The combination of Daphnes Cortex(DC)and Liquorice Root(LR),two traditional Chinese medicinal herbs,has shown significant therapeutic effects on rheumatoid arthritis(RA),but its synergistic mechanism of action remains...The combination of Daphnes Cortex(DC)and Liquorice Root(LR),two traditional Chinese medicinal herbs,has shown significant therapeutic effects on rheumatoid arthritis(RA),but its synergistic mechanism of action remains to be elucidated.Employing a network pharmacology and molecular docking approach,this study systematically investigated the synergistic mechanism of the herb pair DC and LR in RA treatment.Active components and their corresponding targets were retrieved from the TCMSP database and relevant literature,and RA-related targets were collected from established disease databases.A total of 73 overlapping targets between DC-LR and RA were identified,among which core targets such as AKT1,TNF,and CASP3 were highlighted.GO and KEGG enrichment analyses revealed that these targets are involved in biological processes such as oxidative stress response and cell migration,and are significantly enriched in key pathways including HIF-1,TNF,and PI3K-Akt signaling pathways.Compatibility analysis further revealed that the combination of DC and LR may enhance therapeutic effects through synergistic regulation of shared targets and complementary modulation of upstream and downstream pathway components.Molecular docking confirmed strong binding affinities between core active components and key targets.This study provides a multi-dimensional“component-target-pathway”perspective on the potential synergistic anti-RA mechanism of the DC-LR herb pair,offering a theoretical basis for further experimental validation and clinical application.展开更多
为了掌握芫花(Daphne genkwa Sieb. et Zucc.)1年生播种苗的生长规律,通过采用非线性回归方式对其生长曲线进行logistic模型拟合,以定性的数学模型模拟芫花苗期生长发育的变化规律。结果表明:logistic方程对芫花1年生播种苗苗高和地径...为了掌握芫花(Daphne genkwa Sieb. et Zucc.)1年生播种苗的生长规律,通过采用非线性回归方式对其生长曲线进行logistic模型拟合,以定性的数学模型模拟芫花苗期生长发育的变化规律。结果表明:logistic方程对芫花1年生播种苗苗高和地径生长曲线的拟合关系均表现为极显著,用模型的拟合结果来分析判定芫花播种苗的年周期生长规律,可把芫花的生长划分为4个时期,芫花的苗高和地径生长发育都呈现出慢、快、慢的S型生长变化规律,研究结论可为育苗经验较欠缺的新兴树种芫花的育苗提供理论基础。展开更多
AIM： To evaluate the anti-HIV activity and mechanism of action of wikstroelide M, a daphnane diterpene from Daphne acutiloba Rehder （Thymelaeaceae）. METHOD： The anti-HIV activities of wikstroelide M against differ...AIM： To evaluate the anti-HIV activity and mechanism of action of wikstroelide M, a daphnane diterpene from Daphne acutiloba Rehder （Thymelaeaceae）. METHOD： The anti-HIV activities of wikstroelide M against different HIV strains were evaluated by cytopathic effect assay and p24 quantification assay with ELISA. The inhibitory effect of wikstroelide M on HIV reverse transcription was analyzed by real-time PCR and ELISA. The effect of wikstroelide M on HIV-1 integrase nuclear translocation was observed with a cell-based imaging assay. The effect of wikstroelide M on LEDGF/p75-IN interaction was assayed by molecular docking. RESULTS： Wikstroelide M potently inhibited different HIV-1 strains, including HIV-lmn, HIV-1AI7, and HIV-19495, induced a cytopathic effect, with ECs0 values ranging from 3.81 to 15.65 ng.mL-I. Wikstroelide M also had high inhibitory activities against HIV-2noD and HIV-2cBL_20-induced cytopathic effects with ECs0 values of 18.88 and 31.90 ng.mL 1. The inhibitory activities of wikstroelide M on the three HIV-1 strains were further confirmed by p24 quantification assay, with ECs0 values ranging from 15.16 to 35.57 ng.mL-1. Wikstroelide M also potently inhibited HIV-lnm induced cytolysis in MT-4 cells, with an ECs0 value of 9.60 ng.mL ~. The mechanistic assay showed that wikstroelide M targeted HIV-I reverse transcriptase and nuclear translocation of integrase through disrupting the interaction between integrase and LEDGF/p75. CONCLUSION： Wikslroelide M may be a potent HIV-1 and HIV-2 inhibitor, the mechanisms of action may include inhibition of reverse trascriptase activity and inhibition of integrase nuclear Iranslocation through dismpting the interaction between integrase and LEDGF/p75.展开更多
