Pub Date : 2024-04-01DOI: 10.1177/1934578x241248231
Tiancheng Gu, Wei Liu, Laiyou Wang, Jisheng Cheng
Objective/Background: This study aims to explore the Kadsura coccinea extract (KCE)'s effect on lipid accumulation in vitro and its chemical components characterizations, aiming at developing a new alternative plant medicinal resource to fight against non-alcoholic fatty liver disease (NAFLD). Methods: After toxicological evaluation of KCE on HepG2 cells, Oil red O staining model and intracellular TGs quantification kit were used to examine the effects of KCE on lipid accumulation in vitro. The chemical components characterizations and potential active chemical constituents of the bioactive KCE were analyzed using ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) technology. Results: Among the chosen non-toxic concentrations of KCE (5, 10, 20 μg/mL), KCE can reduce the number and volume of lipid droplets in the oleic acid induced HepG2 cells in a dose-dependent manner, and the results of TGs quantification were almost consistent with the results of the oil red O staining experiment. These data indicate the KCE has ameliorative effect on lipid accumulation in vitro. In addition, a total of 26 compounds from the KCE were tentatively identified, dibenzocyclooctadiene lignans (DCLs) including Kadsulignan L and Gomisin J could be the main supposed components. Conclusion: These findings support further investigation into Kadsura coccinea containing DCLs as a new alternative medicinal arsenal to battle against NAFLD.
{"title":"UPLC-Q-TOF-MS Analysis of Chemical Constituents of the Kadsura coccinea Extract with Effect of Attenuating Lipid Accumulation in Vitro","authors":"Tiancheng Gu, Wei Liu, Laiyou Wang, Jisheng Cheng","doi":"10.1177/1934578x241248231","DOIUrl":"https://doi.org/10.1177/1934578x241248231","url":null,"abstract":"Objective/Background: This study aims to explore the Kadsura coccinea extract (KCE)'s effect on lipid accumulation in vitro and its chemical components characterizations, aiming at developing a new alternative plant medicinal resource to fight against non-alcoholic fatty liver disease (NAFLD). Methods: After toxicological evaluation of KCE on HepG2 cells, Oil red O staining model and intracellular TGs quantification kit were used to examine the effects of KCE on lipid accumulation in vitro. The chemical components characterizations and potential active chemical constituents of the bioactive KCE were analyzed using ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) technology. Results: Among the chosen non-toxic concentrations of KCE (5, 10, 20 μg/mL), KCE can reduce the number and volume of lipid droplets in the oleic acid induced HepG2 cells in a dose-dependent manner, and the results of TGs quantification were almost consistent with the results of the oil red O staining experiment. These data indicate the KCE has ameliorative effect on lipid accumulation in vitro. In addition, a total of 26 compounds from the KCE were tentatively identified, dibenzocyclooctadiene lignans (DCLs) including Kadsulignan L and Gomisin J could be the main supposed components. Conclusion: These findings support further investigation into Kadsura coccinea containing DCLs as a new alternative medicinal arsenal to battle against NAFLD.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140779039","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x231224988
Zhimin Zhang, Qian Su, Yan Lin, Bohou Xia, Yamei Li, Jingchen Xie, Ping Wu, Duanfang Liao, Limei Lin
To investigate the scientific connotation of harvest period for Prunella vulgaris L. ( P vulgaris, known as Prunellae Spica), the triterpenoids and phenols of Prunellae Spica in developmental stages were quantified by high performance liquid chromatography, and the anti-inflammatory and anti-breast cancer properties of which were investigated. Furthermore, Grey correlation and Pearson correlation analysis were used to screen the anti-inflammatory and anti-breast cancer–related effective ingredients, and a multidimensional network of “ingredient-target-pathway” through network pharmacology was constructed. The results showed that the harvest time of Prunellae Spica was closely related to its chemical composition and pharmacological activity. Phenols, such as salvianic acid A, caffeic acid, and salviaflaside, mainly accumulated in late development, while rosmarinic acid showed the opposite. Triterpenes, such as oleanolic acid and ursolic acid, mainly accumulated in early development, while betulinic acid accumulated during ripening. The anti-breast cancer activity of Prunellae Spica in early development was stronger than that in the later, but the anti-inflammatory activity in late development was stronger than that in the early stage. Significantly associated with anti-inflammatory activity in Prunellae Spica was salviaflaside, which may regulate TNF and NOD-like receptor signaling pathways by acting on targets such as CASP7, CASP8, CASP3, NOD2, and CASP1. Significantly associated with anti-breast cancer activity were oleanolic acid and ursolic acid, which may regulate Ovarian steroidogenesis and Prolactin signaling pathways on targets such as PTGS2, CYP19A1, ESR2, CYP17A1, and MAPK3. These results suggest that P vulgaris could be harvested before ripening for its anti-breast cancer use, and after ripening for its anti-inflammatory use.
