addition, AG is not stable in gastrointestinal alkaline and acidic environments, and has been reported to have a very short half-life. Among the diverse strategies that have been adopted to increase AG water solubility and permeability, the technological approach is the most useful way to develop appropriate delivery systems. This review reports on published studies related to microparticles (MPs) and nanoparticles (NPs) loaded with AG. MPs based on polylactic-glycolic acid (PLGA), alginic acid, and glucan derivatives have been developed for parenteral oral and pulmonary administration, respectively. NPs include vesicles (both liposomes and niosomes);polymeric NPs (based on polyvinyl alcohol, polymerized phenylboronic acid, PLGA, human serum albumin, poly ethylcyanoacrylate, and polymeric micelles);solid lipid NPs;microemulsions and nanoemulsions;gold NPs;nanocrystals;and nanosuspensions. Improved bioavailability, target-tissue distribution, and efficacy of AG loaded in the described drug delivery systems have been reported.
文摘Tumor necrosis factor-related apoptosis-inducing ligand （TRAIL） is a promising agent for anticancer therapy. The identification of small molecules that can establish the sensitivity of prostate cancer （PCa） cells to TRAIL-induced apoptosis is crucial for the targeted treatment of PCa. PC3, DU145, JAC-1, TsuPrl, and LNCaP cells were treated with Andrographolide （Andro） and TRAIL, and the apoptosis was measured using the Annexin V/PI double staining method. Real time-polymerase chain reaction （PCR） and Western blot analysis were performed to measure the expression levels of target molecules. RNA interference technique was used to down-regulate the expression of the target protein. We established a nude mouse xenograft model of PCa, which was used to measure the caspase-3 activity in the tumor cells using flow cytometry. In this research study, our results demonstrated that Andro preferentially increased the sensitivity of PCa cells to TRAIL-induced apoptosis at subtoxic concentrations, and the regulation mechanism was related to the up-regulation of DR4. In addition, it also increased the p53 expression and led to the generation of reactive oxygen species （ROS） in the cells. Further research revealed that the DR4 inhibition, p53 expression, and ROS generation can significantly reduce the apoptosis induced by the combination of TRAIL and Andro in PCa cells. In conclusion, Andro increases the sensitivity of PCa cells to TRAIL-induced apoptosis through the generation of ROS and up-regulation of p53 and then promotes PCa cell apoptosis associated with the activation of DR4.
文摘Andrographolide is a labdane diterpenoid extracted and purified from the aerial parts of plants belonging to genus Andrographis(Acanthaceae).The research has shown the plant based compound is low cytotoxic,having antimicrobial,anti-cancer,antiviral and anti-parasitic effects.Andrographolide both prevent spread as well as transmission of virus to neighboring cells by interfering with different cell signaling pathways.In addition to its medicinal value,plant has been found having nutritional value.Therefore being cost effective,easy availability and having nutritional value as a natural supplement,can be used to improve the quality of life in countries having low standard of living.Due to the limited number of effective vaccines,the plant-based antiviral drugs have provided considerable hope for fighting against the viral infections.The plant-derived compound when produced in large quantities is cost effective with low cytotoxic effects.However,much deep insight research at the molecular level is needed to develop the molecules against the viral infection.This paper aims to highlight the antiviral role of Andrographolide that can made significant contributions toward the improvement of human health and will also summarize the current status and future strategies concerning the therapeutic applications of Andrographolide to combat different viral disease in humans.
