To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bisp...To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bispyridylanthrahydrazone(9,10‑PAH)were designed and synthesized.Utilizing 9‑PAH and 9,10‑PAH as promising anticancer ligands,their respective copper complexes,namely[Cu(L1)Cl_(2)]Cl(1)and{[Cu_(4)(μ_(2)‑Cl)_(3)Cl_(4)(9,10‑PAH)_(2)(DMSO)_(2)]Cl_(2)}_(n)(2),were subsequently synthesized,where the new ligand L1 is formed by coupling two 9‑PAH ligands in the coordination reaction.The chemical and crystal structures of 1 and 2 were elucidated by IR,MS,elemental analysis,and single‑crystal X‑ray diffraction.Complex 1 forms a mononuclear structure.L1 coordinates with Cu through its three N atoms,together with two Cl atoms,to form a five‑coordinated square pyramidal geometry.Complex 2 constitutes a polymeric structure,wherein each structural unit centrosymmetrically encompasses two five‑coordinated binuclear copper complexes(Cu1,Cu2)of 9,10‑PAH,with similar square pyramidal geometry.A chlorine atom(Cl_(2)),located at the symmetry center,bridges Cu1 and Cu1A to connect the two binuclear copper structures.Meanwhile,the two five‑coordinated Cu2 atoms symmetrically bridge the adjacent structural units via one coordinated Cl atom,respectively,thus forming a 1D chain‑like polymeric structure.In vitro anticancer activity assessments revealed that 1 and 2 showed significant cytotoxicity even higher than cisplatin.Specifically,the IC_(50)values of 2 against HeLa‑229 and SK‑OV‑3 cancer cell lines were determined to be(5.92±0.32)μmol·L^(-1)and(6.48±0.39)μmol·L^(-1),respectively.2 could also block the proliferation of HeLa‑229 cells in S phase and significantly induce cell apoptosis.In addition,fluorescence quenching competition experiments suggested that 2 might interact with DNA by an intercalative binding mode,offering insights into its underlying anticancer mechanism.CCDC:2388918,1;2388919,2.展开更多
Cardamonin is a natural chalcone that has been extensively investigated for its anticancer activity.However,its clinical relevance is still not explicit,limiting its progression into clinical trials and highlighting a...Cardamonin is a natural chalcone that has been extensively investigated for its anticancer activity.However,its clinical relevance is still not explicit,limiting its progression into clinical trials and highlighting a persistent gap between preclinical evidence and practical application.This review aims to assess the readiness of cardamonin to progress from laboratory research to clinical application as an anticancer agent by examining both scientific evidence and translational challenges.Preclinical pharmacokinetic and pharmacodynamic data suggest that cardamonin’s therapeutic potential as an anticancer agent is hindered by its poor oral bioavailability.Although its molecular targets remain undefined,evidence indicates that cardamonin can inhibit various signaling pathways,including nuclear factor kappa-light-chain-enhancer of activated B cells,mammalian target of rapamycin,signal transducer and activator of transcription 3,and Wnt/β-catenin.The lack of in vivo toxicity studies creates uncertainty regarding the balance between its therapeutic benefits and potential adverse effects when moving from laboratory research to human trials.Despite these limitations,cardamonin has,however,demonstrated antiproliferative,anti-metastatic,and chemosensitizing effects,mainly against breast,colorectal,and ovarian cancers.Nevertheless,exploring its combination with standard chemotherapeutic agents may offer a promising foundation for advancing cardamonin into clinical trials.展开更多
Terpenes are a structurally diverse family of secondary metabolites found mostly in plants and microorganisms.Beta-caryophyllene and d-limonene are abundant in aromatic medicinal plants.Beta-caryophyllene can be sourc...Terpenes are a structurally diverse family of secondary metabolites found mostly in plants and microorganisms.Beta-caryophyllene and d-limonene are abundant in aromatic medicinal plants.Beta-caryophyllene can be sourced from clove and cannabis amongst others,and d-limonene is abundant in the Citrus genera.Apart from their use in agriculture,cosmetics,and food industries,these terpenes possess a wide range of therapeutic activities,including antimicrobial,analgesic,and anticancer activities.This review discusses the anticancer effects of these two compounds against malignant tumors including breast,lung,gastrointestinal,bone,blood,endometrial,and bladder cancer.Beta-caryophyllene induces apoptosis and prevents proliferation and metastasis through the downregulation of HSP60,HTRA,survivin,XIAP,Bcl-xL,and Bcl-2 and the upregulation of caspase 3,annexin V,p21,Bad,Bak,and Bax.The anticancer activity is also mediated by G1/M arrest,ROS induction,and JAK1/STAT activation.d-Limonene exerts its anticancer effects by upregulating autophagy-linked genes,Bax,and caspase 3 and downregulating cyclin D1 and Bcl-2.These compounds also elicit synergistic effects upon co-administration with anticancer drugs and show great prospects as useful agents in the fight against cancer.展开更多
Background:The increasing incidence of cancers and infectious diseases worldwide presents a significant public health challenge that requires immediate intervention.Our strategy to tackle this issue involves the devel...Background:The increasing incidence of cancers and infectious diseases worldwide presents a significant public health challenge that requires immediate intervention.Our strategy to tackle this issue involves the development of pharmaceutical formulations that combine phytopolyphenols(P),targeted drugs(T),and metal ions(M),collectively referred to as PTM regimens.The diverse pharmacological properties of PTM regimens are hypothesized to effectively reduce the risk factors associated with both cancers and infectious diseases.Methods:The effects of the pharmaceutical agents on the proliferation of cultured cancer cells and pathogens were assessed after 72 h and 48 h,respectively,using the MTT(3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide)assay and optical density at 600 nm(OD600).The synergistic effects of drug combinations were evaluated by combination index(CI),where CI<1 indicates synergism,CI=1 indicates addition,and CI>1 indicates antagonism.Efficacy index(EI)was also calculated.Assays of efflux pump ATPase activities were conducted using a colorimetric method.Results:This study evaluated the anticancer and antibacterial efficacy of PTM regimens that included phytopolyphenols(specifically curcumin(C)and green tea polyphenols(G)),repurposed drugs(memantine(Mem),thioridazine(TRZ),cisplatin(Cis),and 5-fluorouracil(5FU)),and ZnSO_(4)(Zn)across three