Under the guidance of the approach which integrates molecular networking,MolNetEnhancer and Net-work Annotation Propagation(NAP),daphnaltaicanoids A and B(1 and 2)with unprecedented 9-oxa-tetracyclo[6.6.1.0^(2,6).0^(8...Under the guidance of the approach which integrates molecular networking,MolNetEnhancer and Net-work Annotation Propagation(NAP),daphnaltaicanoids A and B(1 and 2)with unprecedented 9-oxa-tetracyclo[6.6.1.0^(2,6).0^(8,13)]pentadecane and tetracyclo[5.3.0.1^(2,5).2^(4,11)]tridecane central frameworks were iso-lated from Daphne altaica Pall.,representing two types of unparalleled meroterpenoid cores.Their struc-tures were elucidated by extensive spectroscopic analysis,nuclear magnetic resonance(NMR)calcula-tions,DP4+analysis and electronic circular dichroism(ECD)calculations.The plausible biosynthetic path-ways for 1 and 2 were postulated.Biologically,2 exerted potent neuroprotective activities which were su-perior to trolox at 12.5 and 25μmol/L.Moreover,1 and 2 exhibited more noticeable acetylcholinesterase inhibitory activities than donepezil.Molecular docking simulations were performed to explore the inter-molecular interaction of compounds 1 and 2 with acetylcholinesterase.The bioactivity evaluation results highlight the prospects of 1 and 2 as a novel category of neurological agents.展开更多
A new daphnane diterpene was isolated from the root barks of Daphne tangutica Maxim. Its structure was elucidated as 1, 2α-dihydro-20-palimoyldaphnctoxin by the spectroscopic evidence including 2D-NMR.
Background: Daphne Mucronata extract has a decreasing effect on the size of breast adenocarcinoma in rats. So in this study, the effect of Daphne Mucronata purified diterpene were investigated on co culture of human m...Background: Daphne Mucronata extract has a decreasing effect on the size of breast adenocarcinoma in rats. So in this study, the effect of Daphne Mucronata purified diterpene were investigated on co culture of human monocytes and two human leukemia cell lines (K562, CCRF-CEM). Materials and Methods: Each cell line mono-layer culture, in log phase growth, was treated with 10 to 160 μL of the extract (1 g/ml leave powder) and purified compound (0.94 nM). For a comparative study, Taxol (5 to 40 μM) was used in the presence and absence of LPS. Human monocytes were isolated by adhesion method. TNF-α in cultured media were measured by sensitive biotin-streptoavidin ELISA method. Results: Fifty percent of growth inhibition was shown by 160 μL (1:100 dilution, 0.5 g of the powdered leaves/ml) of the extract and 0.94 nM of the purified component, and there was more inhibition in K562 cells (P < 0.05). Four fold increases in growth inhibition was shown in co culture of isolated human monocytes and leukemia cell lines. There was a direct relationship between monocytes TNF-α secretion and growth inhibition degree. Conclusion: Daphne Mucronata extract and its purified diterpene through increasing monocytes TNF-α releasing, potentially inhibit Leukemia cell line.展开更多
Objective: To investigate the analgesic and anti-inflammatory property and possible involvement of opioid receptors of ethyl acetate extract from aerial parts of Daphne mucronata(D. mucronata) in mice by formalin test...Objective: To investigate the analgesic and anti-inflammatory property and possible involvement of opioid receptors of ethyl acetate extract from aerial parts of Daphne mucronata(D. mucronata) in mice by formalin test.Methods: Single doses of 2.5, 5.0 and 10.0 mg/kg of body weight of ethyl acetate extract of D. mucronata were intraperitoneally administered to the mice 30 min before analgesic test. The anti-nociceptive effect of preparations was evaluated based on the formalin in mice.Results: The results indicated that the extract(2.5, 5.0 and 10.0 mg/kg) increased the pain threshold of mice and induced analgesia in both phases of formalin test. Like morphine sulfate(5.0 mg/kg, i.p.), the extract also showed more effective analgesic effect on the late phase of formalin test. Pre-treatment of animals with naloxone(5.0 mg/kg i.p.)did not inhibit the effects of the extract.Conclusions: Our findings suggest that D. mucronata contains potential analgesic and anti-inflammatory compounds which support its traditional use. Moreover, it seems that the analgesic and anti-inflammatory effects of the extract is mediated by non-opioid mechanisms. Further pharmacological studies are required to determine whether the analgesic mechanisms are actually responsible for such properties.展开更多