{"title":"The Dynamics of Bioactive Ingredients With Anti-Inflammatory and Anti-Breast Cancer Activity During Prunellae Spica Development","authors":"Zhimin Zhang, Qian Su, Yan Lin, Bohou Xia, Yamei Li, Jingchen Xie, Ping Wu, Duanfang Liao, Limei Lin","doi":"10.1177/1934578x231224988","DOIUrl":"https://doi.org/10.1177/1934578x231224988","url":null,"abstract":"To investigate the scientific connotation of harvest period for Prunella vulgaris L. ( P vulgaris, known as Prunellae Spica), the triterpenoids and phenols of Prunellae Spica in developmental stages were quantified by high performance liquid chromatography, and the anti-inflammatory and anti-breast cancer properties of which were investigated. Furthermore, Grey correlation and Pearson correlation analysis were used to screen the anti-inflammatory and anti-breast cancer–related effective ingredients, and a multidimensional network of “ingredient-target-pathway” through network pharmacology was constructed. The results showed that the harvest time of Prunellae Spica was closely related to its chemical composition and pharmacological activity. Phenols, such as salvianic acid A, caffeic acid, and salviaflaside, mainly accumulated in late development, while rosmarinic acid showed the opposite. Triterpenes, such as oleanolic acid and ursolic acid, mainly accumulated in early development, while betulinic acid accumulated during ripening. The anti-breast cancer activity of Prunellae Spica in early development was stronger than that in the later, but the anti-inflammatory activity in late development was stronger than that in the early stage. Significantly associated with anti-inflammatory activity in Prunellae Spica was salviaflaside, which may regulate TNF and NOD-like receptor signaling pathways by acting on targets such as CASP7, CASP8, CASP3, NOD2, and CASP1. Significantly associated with anti-breast cancer activity were oleanolic acid and ursolic acid, which may regulate Ovarian steroidogenesis and Prolactin signaling pathways on targets such as PTGS2, CYP19A1, ESR2, CYP17A1, and MAPK3. These results suggest that P vulgaris could be harvested before ripening for its anti-breast cancer use, and after ripening for its anti-inflammatory use.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139820757","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x241230820
F. Maarouf, H. Rahman
Background: Carvacrol (CAR) is the active component in essential oils (EOs) of many fragrant plants, including oregano and thyme; however, its high toxicity restricts its usage in biomedical fields, and the self-nano-emulsifying drug delivery system (SNEDDS) was suggested to overcome this issue. Objective: To prepare and characterize the CAR-loaded SNEDDS and to assess its toxicity profile towards healthy rats using the in vivo sub-chronic study. Methods: SNEDDS was prepared from olive oil, dimethyl sulfoxide, Tween-80, and distilled water, then CAR-SNEDDS was prepared by adding 0.5% CAR to SNEDDS and both composites were gently agitated for 72 h at room temperature. Later on, both composites were physiochemically characterized for size/charge (Zetasizer), shape (TEM), crystallinity (XRAD), composition (FTIR), and quantitated (UV–Vis). Additionally, the sub-chronic toxicity of both composites at different doses was conducted by orally treating healthy Sprague Dawley for 4 weeks. Then, the treated rats were checked for toxicological symptoms, food/water intake, and behavioral abnormality. In addition, the blood samples were tested for hematologic/biochemical changes, while vital organs (liver and kidney) were assessed for histopathological alterations. Results: The average globule size, zeta potential, and polydispersity index of CAR-SNEDDS were 158.93 ± 22.18 nm, −22.56 ± 1.77 mV, 0.553 ± 0.31, respectively. All treated animal tissues, serum biochemical profiles, and total hemograms were normal. At 30-90 mg/kg oral doses, CAR-SNEDDS was not toxic and did not cause mortality. Conclusions: CAR-SNEDDS was successfully synthesized and characterized, and the results from sub-chronic oral toxicity studies showed that the CAR-SNEDDS were non-toxic and safe for biomedical fields.