cultured cancer cell lines and four cultured pathogens.The most effective regimens,GC·Mem·Zn and GC·TRZ·Zn,significantly enhanced the anticancer efficacy(EI)of cisplatin across the three cancer lines(OECM-1,A549 and DLD-1)by 7,11 and 21;7,9,and 17 fold,respectively,while the enhancements for 5-fluorouracil were 5,6 and 12;5,5 and 9 fold,respectively.Furthermore,these PTM regimens demonstrated substantial synergistic inhibition of Na^(+)-K^(+)-Mg^(2+)-ATPase and Mg^(2+)-ATPase in the cultured cancer cells,as well as a reduction in biofilm formation by the four cultured pathogens,suggesting their potential to address the challenges of multidrug resistance in cancers and infectious diseases.Conclusion:Given that all drugs incorporated in the PTM regimens have been clinically validated for safety and efficacy,particularly regarding their synergistic selective anticancer efficacy,inhibition of efflux pump ATPase,and antibiofilm formation of pathogens,these regimens may offer a promising therapeutic strategy to alleviate the severe side effects and drug resistance typically associated with chemotherapeutic agents.Further preclinical and clinical investigations are warranted.展开更多
Marine natural products have long been recognized as a vast and diverse source of bioactive compounds with potential therapeutic applications,particularly in oncology.This review provides an updated overview of the si...Marine natural products have long been recognized as a vast and diverse source of bioactive compounds with potential therapeutic applications,particularly in oncology.This review provides an updated overview of the significant advances made in the discovery and development of marine-derived anticancer drugs between 2019 and 2023.With a focus on recent research findings,the review explores the rich biodiversity of marine organisms,including sponges,corals,algae,and microorganisms,which have yielded numerous compounds exhibiting promising anticancer properties.Emphasizing the multifaceted mechanisms of action,the review discusses the molecular targets and pathways targeted by these compounds,such as cell cycle regulation,apoptosis induction,angiogenesis inhibition,and modulation of signaling pathways.Additionally,the review highlights the innovative strategies employed in the isolation,structural elucidation,and chemical modification of marine natural products to enhance their potency,selectivity,and pharmacological properties.Furthermore,it addresses the challenges and opportunities associated with the development of marine-derived anticancer drugs,including issues related to supply,sustainability,synthesis,and clinical translation.Finally,the review underscores the immense potential of marine natural products as a valuable reservoir of novel anticancer agents and advocates for continued exploration and exploitation of the marine environment to address the unmet medical needs in cancer therapy.展开更多
Rice callus suspension culture(RCSC)has been shown to have anticancer activity based on cytotoxic activity on human colon and lung cancer cell lines.In the present study,the effect of RCSC on the expression of protein...Rice callus suspension culture(RCSC)has been shown to have anticancer activity based on cytotoxic activity on human colon and lung cancer cell lines.In the present study,the effect of RCSC on the expression of proteins in lung(A549)and colon(HT29)cancer cell lines was examined by using proteomics analysis.The protein-protein interaction study of differentially expressed proteins was done by using the Search Tool for the Retrieval of Interacting Genes(STRING),and the results showed that the proteins interacting with each other belong to different pathways.展开更多
The anticancer potential of quassinoids has attracted a great deal of attention for decades,and scientific data revealing their possible applications in cancer management are continuously increasing in the literature....The anticancer potential of quassinoids has attracted a great deal of attention for decades,and scientific data revealing their possible applications in cancer management are continuously increasing in the literature.Aside from the potent cytotoxic and antitumor properties of these degraded triterpenes,several quassinoids have exhibited synergistic effects with anticancer drugs.This article provides an overview of the potential anticancer properties of quassinoids,including their cytotoxic and antitumor activities,mechanisms of action,safety evaluation,and potential benefits in combination with anticancer drugs.展开更多
Tissue culture techniques were used to produce large amounts of bioactive compounds with medicinal potential, overcoming space and time constraints for cancer prevention. Rice callus suspension cultures(RCSC) and seed...Tissue culture techniques were used to produce large amounts of bioactive compounds with medicinal potential, overcoming space and time constraints for cancer prevention. Rice callus suspension cultures(RCSC) and seed extracts prepared from aromatic rice varieties were used to evaluate the cytotoxic impact on human colon and lung cancer cell lines, as well as a normal control cell line, using Taxol as a positive control. RCSC and seed extracts from two Indian aromatic rice varieties were applied at different concentrations to treat the cancer cell lines and normal lung fibroblasts over varying time intervals. Apoptosis was assessed in 1:5 dilutions of the A549 and HT-29 cell lines treated with RCSC for 72 h, using propidium iodide staining and flow cytometry. RCSC showed a more potent cytotoxic effect than seed extracts with minimal effect on the normal cell line, in contrast to Taxol. Confocal microscopy and flow cytometry further confirmed the apoptotic effect of RCSC. Gas chromatography-mass spectrometry-based metabolic profiling identified metabolites involved in cytotoxicity and highlighted altered pathways. RCSC is proposed as an alternative source for the development of novel anticancer drugs with reduced side effects.展开更多
Photodynamic therapy(PDT)is a promising cancer treatment modality owing to its high spatiotempora selectivity and noninvasive nature.However,conventional photosensitizers(PSs)used in PDT are respon sive only to visibl...Photodynamic therapy(PDT)is a promising cancer treatment modality owing to its high spatiotempora selectivity and noninvasive nature.However,conventional photosensitizers(PSs)used in PDT are respon sive only to visible light,which makes them unsuitable for tissue penetration.In this study,we propose a PS based on hot band absorption(HBA),which can be triggered by anti-Stokes light at 808 nm via a one-photon process.The introduction of selenium(Se)into pentamethine cyanine(Secy5)not only facili tates intersystem crossing for reactive oxygen species(ROS)production but also enhances HBA efficiency thereby prolonging the excitation wavelength.In addition,Secy5 demonstrates excellent biocompatibility unlike its I-substituted counterpart(Icy5),and produces not only^(1)O_(2)but also O_(2)^(·-),making it a desirable candidate for treating hypoxic solid tumors.According to the results of in vivo and in vitro experiments Secy5 can efficiently inhibit cancer cell growth via anti-Stokes activation processes,thereby providing a novel approach to design anti-Stokes excitation PSs for anticancer treatment.展开更多