A new compound, named daphnolin （1）, was isolated from the stem barks of Daphne giraldii Nitsche. Its structure was elucidated as 8-hydroxy-7-O-β-D-glucopyranosyl-5-（2-oxo-2H-1-benzopyran-7-hydroxy-8-yloxy）-2H-1-...A new compound, named daphnolin （1）, was isolated from the stem barks of Daphne giraldii Nitsche. Its structure was elucidated as 8-hydroxy-7-O-β-D-glucopyranosyl-5-（2-oxo-2H-1-benzopyran-7-hydroxy-8-yloxy）-2H-1-benzopyran-2-one by means of NMR and MS analysis.展开更多
OBJECTIVE:To aim at preliminary phytochemical screening of Daphne mucronata and evaluate its antioxidant and antibacterial activities.METHODS:Preliminary phytochemical screening was conducted for the crude extracts us...OBJECTIVE:To aim at preliminary phytochemical screening of Daphne mucronata and evaluate its antioxidant and antibacterial activities.METHODS:Preliminary phytochemical screening was conducted for the crude extracts using standard methods.Antioxidant properties of crude methanolic extracts,n-hexane,chloroform,ethyl acetate and aqueous fractions of leaves,roots and bark were evaluated following standard procedures.The antibacterial activities were checked against Acinetobacter baumannii(A.baumannii),Escherichia coli(E.coli),Pseudomonas aeruginosa(P.aeruginosa),Staphylococcus aureus(S.aureus),Morganella morganii(M.morganii)and vancomycin resistant S.aureus(VRSA).RESULTS:Carbohydrates,saponins,steroids,phenols/tannins,flavonoids and glycosides were present in different parts of Daphne mucronata.The extracts showed good antioxidant activity with EC50 values of 157.82-361.61μg/m L.Methanolic extracts of roots showed good activity against A.baumannii(86.95%),E.coli(85.18%)and S.aureus(84.61%).Methanolic extracts of bark were active against A.bumanni(65.21%),M.morganii(65.21%)and E.coli(62.96%).Methanolic extracts of leaves showed good activity against A.bumanni(78.26%),E.coli(77.78%),P.aeruginosa(74.07%),S.aureus(73.07%),M.morganii(69.56%),VRSA(68%)and Proteus vulgaris(60%).The n-hexane fraction of roots was effective against A.bumanni(78.26%).Chlorofom fraction of roots showed moderate activity against A.bumanni(60.86%)and S.aureus(61.53%).Ethyl acetate fraction of roots showed moderate activity against A.bumanii(69.56%),E.coli(62.96%)and S.aureus(69.23%).CONCLUSION:This study illustrates that Daphne mucronata possesses good antioxidant and antibacterial properties.The plant could be further exploited as potential natural antioxidant and as a new source of antimicrobials for treatment of various infections.展开更多
基金supported by National Training Program of Innovation and Entrepreneurship for Undergraduates(202510163044).
文摘The combination of Daphnes Cortex(DC)and Liquorice Root(LR),two traditional Chinese medicinal herbs,has shown significant therapeutic effects on rheumatoid arthritis(RA),but its synergistic mechanism of action remains to be elucidated.Employing a network pharmacology and molecular docking approach,this study systematically investigated the synergistic mechanism of the herb pair DC and LR in RA treatment.Active components and their corresponding targets were retrieved from the TCMSP database and relevant literature,and RA-related targets were collected from established disease databases.A total of 73 overlapping targets between DC-LR and RA were identified,among which core targets such as AKT1,TNF,and CASP3 were highlighted.GO and KEGG enrichment analyses revealed that these targets are involved in biological processes such as oxidative stress response and cell migration,and are significantly enriched in key pathways including HIF-1,TNF,and PI3K-Akt signaling pathways.Compatibility analysis further revealed that the combination of DC and LR may enhance therapeutic effects through synergistic regulation of shared targets and complementary modulation of upstream and downstream pathway components.Molecular docking confirmed strong binding affinities between core active components and key targets.This study provides a multi-dimensional“component-target-pathway”perspective on the potential synergistic anti-RA mechanism of the DC-LR herb pair,offering a theoretical basis for further experimental validation and clinical application.