基金This work was funded by the National Key Research and Development Program of China(Grant 2017YFD0501404)the National Natural Science Foundation of China(Grant 31872521)+1 种基金the Local Innovative and Research Teams Project of Guangdong Pearl River Talents Program(Grant 2019BT02N054)the Basic Research&Applying Basic Research Foundation of Guangdong Province(Grant 2019B1515210007)。
文摘Porcine reproductive and respiratory syndrome virus(PRRSV) continues to cause significant economic loss worldwide and remains a serious threat to the pork industry. Currently, vaccination strategies provide limited protection against PRRSV infection, and consequently, new antiviral strategies are urgently required. Andrographolide(Andro) and its derivative potassium dehydrographolide succinate(PDS) have been used clinically in China and other Asian countries as therapies for inflammation-related diseases, including bacterial and viral infections, for decades. Here, we demonstrate that Andro and PDS exhibit robust activity against PRRSV replication in Marc-145 cells and primary porcine alveolar macrophages(PAMs). The two compounds exhibited broad-spectrum inhibitory activities in vitro against clinically circulating type 2 PRRSV GD-HD, XH-GD, and NADC30-like HNhx strains in China. The EC_(50)values of Andro against three tested PRRSV strain infections in Marc-145 cells ranged from 11.7 to 15.3 lmol/L, with selectivity indexes ranging from 8.3 to10.8, while the EC_(50)values of PDS ranged from 57.1 to 85.4 lmol/L, with selectivity indexes ranging from 344 to 515.Mechanistically, the anti-PRRSV activity of the two compounds is closely associated with their potent suppression on NFj B activation and enhanced oxidative stress induced by PRRSV infection. Further mechanistic investigations revealed that PDS, but not Andro, is able to directly interact with PRRSV particles. Taken together, our findings suggest that Andro and PDS are promising PRRSV inhibitors in vitro and deserves further in vivo studies in swine.
基金This research was funded by the National Natural Science Foundation of China(Grant Nos.:81891012 and U19A2010)the National Interdisciplinary Innovation TeamProgram of Traditional Chinese Medicine(Grant No.:ZYYCXTD-D-202209)+1 种基金Chinese Medicine Science and Technology Industry Innovation Team Program of Sichuan Province(Grant No.:2022C001)Chengdu University of Traditional Chinese Medicine“Xinglin Scholars”Discipline Talent Research Promotion Program(Grant No.:XCZX2022010).
文摘Atherosclerotic cardiovascular disease(ASCVD)frequently results in sudden death and poses a serious threat to public health worldwide.The drugs approved for the prevention and treatment of ASCVD are usually used in combination but are inefficient owing to their side effects and single therapeutic targets.Therefore,the use of natural products in developing drugs for the prevention and treatment of ASCVD has received great scholarly attention.Andrographolide(AG)is a diterpenoid lactone compound extracted from Andrographis paniculata.In addition to its use in conditions such as sore throat,AG can be used to prevent and treat ASCVD.It is different from drugs that are commonly used in the prevention and treatment of ASCVD and can not only treat obesity,diabetes,hyperlipidaemia and ASCVD but also inhibit the pathological process of atherosclerosis(AS)including lipid accumulation,inflammation,oxidative stress and cellular abnormalities by regulating various targets and pathways.However,the pharmacological mechanisms of AG underlying the prevention and treatment of ASCVD have not been corroborated,which may hinder its clinical development and application.Therefore,this review summarizes the physiological and pathological mechanisms underlying the development of ASCVD and the in vivo and in vitro pharmacological effects of AG on the relative risk factors of AS and ASCVD.The findings support the use of the old pharmacological compound(‘old bottle’)as a novel drug(‘novel wine’)for the prevention and treatment of ASCVD.Additionally,this review summarizes studies on the availability as well as pharmaceutical and pharmacokinetic properties of AG,aiming to provide more information regarding the clinical application and further research and development of AG.
基金financially supported by the FDCT Project 0029/2018/A1the University of Macao Research Grants(MYRG2019-00041-ICMS)performed in part at the High-Performance Computing Cluster(HPCC)which is supported by Information and Communication Technology Office(ICTO)of the University of Macao。
文摘Current formulation development strongly relies on trial-and-error experiments in the laboratory by pharmaceutical scientists,which is time-consuming,high cost and waste materials.This research aims to integrate various computational tools,including machine learning,molecular dynamic simulation and physiologically based absorption modeling(PBAM),to enhance andrographolide(AG)/cyclodextrins(CDs)formulation design.The light GBM prediction model we built before was utilized to predict AG/CDs inclusion's binding free energy.AG/γ-CD inclusion complexes showed the strongest binding affinity,which was experimentally validated by the phase solubility study.The molecular dynamic simulation was used to investigate the inclusion mechanism between AG andγ-CD,which was experimentally characterized by DSC,FTIR and NMR techniques.PBAM was applied to simulate the in vivo behavior of the formulations,which were validated by cell and animal experiments.Cell experiments revealed that the presence of D-α-Tocopherol polyethylene glycol succinate(TPGS)significantly increased the intracellular uptake of AG in MDCKMDR1 cells and the absorptive transport of AG in MDCK-MDR1 monolayers.The relative bioavailability of the AG-CD-TPGS ternary system in rats was increased to 2.6-fold and 1.59-fold compared with crude AG and commercial dropping pills,respectively.In conclusion,this is the first time to integrate various computational tools to develop a new AG-CD-TPGS ternary formulation with significant improvement of aqueous solubility,dissolution rate and bioavailability.The integrated computational tool is a novel and robust methodology to facilitate pharmaceutical formulation design.