Objective:To evaluate the anticancer potential of Cymbopogon citratus extract.Methods:GC-MS analysis was used to identify phytocomponents in the methanolic extract of Cymbopogon citratus.A fractionation method was emp...Objective:To evaluate the anticancer potential of Cymbopogon citratus extract.Methods:GC-MS analysis was used to identify phytocomponents in the methanolic extract of Cymbopogon citratus.A fractionation method was employed to isolate and assess the bioactivity of different fractions and their cytotoxic activities against cancer cell lines HCT116,LoVo,Caco-2,and HT-29 were investigated.A dual staining method with acridine orange and ethidium bromide was used to assess the effect of the extract on cell apoptosis.Additionally,the expression levels of Bax and TP53 were quantified using real-time PCR in Caco-2 cells treated with the ethyl acetate fraction of Cymbopogon citratus extract.A protein array was employed to profile key pro-and anti-apoptotic proteins in Caco-2 cells.Moreover,molecular docking studies were conducted to investigate the interactions between key compounds of Cymbopogon citratus extract and specific apoptosis-related protein domains(PDB IDs:7wql and 4bkx).Results:A significant growth inhibition was observed in Caco-2 cells treated with Cymbopogon citratus extract.Among the seven fractions of the plant extract,the ethyl acetate fraction showed the highest cytotoxicity against Caco-2 cells with an IC50 value of(6.16±0.01)μg/mL.The immunofluorescence assay showed that the ethyl acetate fraction could induce apoptosis of Caco-2 cells.Moreover,the fraction upregulated the gene expressions of Bax and TP53 in a dose-dependent manner.The docking analysis demonstrated the interaction of five compounds isolated from the ethyl acetate fraction with key proteins in Caco-2 cells,indicating their anticancer properties.Conclusions:Cymbopogon citratus extract shows anticancer activity against Caco-2 cells by inducing apoptosis.It may be a promising candidate for the treatment of colon cancer,which needs further investigation.展开更多
BACKGROUND Colon cancer(CC)is one of the most common malignant tumors in the gastrointestinal system.Overall,CC had the third highest incidence but the second highest mortality rate globally in 2020.Nowadays,CC is mai...BACKGROUND Colon cancer(CC)is one of the most common malignant tumors in the gastrointestinal system.Overall,CC had the third highest incidence but the second highest mortality rate globally in 2020.Nowadays,CC is mainly treated with capecitabine chemotherapy regimen,supplemented by radiotherapy,immunotherapy and targeted therapy,but there are still limitations,so Chinese medicine plays an important role.AIM To investigate the effects of invigorating-spleen and anticancer prescription(ISAP)on body weight,tumor inhibition rate and expression levels of proteins in extracellular-signal-regulated kinase(ERK)/mitogen-activated protein kinase(MAPK)signaling pathway in CC mice model.METHODS The CC mice model were established and the mice were randomly divided into 5 groups,including the control group,capecitabine group,the low-dose,mediumdose and high-dose groups of ISAP,with 8 mice in each group,respectively.After 2 weeks of intervention,the body weight and tumor inhibition rate of mice were observed,and the expression of RAS,ERK,phosphorylated ERK(p-ERK),C-MYC and matrix metalloproteinase 2(MMP2)proteins in the tissues of tumors were detected.RESULTS Compared with the control group,the differences of body weight before and after treatment was much smaller in the groups of ISAP,with the smallest difference in the high-dose group of ISAP,while the capecitabine group had the greatest difference,indicating ISAP had a significant inhibiting effect on the growth of transplanted tumor in mice.The expression of RAS protein was decreased in the low-and medium-dose groups of ISAP,and the change of p-ERK was significant in the medium-and high-dose groups of ISAP.MMP2 protein expression was significantly decreased in both the low-dose and medium-dose groups of ISAP.There were no significant changes in ERK in the ISAP group compared to the capecitabine group,while RAS,MMP2,and C-MYC protein expression were reduced in the ISAP group.The expression level of C-MYC protein decreased after treated with ISAP,and the decrease was the most significant in the medium-dose group of ISAP.CONCLUSION ISAP has a potential inhibiting effect on transplanted tumor in mice,and could maintain the general conditions,physical strength and body weight of mice.The expression levels of RAS,p-ERK,MMP2 and c-myc were also decreased to a certain extent.By inhibiting the expression of upstream proteins,the expression levels of downstream proteins in ERK/MAPK signaling pathway were significantly decreased.Therefore,it can be concluded that ISAP may exert an anti-tumor effect by blocking the ERK/MAPK signaling pathway and inhibiting the expression of MMP2 and c-myc proteins.展开更多
Koumine is an indole alkaloid monomer extracted from the Chinese herb Gelsemium elegans,which has a variety of pharmacological effects.This paper provides a comprehensive summary of the pharmacological effects and mol...Koumine is an indole alkaloid monomer extracted from the Chinese herb Gelsemium elegans,which has a variety of pharmacological effects.This paper provides a comprehensive summary of the pharmacological effects and molecular mechanisms of koumine,with a particular emphasis on its mechanisms of action in the context of anticancer,anti-inflammatory,analgesic,and anxiolytic properties.The aim is to provide a theoretical foundation for further research and the application of koumine in clinical practice.展开更多