文摘为了掌握芫花(Daphne genkwa Sieb. et Zucc.)1年生播种苗的生长规律,通过采用非线性回归方式对其生长曲线进行logistic模型拟合,以定性的数学模型模拟芫花苗期生长发育的变化规律。结果表明:logistic方程对芫花1年生播种苗苗高和地径生长曲线的拟合关系均表现为极显著,用模型的拟合结果来分析判定芫花播种苗的年周期生长规律,可把芫花的生长划分为4个时期,芫花的苗高和地径生长发育都呈现出慢、快、慢的S型生长变化规律,研究结论可为育苗经验较欠缺的新兴树种芫花的育苗提供理论基础。
基金supported,in part,by grants from the National Natural Science Foundation of China(Nos.81102483,81001462)the 973 Program(No.2009CB522306)the Key Scientific and Technological Program of China(Nos.2009-ZX09501-029,2012ZX10001-006,2012ZX10001-007,2012ZX-09103-101-022),and Yunnan(No.2010GA001)
文摘AIM： To evaluate the anti-HIV activity and mechanism of action of wikstroelide M, a daphnane diterpene from Daphne acutiloba Rehder （Thymelaeaceae）. METHOD： The anti-HIV activities of wikstroelide M against different HIV strains were evaluated by cytopathic effect assay and p24 quantification assay with ELISA. The inhibitory effect of wikstroelide M on HIV reverse transcription was analyzed by real-time PCR and ELISA. The effect of wikstroelide M on HIV-1 integrase nuclear translocation was observed with a cell-based imaging assay. The effect of wikstroelide M on LEDGF/p75-IN interaction was assayed by molecular docking. RESULTS： Wikstroelide M potently inhibited different HIV-1 strains, including HIV-lmn, HIV-1AI7, and HIV-19495, induced a cytopathic effect, with ECs0 values ranging from 3.81 to 15.65 ng.mL-I. Wikstroelide M also had high inhibitory activities against HIV-2noD and HIV-2cBL_20-induced cytopathic effects with ECs0 values of 18.88 and 31.90 ng.mL 1. The inhibitory activities of wikstroelide M on the three HIV-1 strains were further confirmed by p24 quantification assay, with ECs0 values ranging from 15.16 to 35.57 ng.mL-1. Wikstroelide M also potently inhibited HIV-lnm induced cytolysis in MT-4 cells, with an ECs0 value of 9.60 ng.mL ~. The mechanistic assay showed that wikstroelide M targeted HIV-I reverse transcriptase and nuclear translocation of integrase through disrupting the interaction between integrase and LEDGF/p75. CONCLUSION： Wikslroelide M may be a potent HIV-1 and HIV-2 inhibitor, the mechanisms of action may include inhibition of reverse trascriptase activity and inhibition of integrase nuclear Iranslocation through dismpting the interaction between integrase and LEDGF/p75.
基金supported by the National Natural Science Foundation of China(Nos.82073736,81872766)Science and Technology Planning Project of Liaoning Province(No.2021JH1/10400049)Liaoning revitalization talents program(Nos.XLYC2002066,XLYC2007180).
文摘Under the guidance of the approach which integrates molecular networking,MolNetEnhancer and Net-work Annotation Propagation(NAP),daphnaltaicanoids A and B(1 and 2)with unprecedented 9-oxa-tetracyclo[6.6.1.0^(2,6).0^(8,13)]pentadecane and tetracyclo[5.3.0.1^(2,5).2^(4,11)]tridecane central frameworks were iso-lated from Daphne altaica Pall.,representing two types of unparalleled meroterpenoid cores.Their struc-tures were elucidated by extensive spectroscopic analysis,nuclear magnetic resonance(NMR)calcula-tions,DP4+analysis and electronic circular dichroism(ECD)calculations.The plausible biosynthetic path-ways for 1 and 2 were postulated.Biologically,2 exerted potent neuroprotective activities which were su-perior to trolox at 12.5 and 25μmol/L.Moreover,1 and 2 exhibited more noticeable acetylcholinesterase inhibitory activities than donepezil.Molecular docking simulations were performed to explore the inter-molecular interaction of compounds 1 and 2 with acetylcholinesterase.The bioactivity evaluation results highlight the prospects of 1 and 2 as a novel category of neurological agents.
文摘A new daphnane diterpene was isolated from the root barks of Daphne tangutica Maxim. Its structure was elucidated as 1, 2α-dihydro-20-palimoyldaphnctoxin by the spectroscopic evidence including 2D-NMR.