{"title":"Preparation, Characterization, and Sub-Chronic Toxicity of Carvacrol-Self-Nano-Emulsifying Drug Delivery System Towards Healthy Sprague Dawley Rats","authors":"F. Maarouf, H. Rahman","doi":"10.1177/1934578x241230820","DOIUrl":"https://doi.org/10.1177/1934578x241230820","url":null,"abstract":"Background: Carvacrol (CAR) is the active component in essential oils (EOs) of many fragrant plants, including oregano and thyme; however, its high toxicity restricts its usage in biomedical fields, and the self-nano-emulsifying drug delivery system (SNEDDS) was suggested to overcome this issue. Objective: To prepare and characterize the CAR-loaded SNEDDS and to assess its toxicity profile towards healthy rats using the in vivo sub-chronic study. Methods: SNEDDS was prepared from olive oil, dimethyl sulfoxide, Tween-80, and distilled water, then CAR-SNEDDS was prepared by adding 0.5% CAR to SNEDDS and both composites were gently agitated for 72 h at room temperature. Later on, both composites were physiochemically characterized for size/charge (Zetasizer), shape (TEM), crystallinity (XRAD), composition (FTIR), and quantitated (UV–Vis). Additionally, the sub-chronic toxicity of both composites at different doses was conducted by orally treating healthy Sprague Dawley for 4 weeks. Then, the treated rats were checked for toxicological symptoms, food/water intake, and behavioral abnormality. In addition, the blood samples were tested for hematologic/biochemical changes, while vital organs (liver and kidney) were assessed for histopathological alterations. Results: The average globule size, zeta potential, and polydispersity index of CAR-SNEDDS were 158.93 ± 22.18 nm, −22.56 ± 1.77 mV, 0.553 ± 0.31, respectively. All treated animal tissues, serum biochemical profiles, and total hemograms were normal. At 30-90 mg/kg oral doses, CAR-SNEDDS was not toxic and did not cause mortality. Conclusions: CAR-SNEDDS was successfully synthesized and characterized, and the results from sub-chronic oral toxicity studies showed that the CAR-SNEDDS were non-toxic and safe for biomedical fields.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139883873","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x241231433
Si-Cheng Yang, Xia Lei, Sifang Xie, Ju Huang, Feng-Qin Yue, Si-Di Chen, Wei Peng, Heng Fan, Sen Li, Xue-Yun Duan, Wan-Jin Sun
Objective: Analyzing the chemical composition and blood-entry components of Nourishing Blood Diuretic Formula (NBDF) by Liquid Chromatography-Mass Spectrometry (LC-MS), and analyzing the mechanism of NBDF in the treatment of chronic renal failure by combining network pharmacology and molecular docking technology. Methods: The prototype components were obtained by LC-MS, and the targets of the prototype components and the targets for the treatment of chronic renal failure (CRF) were predicted by network pharmacology to obtain the common targets of the drug and the disease, which were then subjected to gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses, and molecular docking was carried out between the compounds of the prototype components and the key targets, so as to screen out the active ingredients, the targets and the signaling pathways that were closely related to the efficacy of NBDF. Results: Synthesizing the test information, 125 compounds were identified from the solution of NBDF, and 48 blood-entry components were identified from rat plasma containing the drug, including 6 prototypical components, and 102 potential targets of action, 515 GO entries, and 133 KEGG pathways were obtained from the web-based pharmacological analyses, and molecular docking was performed to obtain the binding of the 6 prototypical component compounds and the 9 key targets, and the formononetin, emodin, epicatechin, chlorogenic acid, sennoside A, and astragaloside III were hypothesized to be the active components of NBDF in the treatment of CRF. Conclusion: This study initially demonstrated that Nourishing Blood and Diuretic Formula exert its therapeutic effects on CRF through multicomponents, multitargets, and multimethods, and elucidated its pharmacological material basis and therapeutic mechanism.