Among microorganisms,fungi are the ones that have the most imagination in producing secondary metabolites with the most varied structural differences,which are produced through different biosynthetic pathways.Therefor...Among microorganisms,fungi are the ones that have the most imagination in producing secondary metabolites with the most varied structural differences,which are produced through different biosynthetic pathways.Therefore,they synthesize secondary metabolites classifiable into numerous families of natural compounds such as amino acids,alkaloids,anthraquinones,aromatic compounds,cyclohexene epoxides,furanones,macrolides,naphthoquinones,polyketides,pyrones,terpenes,etc.They also produced metabolites with very complex structures that can not be classified in the known families of natural compounds.Many fungal metabolites show different biological activities with potential applications in agriculture,food chemistry,cosmetics,pharmacology and medicine.This review is focused on the fungal secondary metabolites with anticancer activity isolated in the last ten years.For some metabolites,when described,their biosynthetic origin,the mode of action and the results of structure activity relationships studies are also reported.展开更多
Cancer occurs when the body’s cells grow beyond the usual control. Normal body cells multiply in a controlled manner and undergo apoptosis when the body no longer needs them. Different types of cancers exist, and the...Cancer occurs when the body’s cells grow beyond the usual control. Normal body cells multiply in a controlled manner and undergo apoptosis when the body no longer needs them. Different types of cancers exist, and the common ones include breast, cervical, prostate, lung, colon, and skin cancers. Several factors have been associated with cancers, and these factors include poor dieting, exposure to harmful chemicals and radiation, weak immune system, and genetics. Cancer presents an enormous health threat in the modern world and thus the need to identify an effective treatment. The conventional treatments used in the management of cancer include chemotherapy and physiotherapy. These forms of cancer treatments usually have enormous side effects on the subjects. In this respect, an alternative form of treatment would be effective in managing cancer patients. A substantial number of natural products have been observed to be effective in the management of cancer. These natural products include plants and other natural substances such as honey. This study focuses on the efficiency of natural products in the treatment of cancer. Also, the anticancer effects of Peganum harmala, Manuka honey, and Saudi honey will be analyzed. Bee honey and Peganum harmala have been traditionally used in the treatment of cancer. The extracts from Peganum harmala plant have also been shown to exhibit divers’ antitumor effects similar to the mode of action of a vast number of anticancer agents. These established hypotheses thus give the rationale for this study. In this experiment, extracts were obtained from Peganum harmala leaves and exposed to cervical, lung, and prostate cancer cells. Similarly, solutions of Manuka honey and Saudi honey were exposed to the cervical, lung, and prostate cancer cells. The experiment duration was 24 hours, which obtained results were recorded and analyzed. Peganum harmala extracts inhibit cancer cell growth at different and achievable concentrations. Manuka honey highly inhibits the growth of HeLa cancer cells while Saudi honey highly inhibits the growth of A549 cells. Peganum harmala can form an effective treatment for managing several types of cancers. Manuka Honey can be applied as an effective treatment for managing cervical cancer while Saudi honey can form an effective treatment for managing lung cancers.展开更多
Purpose:This research aimed to identify leading factors that affect nurses’compliance with the safe handling of anticancer agents.Methods:Data were collected from 114 nurses working in the university hospital and wer...Purpose:This research aimed to identify leading factors that affect nurses’compliance with the safe handling of anticancer agents.Methods:Data were collected from 114 nurses working in the university hospital and were analyzed through independent t-test,one-way ANOVA,Pearson’s correlation coefficient,and multiple regression analysis using SPSS25.0.Results:The average level of compliance with the safe handling of anticancer agents was 3.73±0.33 out of 5 points.Workplace safety culture(β=0.40,P<0.001)and knowledge of safe handling(β=0.18,P=0.030)had significant influences on nurses’compliance with the safe handling of anticancer agents.The explained variance for compliance was 28.3%.Conclusion:To enhance the implementation of safety management for anticancer agents,each institution should strive to support human and material resources and enhance specialization in the workplace safety culture through system improvement.Based on the results of this study,we suggest research for the development of a training program for anticancer agent safety management.展开更多
Calotropisprocera(Cp)is a traditional medicinal plant that has attracted significant attention for its potential anticancer properties.This review consolidates current research on the Cp bioactive compounds found in C...Calotropisprocera(Cp)is a traditional medicinal plant that has attracted significant attention for its potential anticancer properties.This review consolidates current research on the Cp bioactive compounds found in Cp,including cardenolides,flavonoids,and terpenoids,which exhibit cytotoxic effects against various cancer cells.These compounds function through multiple mechanisms,such as inducing apoptosis,inhibiting cell proliferation,suppressing angiogenesis,and modulating oxidative stress.Preclinical studies demonstrate that Cp extracts effectively reduce tumor size and improve survival rates in animal models.Furthermore,Cp influences key signaling pathways like PI3K/Akt and NF-κB,which contribute to its anticancer potential.Its therapeutic effects extend beyond oncology,encompassing,antinociceptive,anticonvulsant,antimalarial,anthelmintic,antioxidant,antidiabetic,myocardial infarction prevention,schizontocidal,antimicrobial,anti-inflammatory,larvicidal,immunomodulatory,antiulcer,Antifertility,antidiarrheal,estrogenic,and Dermatophytic properties.Despite the promising preclinical data,further investigation is necessary to address challenges such as bioavailability,toxicity,and the standardization of Cp-based treatments.This review highlights the therapeutic promise of Cp as a complementary anticancer agent while emphasizing the need for rigorous clinical trials to confirm its safety and efficacy.展开更多
Caffeic acid phenethyl ester (CAPE) and sixteen substituted cinnamic acid phenethyl esters were prepared via conventional procedures in order to test their in vitro anticancer activities by either MTT assay or SRB...Caffeic acid phenethyl ester (CAPE) and sixteen substituted cinnamic acid phenethyl esters were prepared via conventional procedures in order to test their in vitro anticancer activities by either MTT assay or SRB assay on six different human cancer cell lines. The results indicated that in the concentration of 10 μmol·L -1 the lead compound CAPE possessed anticancer activities against human HL 60, Bel 7402, and Hela cell lines, and two other compounds possessed potent anticancer activities against Bel 7402 and Hela cell lines.展开更多