基金supported by the National Natural Science Foundation of China(No.82270317)the Zhejiang Provincial Natural Science Foundation of China(No.LY19H020011).
文摘Atrial fibrillation(AF)is the most prevalent cardiac arrhythmia seen in clinical settings,which has been associated with substantial rates of mortality and morbidity.However,clinically available drugs have limited efficacy and adverse effects.We aimed to investigate the mechanisms of action of andrographolide(Andr)with respect to AF.We used network pharmacology approaches to investigate the possible therapeutic effect of Andr.To define the role of Andr in AF,HL-1 cells were pro-treated with Andr for 1 h before rapid electronic stimulation(RES)and rabbits were pro-treated for 1 d before rapid atrial pacing(RAP).Apoptosis,myofibril degradation,oxidative stress,and inflammation were determined.RNA sequencing(RNA-seq)was performed to investigate the relevant mechanism.Andr treatment attenuated RAP-induced atrial electrophysiological changes,inflammation,oxidative damage,and apoptosis both in vivo and in vitro.RNA-seq indicated that oxidative phosphorylation played an important role.Transmission electron microscopy and adenosine triphosphate(ATP)content assay respectively validated the morphological and functional changes in mitochondria.The translocation of nuclear factor erythroid 2-related factor 2(Nrf2)to the nucleus and the molecular docking suggested that Andr might exert a therapeutic effect by influencing the Keap1-Nrf2 complex.In conclusions,this study revealed that Andr is a potential preventive therapeutic drug toward AF via activating the translocation of Nrf2 to the nucleus and the upregulation of heme oxygenase-1(HO-1)to promote mitochondrial bioenergetics.
基金supported by the National Natural Science Foundation of China(Nos.81872823 and 82073782)the Shanghai Science and Technology Committee(No.19430741500)the Key Laboratory of Modern Chinese Medicine Preparation of Ministry of Education of Jiangxi University of Traditional Chinese Medicine,China(No.zdsys-202103)。
文摘Macrophages play a crucial role in initiating,maintaining,and resolving inflammation through the phenotypic shift,inducing or inhibiting the production of inflammatory cytokines.Therefore,macrophages are potential targets for treating inflammatory diseases.Andrographolide(AND)is a potent anti-inflammatory drug that can reduce pro-inflammatory cytokines and suppress NF-κB/MAPK pathway in activated macrophages.Although AND has many medicinal properties,its lower water solubility and first-pass effect in the liver have hindered its clinical application.In this context,by using a metal phenolic network as a stabilizer,we designed and prepared highly stabilized AND nanocrystals(AND-MPN Ns)with high drug loading capacity to facilitate the clinical application of AND.Our findings showed that AND-MPN Ns could be used to enhance the anti-inflammation in-vitro via macrophage polarization,reducing proinflammatory cytokines IL-6 and TNF-α,and suppressing the NF-κB signaling pathway activation.The results demonstrated the potential of AND-MPN Ns to combat inflammatory diseases effectively.
基金Supported by the Intensification of Research in Priority Areas Project (IRPA)Ministry of Science, Technology and Innovation,Malaysia (No.09-02-03-0101-EA0001).
文摘Andrographis paniculata Nees has been extensively used for traditional medicine and help against fever dysentery, diarrhoea, inflammation, and sore throat. In this study, andrographolide, the main component of this plant was extracted from the leaves of A. paniculata using supercritical carbon dioxide. The operating pressures were varied from 7.50 to 20MPa, the temperatures were varied from 30℃ to 60℃, and the flow rates were varied from 0.5 to 4ml.min^-1. The best extraction condition occurred at 10MPa, 40℃, and a flow rate of 2ml.min^-1 for a 3g sample of A. paniculata ground-dried leaves. The measured extraction rate was found to be about 0.0174g of andrographolide per gram of andrographolide present in the leaves per hour of operation. The future studies must focus on the interaction between the various operating parameters such as temperature, pressure, and flow rate of supercritical carbon dioxide.