目的利用液相色谱-质谱联用技术（LC-MS）分析养血利尿方（NBDF）的化学成分和入血成分，并结合网络药理学和分子对接技术分析NBDF治疗慢性肾功能衰竭的机理。研究方法通过液相色谱-质谱（LC-MS）技术获得原型成分，并通过网络药理学预测原型成分的靶点和治疗慢性肾衰竭（CRF）的靶点，从而获得药物和疾病的共同靶点、然后进行基因本体（GO）和京都基因组百科全书（KEGG）富集分析，并对原型成分化合物与关键靶点进行分子对接，从而筛选出与NBDF疗效密切相关的有效成分、靶点和信号通路。研究结果综合测试信息，从NBDF溶液中鉴定出125个化合物，从含药大鼠血浆中鉴定出48种入血成分，其中包括6种原型成分，从网络药理分析中获得102个潜在作用靶点、515个GO条目和133条KEGG通路、并通过分子对接获得了 6 种原型成分化合物与 9 个关键靶点的结合情况，推测甲酮宁、大黄素、表儿茶素、绿原酸、番泻苷 A 和黄芪苷 III 是 NBDF 治疗 CRF 的活性成分。结论本研究初步证实了养血利尿方通过多成分、多靶点、多方法对CRF发挥治疗作用，阐明了其药理物质基础和治疗机制。
{"title":"Study on the Chemical Composition and Blood-Entry Components of Nourishing Blood Diuretic Formula Based on Liquid Chromatography-Mass Spectrometry and Network Pharmacology Techniques","authors":"Si-Cheng Yang, Xia Lei, Sifang Xie, Ju Huang, Feng-Qin Yue, Si-Di Chen, Wei Peng, Heng Fan, Sen Li, Xue-Yun Duan, Wan-Jin Sun","doi":"10.1177/1934578x241231433","DOIUrl":"https://doi.org/10.1177/1934578x241231433","url":null,"abstract":"Objective: Analyzing the chemical composition and blood-entry components of Nourishing Blood Diuretic Formula (NBDF) by Liquid Chromatography-Mass Spectrometry (LC-MS), and analyzing the mechanism of NBDF in the treatment of chronic renal failure by combining network pharmacology and molecular docking technology. Methods: The prototype components were obtained by LC-MS, and the targets of the prototype components and the targets for the treatment of chronic renal failure (CRF) were predicted by network pharmacology to obtain the common targets of the drug and the disease, which were then subjected to gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses, and molecular docking was carried out between the compounds of the prototype components and the key targets, so as to screen out the active ingredients, the targets and the signaling pathways that were closely related to the efficacy of NBDF. Results: Synthesizing the test information, 125 compounds were identified from the solution of NBDF, and 48 blood-entry components were identified from rat plasma containing the drug, including 6 prototypical components, and 102 potential targets of action, 515 GO entries, and 133 KEGG pathways were obtained from the web-based pharmacological analyses, and molecular docking was performed to obtain the binding of the 6 prototypical component compounds and the 9 key targets, and the formononetin, emodin, epicatechin, chlorogenic acid, sennoside A, and astragaloside III were hypothesized to be the active components of NBDF in the treatment of CRF. Conclusion: This study initially demonstrated that Nourishing Blood and Diuretic Formula exert its therapeutic effects on CRF through multicomponents, multitargets, and multimethods, and elucidated its pharmacological material basis and therapeutic mechanism.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139892120","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x231222102
Yuanru Wang, Lubiao Liang, Yajin Zhao
Curcumin, a natural polyphenol compound found in turmeric, exhibits significant anti-cancer activity in preclinical studies. However, its clinical application is limited by poor bioavailability and low solubility in aqueous media. To overcome these challenges, various curcumin delivery systems (CDSs) have been developed to enhance the pharmacokinetics and pharmacodynamics of curcumin, aiming to improve its solubility, stability, and targeted delivery to tumor cells. Preclinical studies have shown that CDSs can improve pharmacokinetics, enhance anti-tumor efficacy, and reduce toxicity in various cancers. Several CDSs have also advanced into clinical trials, demonstrating safety and efficacy in cancer patients. Despite the promising results, challenges remain, such as optimizing formulation and dosage, investigating curcumin's influence on the carriers in drug delivery and release, evaluating long-term safety and toxicity, and conducting large-scale clinical trials. Understanding the effect of gut microbiota on CDSs metabolism and bioavailability is critical for enhancing their clinical effectiveness in tumor therapy. Further research and development are necessary to fully exploit the potential of CDSs in cancer treatment. This review summarizes recent progress in CDSs research and their potential application in tumor therapy, encompassing formulation strategies, delivery routes, as well as preclinical and clinical evaluations. It not only provides valuable insights into the future rational design and development of curcumin dosage forms and their cancer therapeutic potential but also facilitates the clinical translation of curcumin and CDSs.