Aim To investigate the anticancer activity of two new cytotoxins from thevenom of Agkistrodon acutus. Methods The venom was isolated by FPLC column chromatography consistingof DEAE Sepharose FF and Source 30S. The cyt...Aim To investigate the anticancer activity of two new cytotoxins from thevenom of Agkistrodon acutus. Methods The venom was isolated by FPLC column chromatography consistingof DEAE Sepharose FF and Source 30S. The cytotoxic activity on tumor cells was detected by MITmethod. Purity and molecular weight were determined by SDS-PAGE (silver staining). Their stabilitiesto temperature and pH were also detected. Results Two pure cytotoxins named ACTX-6 and ACTX-8 wereobtained. Their molecular weights are 98 kDa and 27 kDa, respectively. ACTX-6 consists of twosubunits bonded together by disulfide bonds. Conclusion ACTX-6 and ATCX-8 have highest inhibitoryactivity on lung cancer cell A549. ACTX-6 is stable to heat while ACTX-8 not. ACTX-6 is stablebetween pH 7-9 and ACTX-8 between pH 6 - 9.展开更多
A series of β-carboline derivatives （1–6） have been synthesized and evaluated for their anticancer activities. We observed that compound 5 exhibited significant anticancer activities over both human gastric cancer...A series of β-carboline derivatives （1–6） have been synthesized and evaluated for their anticancer activities. We observed that compound 5 exhibited significant anticancer activities over both human gastric cancer and human hepatic cancer cell lines, and compound 6, which is slightly different from 5 in its structure, showed good anticancer activity over human colorectal cancer cell line.展开更多
文摘To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bispyridylanthrahydrazone(9,10‑PAH)were designed and synthesized.Utilizing 9‑PAH and 9,10‑PAH as promising anticancer ligands,their respective copper complexes,namely[Cu(L1)Cl_(2)]Cl(1)and{[Cu_(4)(μ_(2)‑Cl)_(3)Cl_(4)(9,10‑PAH)_(2)(DMSO)_(2)]Cl_(2)}_(n)(2),were subsequently synthesized,where the new ligand L1 is formed by coupling two 9‑PAH ligands in the coordination reaction.The chemical and crystal structures of 1 and 2 were elucidated by IR,MS,elemental analysis,and single‑crystal X‑ray diffraction.Complex 1 forms a mononuclear structure.L1 coordinates with Cu through its three N atoms,together with two Cl atoms,to form a five‑coordinated square pyramidal geometry.Complex 2 constitutes a polymeric structure,wherein each structural unit centrosymmetrically encompasses two five‑coordinated binuclear copper complexes(Cu1,Cu2)of 9,10‑PAH,with similar square pyramidal geometry.A chlorine atom(Cl_(2)),located at the symmetry center,bridges Cu1 and Cu1A to connect the two binuclear copper structures.Meanwhile,the two five‑coordinated Cu2 atoms symmetrically bridge the adjacent structural units via one coordinated Cl atom,respectively,thus forming a 1D chain‑like polymeric structure.In vitro anticancer activity assessments revealed that 1 and 2 showed significant cytotoxicity even higher than cisplatin.Specifically,the IC_(50)values of 2 against HeLa‑229 and SK‑OV‑3 cancer cell lines were determined to be(5.92±0.32)μmol·L^(-1)and(6.48±0.39)μmol·L^(-1),respectively.2 could also block the proliferation of HeLa‑229 cells in S phase and significantly induce cell apoptosis.In addition,fluorescence quenching competition experiments suggested that 2 might interact with DNA by an intercalative binding mode,offering insights into its underlying anticancer mechanism.CCDC:2388918,1;2388919,2.
基金Supported by Malaysian Ministry of Higher Education through the Fundamental Research Grant Scheme,No.FP103-2019.
文摘Cardamonin is a natural chalcone that has been extensively investigated for its anticancer activity.However,its clinical relevance is still not explicit,limiting its progression into clinical trials and highlighting a persistent gap between preclinical evidence and practical application.This review aims to assess the readiness of cardamonin to progress from laboratory research to clinical application as an anticancer agent by examining both scientific evidence and translational challenges.Preclinical pharmacokinetic and pharmacodynamic data suggest that cardamonin’s therapeutic potential as an anticancer agent is hindered by its poor oral bioavailability.Although its molecular targets remain undefined,evidence indicates that cardamonin can inhibit various signaling pathways,including nuclear factor kappa-light-chain-enhancer of activated B cells,mammalian target of rapamycin,signal transducer and activator of transcription 3,and Wnt/β-catenin.The lack of in vivo toxicity studies creates uncertainty regarding the balance between its therapeutic benefits and potential adverse effects when moving from laboratory research to human trials.Despite these limitations,cardamonin has,however,demonstrated antiproliferative,anti-metastatic,and chemosensitizing effects,mainly against breast,colorectal,and ovarian cancers.Nevertheless,exploring its combination with standard chemotherapeutic agents may offer a promising foundation for advancing cardamonin into clinical trials.
文摘Terpenes are a structurally diverse family of secondary metabolites found mostly in plants and microorganisms.Beta-caryophyllene and d-limonene are abundant in aromatic medicinal plants.Beta-caryophyllene can be sourced from clove and cannabis amongst others,and d-limonene is abundant in the Citrus genera.Apart from their use in agriculture,cosmetics,and food industries,these terpenes possess a wide range of therapeutic activities,including antimicrobial,analgesic,and anticancer activities.This review discusses the anticancer effects of these two compounds against malignant tumors including breast,lung,gastrointestinal,bone,blood,endometrial,and bladder cancer.Beta-caryophyllene induces apoptosis and prevents proliferation and metastasis through the downregulation of HSP60,HTRA,survivin,XIAP,Bcl-xL,and Bcl-2 and the upregulation of caspase 3,annexin V,p21,Bad,Bak,and Bax.The anticancer activity is also mediated by G1/M arrest,ROS induction,and JAK1/STAT activation.d-Limonene exerts its anticancer effects by upregulating autophagy-linked genes,Bax,and caspase 3 and downregulating cyclin D1 and Bcl-2.These compounds also elicit synergistic effects upon co-administration with anticancer drugs and show great prospects as useful agents in the fight against cancer.