文摘Background: Daphne Mucronata extract has a decreasing effect on the size of breast adenocarcinoma in rats. So in this study, the effect of Daphne Mucronata purified diterpene were investigated on co culture of human monocytes and two human leukemia cell lines (K562, CCRF-CEM). Materials and Methods: Each cell line mono-layer culture, in log phase growth, was treated with 10 to 160 μL of the extract (1 g/ml leave powder) and purified compound (0.94 nM). For a comparative study, Taxol (5 to 40 μM) was used in the presence and absence of LPS. Human monocytes were isolated by adhesion method. TNF-α in cultured media were measured by sensitive biotin-streptoavidin ELISA method. Results: Fifty percent of growth inhibition was shown by 160 μL (1:100 dilution, 0.5 g of the powdered leaves/ml) of the extract and 0.94 nM of the purified component, and there was more inhibition in K562 cells (P < 0.05). Four fold increases in growth inhibition was shown in co culture of isolated human monocytes and leukemia cell lines. There was a direct relationship between monocytes TNF-α secretion and growth inhibition degree. Conclusion: Daphne Mucronata extract and its purified diterpene through increasing monocytes TNF-α releasing, potentially inhibit Leukemia cell line.
基金supported by a Pharmaceutical Sciences Branch, Islamic Azad University (IAUPS) Grant
文摘Objective: To investigate the analgesic and anti-inflammatory property and possible involvement of opioid receptors of ethyl acetate extract from aerial parts of Daphne mucronata(D. mucronata) in mice by formalin test.Methods: Single doses of 2.5, 5.0 and 10.0 mg/kg of body weight of ethyl acetate extract of D. mucronata were intraperitoneally administered to the mice 30 min before analgesic test. The anti-nociceptive effect of preparations was evaluated based on the formalin in mice.Results: The results indicated that the extract(2.5, 5.0 and 10.0 mg/kg) increased the pain threshold of mice and induced analgesia in both phases of formalin test. Like morphine sulfate(5.0 mg/kg, i.p.), the extract also showed more effective analgesic effect on the late phase of formalin test. Pre-treatment of animals with naloxone(5.0 mg/kg i.p.)did not inhibit the effects of the extract.Conclusions: Our findings suggest that D. mucronata contains potential analgesic and anti-inflammatory compounds which support its traditional use. Moreover, it seems that the analgesic and anti-inflammatory effects of the extract is mediated by non-opioid mechanisms. Further pharmacological studies are required to determine whether the analgesic mechanisms are actually responsible for such properties.
文摘A new compound, named daphnolin （1）, was isolated from the stem barks of Daphne giraldii Nitsche. Its structure was elucidated as 8-hydroxy-7-O-β-D-glucopyranosyl-5-（2-oxo-2H-1-benzopyran-7-hydroxy-8-yloxy）-2H-1-benzopyran-2-one by means of NMR and MS analysis.
文摘OBJECTIVE:To aim at preliminary phytochemical screening of Daphne mucronata and evaluate its antioxidant and antibacterial activities.METHODS:Preliminary phytochemical screening was conducted for the crude extracts using standard methods.Antioxidant properties of crude methanolic extracts,n-hexane,chloroform,ethyl acetate and aqueous fractions of leaves,roots and bark were evaluated following standard procedures.The antibacterial activities were checked against Acinetobacter baumannii(A.baumannii),Escherichia coli(E.coli),Pseudomonas aeruginosa(P.aeruginosa),Staphylococcus aureus(S.aureus),Morganella morganii(M.morganii)and vancomycin resistant S.aureus(VRSA).RESULTS:Carbohydrates,saponins,steroids,phenols/tannins,flavonoids and glycosides were present in different parts of Daphne mucronata.The extracts showed good antioxidant activity with EC50 values of 157.82-361.61μg/m L.Methanolic extracts of roots showed good activity against A.baumannii(86.95%),E.coli(85.18%)and S.aureus(84.61%).Methanolic extracts of bark were active against A.bumanni(65.21%),M.morganii(65.21%)and E.coli(62.96%).Methanolic extracts of leaves showed good activity against A.bumanni(78.26%),E.coli(77.78%),P.aeruginosa(74.07%),S.aureus(73.07%),M.morganii(69.56%),VRSA(68%)and Proteus vulgaris(60%).The n-hexane fraction of roots was effective against A.bumanni(78.26%).Chlorofom fraction of roots showed moderate activity against A.bumanni(60.86%)and S.aureus(61.53%).Ethyl acetate fraction of roots showed moderate activity against A.bumanii(69.56%),E.coli(62.96%)and S.aureus(69.23%).CONCLUSION:This study illustrates that Daphne mucronata possesses good antioxidant and antibacterial properties.The plant could be further exploited as potential natural antioxidant and as a new source of antimicrobials for treatment of various infections.