{"title":"Curcumin Delivery Systems: How Far from Clinical Application in Tumor Therapy?","authors":"Yuanru Wang, Lubiao Liang, Yajin Zhao","doi":"10.1177/1934578x231222102","DOIUrl":"https://doi.org/10.1177/1934578x231222102","url":null,"abstract":"Curcumin, a natural polyphenol compound found in turmeric, exhibits significant anti-cancer activity in preclinical studies. However, its clinical application is limited by poor bioavailability and low solubility in aqueous media. To overcome these challenges, various curcumin delivery systems (CDSs) have been developed to enhance the pharmacokinetics and pharmacodynamics of curcumin, aiming to improve its solubility, stability, and targeted delivery to tumor cells. Preclinical studies have shown that CDSs can improve pharmacokinetics, enhance anti-tumor efficacy, and reduce toxicity in various cancers. Several CDSs have also advanced into clinical trials, demonstrating safety and efficacy in cancer patients. Despite the promising results, challenges remain, such as optimizing formulation and dosage, investigating curcumin's influence on the carriers in drug delivery and release, evaluating long-term safety and toxicity, and conducting large-scale clinical trials. Understanding the effect of gut microbiota on CDSs metabolism and bioavailability is critical for enhancing their clinical effectiveness in tumor therapy. Further research and development are necessary to fully exploit the potential of CDSs in cancer treatment. This review summarizes recent progress in CDSs research and their potential application in tumor therapy, encompassing formulation strategies, delivery routes, as well as preclinical and clinical evaluations. It not only provides valuable insights into the future rational design and development of curcumin dosage forms and their cancer therapeutic potential but also facilitates the clinical translation of curcumin and CDSs.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139815263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x241226562
Zhiyuan Xu, Haixin Ding, Fu Xin, Xu Yan, Zhu Fadi, Huochun Ye, Zhang Yuan Yuan, Yongxia Guo, Zhang Jing, Feng Gang
Due to the urgent need to develop innovative, environmentally sustainable bactericides, we use the natural product isoquinoline as a lead compound to discover highly active bactericides from isoquinoline derivatives. In this paper, the antibacterial activity of 49 isoquinoline derivatives was evaluated against three plant bacteria in vitro. Among all the derivatives, isoquinoline-3-carboxylic acid (IQ3CA) demonstrated significant antibacterial activity against Ralstonia solanacearum ( Rs), Acidovorax citrulli ( Ac), X. oryzae pv. oryzicola ( Xoc), X. campestris pv. campestris ( Xcc), P. carotovorum subsp. carotovorum ( Pcc), and X. fragariae ( Xf), with EC50 values ranging from 8.38 to 17.35 μg/mL. Furthermore, IQ3CA exhibited a potent protective effect against Ac, with an efficacy of 68.56% at 200 μg/mL, which was not significantly different from that of the positive control kasugamycin (72.48%) and was superior to that of the positive control thiosen copper (64.62%). The scanning electron microscopy observations revealed that treatment of Ac cells with IQ3CA at a concentration of 25 μg/mL resulted in a curved and sunken cell morphology, along with destroyed cell membrane integrity. Additionally, the motility and exopolysaccharides production of Ac were inhibited, and biofilm formation was prevented. These results suggest that IQ3CA holds promise as a lead compound with antibacterial properties against plant diseases.