文摘Background:The increasing incidence of cancers and infectious diseases worldwide presents a significant public health challenge that requires immediate intervention.Our strategy to tackle this issue involves the development of pharmaceutical formulations that combine phytopolyphenols(P),targeted drugs(T),and metal ions(M),collectively referred to as PTM regimens.The diverse pharmacological properties of PTM regimens are hypothesized to effectively reduce the risk factors associated with both cancers and infectious diseases.Methods:The effects of the pharmaceutical agents on the proliferation of cultured cancer cells and pathogens were assessed after 72 h and 48 h,respectively,using the MTT(3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide)assay and optical density at 600 nm(OD600).The synergistic effects of drug combinations were evaluated by combination index(CI),where CI<1 indicates synergism,CI=1 indicates addition,and CI>1 indicates antagonism.Efficacy index(EI)was also calculated.Assays of efflux pump ATPase activities were conducted using a colorimetric method.Results:This study evaluated the anticancer and antibacterial efficacy of PTM regimens that included phytopolyphenols(specifically curcumin(C)and green tea polyphenols(G)),repurposed drugs(memantine(Mem),thioridazine(TRZ),cisplatin(Cis),and 5-fluorouracil(5FU)),and ZnSO_(4)(Zn)across three cultured cancer cell lines and four cultured pathogens.The most effective regimens,GC·Mem·Zn and GC·TRZ·Zn,significantly enhanced the anticancer efficacy(EI)of cisplatin across the three cancer lines(OECM-1,A549 and DLD-1)by 7,11 and 21;7,9,and 17 fold,respectively,while the enhancements for 5-fluorouracil were 5,6 and 12;5,5 and 9 fold,respectively.Furthermore,these PTM regimens demonstrated substantial synergistic inhibition of Na^(+)-K^(+)-Mg^(2+)-ATPase and Mg^(2+)-ATPase in the cultured cancer cells,as well as a reduction in biofilm formation by the four cultured pathogens,suggesting their potential to address the challenges of multidrug resistance in cancers and infectious diseases.Conclusion:Given that all drugs incorporated in the PTM regimens have been clinically validated for safety and efficacy,particularly regarding their synergistic selective anticancer efficacy,inhibition of efflux pump ATPase,and antibiofilm formation of pathogens,these regimens may offer a promising therapeutic strategy to alleviate the severe side effects and drug resistance typically associated with chemotherapeutic agents.Further preclinical and clinical investigations are warranted.
文摘Marine natural products have long been recognized as a vast and diverse source of bioactive compounds with potential therapeutic applications,particularly in oncology.This review provides an updated overview of the significant advances made in the discovery and development of marine-derived anticancer drugs between 2019 and 2023.With a focus on recent research findings,the review explores the rich biodiversity of marine organisms,including sponges,corals,algae,and microorganisms,which have yielded numerous compounds exhibiting promising anticancer properties.Emphasizing the multifaceted mechanisms of action,the review discusses the molecular targets and pathways targeted by these compounds,such as cell cycle regulation,apoptosis induction,angiogenesis inhibition,and modulation of signaling pathways.Additionally,the review highlights the innovative strategies employed in the isolation,structural elucidation,and chemical modification of marine natural products to enhance their potency,selectivity,and pharmacological properties.Furthermore,it addresses the challenges and opportunities associated with the development of marine-derived anticancer drugs,including issues related to supply,sustainability,synthesis,and clinical translation.Finally,the review underscores the immense potential of marine natural products as a valuable reservoir of novel anticancer agents and advocates for continued exploration and exploitation of the marine environment to address the unmet medical needs in cancer therapy.
文摘Rice callus suspension culture(RCSC)has been shown to have anticancer activity based on cytotoxic activity on human colon and lung cancer cell lines.In the present study,the effect of RCSC on the expression of proteins in lung(A549)and colon(HT29)cancer cell lines was examined by using proteomics analysis.The protein-protein interaction study of differentially expressed proteins was done by using the Search Tool for the Retrieval of Interacting Genes(STRING),and the results showed that the proteins interacting with each other belong to different pathways.
基金supported by the National Natural Science Foundation of China(82274085)the Natural Science Foundation of Jiangsu Province(BK20220478)the Natural Science Foundation of Jiangsu Higher Education institutions of China(22KJB360010).
文摘The anticancer potential of quassinoids has attracted a great deal of attention for decades,and scientific data revealing their possible applications in cancer management are continuously increasing in the literature.Aside from the potent cytotoxic and antitumor properties of these degraded triterpenes,several quassinoids have exhibited synergistic effects with anticancer drugs.This article provides an overview of the potential anticancer properties of quassinoids,including their cytotoxic and antitumor activities,mechanisms of action,safety evaluation,and potential benefits in combination with anticancer drugs.
基金partly funded by the Department of Science and Technology Fund for Improvement of S&T Infrastructure (Grant No. SR/FST/LS-I/2018/125)。
文摘Tissue culture techniques were used to produce large amounts of bioactive compounds with medicinal potential, overcoming space and time constraints for cancer prevention. Rice callus suspension cultures(RCSC) and seed extracts prepared from aromatic rice varieties were used to evaluate the cytotoxic impact on human colon and lung cancer cell lines, as well as a normal control cell line, using Taxol as a positive control. RCSC and seed extracts from two Indian aromatic rice varieties were applied at different concentrations to treat the cancer cell lines and normal lung fibroblasts over varying time intervals. Apoptosis was assessed in 1:5 dilutions of the A549 and HT-29 cell lines treated with RCSC for 72 h, using propidium iodide staining and flow cytometry. RCSC showed a more potent cytotoxic effect than seed extracts with minimal effect on the normal cell line, in contrast to Taxol. Confocal microscopy and flow cytometry further confirmed the apoptotic effect of RCSC. Gas chromatography-mass spectrometry-based metabolic profiling identified metabolites involved in cytotoxicity and highlighted altered pathways. RCSC is proposed as an alternative source for the development of novel anticancer drugs with reduced side effects.
基金financially supported by the National Natural Science Foundation of China(Nos.21925802,22022803,22078046)the Fundamental Research Funds for the Central Universities(No.DUT22LAB601)。
文摘Photodynamic therapy(PDT)is a promising cancer treatment modality owing to its high spatiotempora selectivity and noninvasive nature.However,conventional photosensitizers(PSs)used in PDT are respon sive only to visible light,which makes them unsuitable for tissue penetration.In this study,we propose a PS based on hot band absorption(HBA),which can be triggered by anti-Stokes light at 808 nm via a one-photon process.The introduction of selenium(Se)into pentamethine cyanine(Secy5)not only facili tates intersystem crossing for reactive oxygen species(ROS)production but also enhances HBA efficiency thereby prolonging the excitation wavelength.In addition,Secy5 demonstrates excellent biocompatibility unlike its I-substituted counterpart(Icy5),and produces not only^(1)O_(2)but also O_(2)^(·-),making it a desirable candidate for treating hypoxic solid tumors.According to the results of in vivo and in vitro experiments Secy5 can efficiently inhibit cancer cell growth via anti-Stokes activation processes,thereby providing a novel approach to design anti-Stokes excitation PSs for anticancer treatment.