基金supported by the National Natural Science Fundation of China(No.30772647)the special major science and technology project of"Creation of Major New Drugs"(No.2009ZX09102-033)
文摘A series of Andro derivatives were described and evaluated for their anti-HIV activity in vitro. Compound 10 and 16b, of which TI were 〉 10, had some anti-HIV-1 activity in vitro. Therein, compound 10 which was the best potent compound, could serve as a new lead for further development of anti-AIDS agents.
基金supported by the National Natural Science Foundation of China(No.81873079)。
文摘One-sixth of the currently known natural products containα,β-unsaturated carbonyl groups.Our previous studies reported a rare C-sulfonate metabolic pathway.Sulfonate groups were linked to theβ-carbon ofα,β-unsaturated carbonyl-based natural compounds through this pathway.However,the mechanism of this type of metabolism is still not fully understood,especially whether it is formed through enzyme-mediated biotransformation or direct sulfite addition.In this work,the enzyme-mediated and non-enzymatic pathways were studied.First,the sulfite content in rat intestine was determined by LC-MS/MS.The results showed that the amount of sulfite in rat intestinal contents was from 41.5 to 383μg·g^(-1),whereas the amount of sulfite in rat feed was lower than the lower limit of quantitation(20μg·g^(-1)).Second,the reaction kinetics of sulfite-andrographolide reactions in phosphate buffer solutions(pH 6-8)was studied.The half-lives of andrographolide ranged from minutes to hours.This was suggested that the C-sulfonate reaction of andrographolide was very fast.Third,the C-sulfonate metabolites of andrographolide were both detected when andrographolide and L-cysteine-S-conjugate andrographolide were incubated with the rat small intestine contents or sulfite,indicating that the sulfite amount in rat intestine contents was high enough to react with andrographolide,which assisted a significant portion of andrographolide metabolism.Finally,the comparison of andrographolide metabolite profiles among liver homogenate(with NADPH),liver S9(with NADPH),small intestine contents homogenate(with no NADPH),and sulfite solution incubations showed that the C-sulfonate metabolites were predominantly generated in the intestinal tract by non-enzymatic pathway.In summary,sulfite can serve as a substrate for C-sulfonate metabolism,and these results identified non-enzymatically nucleophilic addition as the potential mechanism for C-sulfonate metabolism of compounds containingα,β-unsaturated carbonyl moiety.
文摘An inclusion complex of b-cyclodextrin with andrographolide (Andro) was prepared by using a convenient method of microwave irradiation. The structure of the inclusion complex was determined by the 1H NMR, 2D NMR spectroscopy as well as the elemental analysis.
基金supported by the Guangdong Pharmacological Society of China(No.2009ZX09502-030)
文摘Andrographolide total ester sulfonate（ATES） injection is one of the products of traditional Chinese medicine（TCM） currently used against viral infection in China.ATES injection was approved for manufacturing and marketing in January 2002.It is indicated for acute respiratory infections,tonsillitis,chronic obstructive pulmonary disease,influenza,foot and mouth disease,bronchiolitis,herpangina,mumps,infectious mononucleosis and psychosis.However,its usage also carries risk.We investigated the use of ATES at the Wuhan Union Hospital from January 2014 to December 2014 and evaluated its real-world clinical application using the hospital centralized monitoring method.A total of 848 cases were enrolled in this study.In these cases,it was mainly used for postoperative anti-inflammation and treating upper respiratory infection,pneumonia and bronchitis.Among them,39.86% were contraindicated.Irregular medication of adults and children accounted for 1.91% and 23.38%,respectively.Improper choice of solvent accounted for 3.18%.The choice of intravenous drip versus aerosol inhalation was reasonable.A case of adverse events（AEs） was observed in the monitoring period,and the incidence of adverse drug reaction（ADR） of ATES injection was 0.12%.ATES injection in our hospital is relatively safe with a low incidence of adverse reactions.The study assesses the clinical usage and adverse reactions of ATES injection,and provides suggestions for rational use in clinical practice.