{"title":"Antibacterial Activity and Possibly Made of Action of Isoquinoline-3-Carboxylic Acid","authors":"Zhiyuan Xu, Haixin Ding, Fu Xin, Xu Yan, Zhu Fadi, Huochun Ye, Zhang Yuan Yuan, Yongxia Guo, Zhang Jing, Feng Gang","doi":"10.1177/1934578x241226562","DOIUrl":"https://doi.org/10.1177/1934578x241226562","url":null,"abstract":"Due to the urgent need to develop innovative, environmentally sustainable bactericides, we use the natural product isoquinoline as a lead compound to discover highly active bactericides from isoquinoline derivatives. In this paper, the antibacterial activity of 49 isoquinoline derivatives was evaluated against three plant bacteria in vitro. Among all the derivatives, isoquinoline-3-carboxylic acid (IQ3CA) demonstrated significant antibacterial activity against Ralstonia solanacearum ( Rs), Acidovorax citrulli ( Ac), X. oryzae pv. oryzicola ( Xoc), X. campestris pv. campestris ( Xcc), P. carotovorum subsp. carotovorum ( Pcc), and X. fragariae ( Xf), with EC50 values ranging from 8.38 to 17.35 μg/mL. Furthermore, IQ3CA exhibited a potent protective effect against Ac, with an efficacy of 68.56% at 200 μg/mL, which was not significantly different from that of the positive control kasugamycin (72.48%) and was superior to that of the positive control thiosen copper (64.62%). The scanning electron microscopy observations revealed that treatment of Ac cells with IQ3CA at a concentration of 25 μg/mL resulted in a curved and sunken cell morphology, along with destroyed cell membrane integrity. Additionally, the motility and exopolysaccharides production of Ac were inhibited, and biofilm formation was prevented. These results suggest that IQ3CA holds promise as a lead compound with antibacterial properties against plant diseases.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139826469","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x241231433
Si-Cheng Yang, Xia Lei, Sifang Xie, Ju Huang, Feng-Qin Yue, Si-Di Chen, Wei Peng, Heng Fan, Sen Li, Xue-Yun Duan, Wan-Jin Sun
Objective: Analyzing the chemical composition and blood-entry components of Nourishing Blood Diuretic Formula (NBDF) by Liquid Chromatography-Mass Spectrometry (LC-MS), and analyzing the mechanism of NBDF in the treatment of chronic renal failure by combining network pharmacology and molecular docking technology. Methods: The prototype components were obtained by LC-MS, and the targets of the prototype components and the targets for the treatment of chronic renal failure (CRF) were predicted by network pharmacology to obtain the common targets of the drug and the disease, which were then subjected to gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses, and molecular docking was carried out between the compounds of the prototype components and the key targets, so as to screen out the active ingredients, the targets and the signaling pathways that were closely related to the efficacy of NBDF. Results: Synthesizing the test information, 125 compounds were identified from the solution of NBDF, and 48 blood-entry components were identified from rat plasma containing the drug, including 6 prototypical components, and 102 potential targets of action, 515 GO entries, and 133 KEGG pathways were obtained from the web-based pharmacological analyses, and molecular docking was performed to obtain the binding of the 6 prototypical component compounds and the 9 key targets, and the formononetin, emodin, epicatechin, chlorogenic acid, sennoside A, and astragaloside III were hypothesized to be the active components of NBDF in the treatment of CRF. Conclusion: This study initially demonstrated that Nourishing Blood and Diuretic Formula exert its therapeutic effects on CRF through multicomponents, multitargets, and multimethods, and elucidated its pharmacological material basis and therapeutic mechanism.