基金supported by Researchers Supporting Project number(RSP2025R414)King Saud University,Riyadh,Saudi Arabia.
文摘Objective:To evaluate the anticancer potential of Cymbopogon citratus extract.Methods:GC-MS analysis was used to identify phytocomponents in the methanolic extract of Cymbopogon citratus.A fractionation method was employed to isolate and assess the bioactivity of different fractions and their cytotoxic activities against cancer cell lines HCT116,LoVo,Caco-2,and HT-29 were investigated.A dual staining method with acridine orange and ethidium bromide was used to assess the effect of the extract on cell apoptosis.Additionally,the expression levels of Bax and TP53 were quantified using real-time PCR in Caco-2 cells treated with the ethyl acetate fraction of Cymbopogon citratus extract.A protein array was employed to profile key pro-and anti-apoptotic proteins in Caco-2 cells.Moreover,molecular docking studies were conducted to investigate the interactions between key compounds of Cymbopogon citratus extract and specific apoptosis-related protein domains(PDB IDs:7wql and 4bkx).Results:A significant growth inhibition was observed in Caco-2 cells treated with Cymbopogon citratus extract.Among the seven fractions of the plant extract,the ethyl acetate fraction showed the highest cytotoxicity against Caco-2 cells with an IC50 value of(6.16±0.01)μg/mL.The immunofluorescence assay showed that the ethyl acetate fraction could induce apoptosis of Caco-2 cells.Moreover,the fraction upregulated the gene expressions of Bax and TP53 in a dose-dependent manner.The docking analysis demonstrated the interaction of five compounds isolated from the ethyl acetate fraction with key proteins in Caco-2 cells,indicating their anticancer properties.Conclusions:Cymbopogon citratus extract shows anticancer activity against Caco-2 cells by inducing apoptosis.It may be a promising candidate for the treatment of colon cancer,which needs further investigation.
基金Liaoning Provincial Science and Technology Department Project,No.2023JH2/101700149Open Fund Project of Liaoning University of Traditional Chinese Medicine,No.zyzx2205.
文摘BACKGROUND Colon cancer(CC)is one of the most common malignant tumors in the gastrointestinal system.Overall,CC had the third highest incidence but the second highest mortality rate globally in 2020.Nowadays,CC is mainly treated with capecitabine chemotherapy regimen,supplemented by radiotherapy,immunotherapy and targeted therapy,but there are still limitations,so Chinese medicine plays an important role.AIM To investigate the effects of invigorating-spleen and anticancer prescription(ISAP)on body weight,tumor inhibition rate and expression levels of proteins in extracellular-signal-regulated kinase(ERK)/mitogen-activated protein kinase(MAPK)signaling pathway in CC mice model.METHODS The CC mice model were established and the mice were randomly divided into 5 groups,including the control group,capecitabine group,the low-dose,mediumdose and high-dose groups of ISAP,with 8 mice in each group,respectively.After 2 weeks of intervention,the body weight and tumor inhibition rate of mice were observed,and the expression of RAS,ERK,phosphorylated ERK(p-ERK),C-MYC and matrix metalloproteinase 2(MMP2)proteins in the tissues of tumors were detected.RESULTS Compared with the control group,the differences of body weight before and after treatment was much smaller in the groups of ISAP,with the smallest difference in the high-dose group of ISAP,while the capecitabine group had the greatest difference,indicating ISAP had a significant inhibiting effect on the growth of transplanted tumor in mice.The expression of RAS protein was decreased in the low-and medium-dose groups of ISAP,and the change of p-ERK was significant in the medium-and high-dose groups of ISAP.MMP2 protein expression was significantly decreased in both the low-dose and medium-dose groups of ISAP.There were no significant changes in ERK in the ISAP group compared to the capecitabine group,while RAS,MMP2,and C-MYC protein expression were reduced in the ISAP group.The expression level of C-MYC protein decreased after treated with ISAP,and the decrease was the most significant in the medium-dose group of ISAP.CONCLUSION ISAP has a potential inhibiting effect on transplanted tumor in mice,and could maintain the general conditions,physical strength and body weight of mice.The expression levels of RAS,p-ERK,MMP2 and c-myc were also decreased to a certain extent.By inhibiting the expression of upstream proteins,the expression levels of downstream proteins in ERK/MAPK signaling pathway were significantly decreased.Therefore,it can be concluded that ISAP may exert an anti-tumor effect by blocking the ERK/MAPK signaling pathway and inhibiting the expression of MMP2 and c-myc proteins.
基金Supported by Central Talent Training Project for the Reform and Development of Local Colleges and Universities(2020GSP16)Guidance Project of Key R&D Plan in Heilongjiang Province(GZ20220039).
文摘Koumine is an indole alkaloid monomer extracted from the Chinese herb Gelsemium elegans,which has a variety of pharmacological effects.This paper provides a comprehensive summary of the pharmacological effects and molecular mechanisms of koumine,with a particular emphasis on its mechanisms of action in the context of anticancer,anti-inflammatory,analgesic,and anxiolytic properties.The aim is to provide a theoretical foundation for further research and the application of koumine in clinical practice.
文摘Among microorganisms,fungi are the ones that have the most imagination in producing secondary metabolites with the most varied structural differences,which are produced through different biosynthetic pathways.Therefore,they synthesize secondary metabolites classifiable into numerous families of natural compounds such as amino acids,alkaloids,anthraquinones,aromatic compounds,cyclohexene epoxides,furanones,macrolides,naphthoquinones,polyketides,pyrones,terpenes,etc.They also produced metabolites with very complex structures that can not be classified in the known families of natural compounds.Many fungal metabolites show different biological activities with potential applications in agriculture,food chemistry,cosmetics,pharmacology and medicine.This review is focused on the fungal secondary metabolites with anticancer activity isolated in the last ten years.For some metabolites,when described,their biosynthetic origin,the mode of action and the results of structure activity relationships studies are also reported.
文摘Cancer occurs when the body’s cells grow beyond the usual control. Normal body cells multiply in a controlled manner and undergo apoptosis when the body no longer needs them. Different types of cancers exist, and the common ones include breast, cervical, prostate, lung, colon, and skin cancers. Several factors have been associated with cancers, and these factors include poor dieting, exposure to harmful chemicals and radiation, weak immune system, and genetics. Cancer presents an enormous health threat in the modern world and thus the need to identify an effective treatment. The conventional treatments used in the management of cancer include chemotherapy and physiotherapy. These forms of cancer treatments usually have enormous side effects on the subjects. In this respect, an alternative form of treatment would be effective in managing cancer patients. A substantial number of natural products have been observed to be effective in the management of cancer. These natural products include plants and other natural substances such as honey. This study focuses on the efficiency of natural products in the treatment of cancer. Also, the anticancer effects of Peganum harmala, Manuka honey, and Saudi honey will be analyzed. Bee honey and Peganum harmala have been traditionally used in the treatment of cancer. The extracts from Peganum harmala plant have also been shown to exhibit divers’ antitumor effects similar to the mode of action of a vast number of anticancer agents. These established hypotheses thus give the rationale for this study. In this experiment, extracts were obtained from Peganum harmala leaves and exposed to cervical, lung, and prostate cancer cells. Similarly, solutions of Manuka honey and Saudi honey were exposed to the cervical, lung, and prostate cancer cells. The experiment duration was 24 hours, which obtained results were recorded and analyzed. Peganum harmala extracts inhibit cancer cell growth at different and achievable concentrations. Manuka honey highly inhibits the growth of HeLa cancer cells while Saudi honey highly inhibits the growth of A549 cells. Peganum harmala can form an effective treatment for managing several types of cancers. Manuka Honey can be applied as an effective treatment for managing cervical cancer while Saudi honey can form an effective treatment for managing lung cancers.
文摘Purpose:This research aimed to identify leading factors that affect nurses’compliance with the safe handling of anticancer agents.Methods:Data were collected from 114 nurses working in the university hospital and were analyzed through independent t-test,one-way ANOVA,Pearson’s correlation coefficient,and multiple regression analysis using SPSS25.0.Results:The average level of compliance with the safe handling of anticancer agents was 3.73±0.33 out of 5 points.Workplace safety culture(β=0.40,P<0.001)and knowledge of safe handling(β=0.18,P=0.030)had significant influences on nurses’compliance with the safe handling of anticancer agents.The explained variance for compliance was 28.3%.Conclusion:To enhance the implementation of safety management for anticancer agents,each institution should strive to support human and material resources and enhance specialization in the workplace safety culture through system improvement.Based on the results of this study,we suggest research for the development of a training program for anticancer agent safety management.
基金this manuscript sincerely acknowledge Central South University for their support through the postdoctoral research initiation grant(164990011).
文摘Calotropisprocera(Cp)is a traditional medicinal plant that has attracted significant attention for its potential anticancer properties.This review consolidates current research on the Cp bioactive compounds found in Cp,including cardenolides,flavonoids,and terpenoids,which exhibit cytotoxic effects against various cancer cells.These compounds function through multiple mechanisms,such as inducing apoptosis,inhibiting cell proliferation,suppressing angiogenesis,and modulating oxidative stress.Preclinical studies demonstrate that Cp extracts effectively reduce tumor size and improve survival rates in animal models.Furthermore,Cp influences key signaling pathways like PI3K/Akt and NF-κB,which contribute to its anticancer potential.Its therapeutic effects extend beyond oncology,encompassing,antinociceptive,anticonvulsant,antimalarial,anthelmintic,antioxidant,antidiabetic,myocardial infarction prevention,schizontocidal,antimicrobial,anti-inflammatory,larvicidal,immunomodulatory,antiulcer,Antifertility,antidiarrheal,estrogenic,and Dermatophytic properties.Despite the promising preclinical data,further investigation is necessary to address challenges such as bioavailability,toxicity,and the standardization of Cp-based treatments.This review highlights the therapeutic promise of Cp as a complementary anticancer agent while emphasizing the need for rigorous clinical trials to confirm its safety and efficacy.
文摘Caffeic acid phenethyl ester (CAPE) and sixteen substituted cinnamic acid phenethyl esters were prepared via conventional procedures in order to test their in vitro anticancer activities by either MTT assay or SRB assay on six different human cancer cell lines. The results indicated that in the concentration of 10 μmol·L -1 the lead compound CAPE possessed anticancer activities against human HL 60, Bel 7402, and Hela cell lines, and two other compounds possessed potent anticancer activities against Bel 7402 and Hela cell lines.
文摘Aim To investigate the anticancer activity of two new cytotoxins from thevenom of Agkistrodon acutus. Methods The venom was isolated by FPLC column chromatography consistingof DEAE Sepharose FF and Source 30S. The cytotoxic activity on tumor cells was detected by MITmethod. Purity and molecular weight were determined by SDS-PAGE (silver staining). Their stabilitiesto temperature and pH were also detected. Results Two pure cytotoxins named ACTX-6 and ACTX-8 wereobtained. Their molecular weights are 98 kDa and 27 kDa, respectively. ACTX-6 consists of twosubunits bonded together by disulfide bonds. Conclusion ACTX-6 and ATCX-8 have highest inhibitoryactivity on lung cancer cell A549. ACTX-6 is stable to heat while ACTX-8 not. ACTX-6 is stablebetween pH 7-9 and ACTX-8 between pH 6 - 9.
基金New Teacher Foundation from Ministry of Education in China (Grant No.20090071120)Foundation of State Key Laboratory of Natural and Biomimetic Drugs (Grant No.K20100106)STCSM (Grant No.10431903200)
文摘A series of β-carboline derivatives （1–6） have been synthesized and evaluated for their anticancer activities. We observed that compound 5 exhibited significant anticancer activities over both human gastric cancer and human hepatic cancer cell lines, and compound 6, which is slightly different from 5 in its structure, showed good anticancer activity over human colorectal cancer cell line.