目的利用液相色谱-质谱联用技术（LC-MS）分析养血利尿方（NBDF）的化学成分和入血成分，并结合网络药理学和分子对接技术分析NBDF治疗慢性肾功能衰竭的机理。研究方法通过液相色谱-质谱（LC-MS）技术获得原型成分，并通过网络药理学预测原型成分的靶点和治疗慢性肾衰竭（CRF）的靶点，从而获得药物和疾病的共同靶点、然后进行基因本体（GO）和京都基因组百科全书（KEGG）富集分析，并对原型成分化合物与关键靶点进行分子对接，从而筛选出与NBDF疗效密切相关的有效成分、靶点和信号通路。研究结果综合测试信息，从NBDF溶液中鉴定出125个化合物，从含药大鼠血浆中鉴定出48种入血成分，其中包括6种原型成分，从网络药理分析中获得102个潜在作用靶点、515个GO条目和133条KEGG通路、并通过分子对接获得了 6 种原型成分化合物与 9 个关键靶点的结合情况，推测甲酮宁、大黄素、表儿茶素、绿原酸、番泻苷 A 和黄芪苷 III 是 NBDF 治疗 CRF 的活性成分。结论本研究初步证实了养血利尿方通过多成分、多靶点、多方法对CRF发挥治疗作用，阐明了其药理物质基础和治疗机制。
{"title":"Study on the Chemical Composition and Blood-Entry Components of Nourishing Blood Diuretic Formula Based on Liquid Chromatography-Mass Spectrometry and Network Pharmacology Techniques","authors":"Si-Cheng Yang, Xia Lei, Sifang Xie, Ju Huang, Feng-Qin Yue, Si-Di Chen, Wei Peng, Heng Fan, Sen Li, Xue-Yun Duan, Wan-Jin Sun","doi":"10.1177/1934578x241231433","DOIUrl":"https://doi.org/10.1177/1934578x241231433","url":null,"abstract":"Objective: Analyzing the chemical composition and blood-entry components of Nourishing Blood Diuretic Formula (NBDF) by Liquid Chromatography-Mass Spectrometry (LC-MS), and analyzing the mechanism of NBDF in the treatment of chronic renal failure by combining network pharmacology and molecular docking technology. Methods: The prototype components were obtained by LC-MS, and the targets of the prototype components and the targets for the treatment of chronic renal failure (CRF) were predicted by network pharmacology to obtain the common targets of the drug and the disease, which were then subjected to gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses, and molecular docking was carried out between the compounds of the prototype components and the key targets, so as to screen out the active ingredients, the targets and the signaling pathways that were closely related to the efficacy of NBDF. Results: Synthesizing the test information, 125 compounds were identified from the solution of NBDF, and 48 blood-entry components were identified from rat plasma containing the drug, including 6 prototypical components, and 102 potential targets of action, 515 GO entries, and 133 KEGG pathways were obtained from the web-based pharmacological analyses, and molecular docking was performed to obtain the binding of the 6 prototypical component compounds and the 9 key targets, and the formononetin, emodin, epicatechin, chlorogenic acid, sennoside A, and astragaloside III were hypothesized to be the active components of NBDF in the treatment of CRF. Conclusion: This study initially demonstrated that Nourishing Blood and Diuretic Formula exert its therapeutic effects on CRF through multicomponents, multitargets, and multimethods, and elucidated its pharmacological material basis and therapeutic mechanism.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139832354","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x231222102
Yuanru Wang, Lubiao Liang, Yajin Zhao
Curcumin, a natural polyphenol compound found in turmeric, exhibits significant anti-cancer activity in preclinical studies. However, its clinical application is limited by poor bioavailability and low solubility in aqueous media. To overcome these challenges, various curcumin delivery systems (CDSs) have been developed to enhance the pharmacokinetics and pharmacodynamics of curcumin, aiming to improve its solubility, stability, and targeted delivery to tumor cells. Preclinical studies have shown that CDSs can improve pharmacokinetics, enhance anti-tumor efficacy, and reduce toxicity in various cancers. Several CDSs have also advanced into clinical trials, demonstrating safety and efficacy in cancer patients. Despite the promising results, challenges remain, such as optimizing formulation and dosage, investigating curcumin's influence on the carriers in drug delivery and release, evaluating long-term safety and toxicity, and conducting large-scale clinical trials. Understanding the effect of gut microbiota on CDSs metabolism and bioavailability is critical for enhancing their clinical effectiveness in tumor therapy. Further research and development are necessary to fully exploit the potential of CDSs in cancer treatment. This review summarizes recent progress in CDSs research and their potential application in tumor therapy, encompassing formulation strategies, delivery routes, as well as preclinical and clinical evaluations. It not only provides valuable insights into the future rational design and development of curcumin dosage forms and their cancer therapeutic potential but also facilitates the clinical translation of curcumin and CDSs.
{"title":"Curcumin Delivery Systems: How Far from Clinical Application in Tumor Therapy?","authors":"Yuanru Wang, Lubiao Liang, Yajin Zhao","doi":"10.1177/1934578x231222102","DOIUrl":"https://doi.org/10.1177/1934578x231222102","url":null,"abstract":"Curcumin, a natural polyphenol compound found in turmeric, exhibits significant anti-cancer activity in preclinical studies. However, its clinical application is limited by poor bioavailability and low solubility in aqueous media. To overcome these challenges, various curcumin delivery systems (CDSs) have been developed to enhance the pharmacokinetics and pharmacodynamics of curcumin, aiming to improve its solubility, stability, and targeted delivery to tumor cells. Preclinical studies have shown that CDSs can improve pharmacokinetics, enhance anti-tumor efficacy, and reduce toxicity in various cancers. Several CDSs have also advanced into clinical trials, demonstrating safety and efficacy in cancer patients. Despite the promising results, challenges remain, such as optimizing formulation and dosage, investigating curcumin's influence on the carriers in drug delivery and release, evaluating long-term safety and toxicity, and conducting large-scale clinical trials. Understanding the effect of gut microbiota on CDSs metabolism and bioavailability is critical for enhancing their clinical effectiveness in tumor therapy. Further research and development are necessary to fully exploit the potential of CDSs in cancer treatment. This review summarizes recent progress in CDSs research and their potential application in tumor therapy, encompassing formulation strategies, delivery routes, as well as preclinical and clinical evaluations. It not only provides valuable insights into the future rational design and development of curcumin dosage forms and their cancer therapeutic potential but also facilitates the clinical translation of curcumin and CDSs.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139875053","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x241228966
Ruiqing Xu, Rui Huang, Jiandang Shi, Dawei Chu, Pengyu Yang
Studies have shown that Momordin Ic (MI) has an antitumor effect on liver cancer, gastric cancer, and colorectal cancer. However, its effect on osteosarcoma has not yet been reported. The purpose of this study was to explore the effect of MI on several malignant phenotypes of osteosarcoma cells. CCK-8 and EdU were used to evaluate the effect of MI on the proliferation of osteosarcoma cells. Apoptosis and cell cycle were observed by flow cytometry. Monodansycadaverine (MDC) staining was used to detect autophagy. Western blot was used to evaluate apoptosis, cell cycle, autophagy, and ferroptosis. Evaluation of osteosarcoma cell migration ability by wound healing assay. Colony formation assay was used to test the ability of cloning. Transwell invasion assay was used to detect the invasion level of osteosarcoma cells. The results showed that MI significantly inhibited the proliferative activity of osteosarcoma cells. Z-VAD-FMK, 3-MA, and Fer-1 were administered separately, and the results showed that except for Fer-1, the other two inhibitors could reverse cell activity to different degrees. Flow cytometry showed that MI induced G0/1 cell cycle arrest and increased apoptosis. MDC showed that MI induced autophagy in osteosarcoma cells. Western blot showed that autophagy and apoptosis proteins were significantly higher in MI group. Transwell invasion assay, wound healing assay, and colony formation assay confirmed that MI could inhibit the invasion, migration, and cloning ability of osteosarcoma cells. In conclusion, our study confirmed that MI may exert antitumor effects by inducing apoptosis and autophagy in osteosarcoma cells.
研究表明，Momordin Ic（MI）对肝癌、胃癌和大肠癌有抗肿瘤作用。但它对骨肉瘤的影响尚未见报道。本研究旨在探讨 MI 对骨肉瘤细胞几种恶性表型的影响。研究使用 CCK-8 和 EdU 评估 MI 对骨肉瘤细胞增殖的影响。流式细胞术观察细胞凋亡和细胞周期。MDC染色用于检测自噬。用 Western 印迹法评估细胞凋亡、细胞周期、自噬和铁变态反应。通过伤口愈合试验评估骨肉瘤细胞的迁移能力。集落形成试验用于检测克隆能力。Transwell 侵袭试验用于检测骨肉瘤细胞的侵袭水平。结果表明，MI能明显抑制骨肉瘤细胞的增殖活性。对Z-VAD-FMK、3-MA和Fer-1分别用药，结果表明除Fer-1外，其他两种抑制剂都能不同程度地逆转细胞活性。流式细胞术显示，MI 能诱导 G0/1 细胞周期停滞并增加细胞凋亡。MDC显示，MI能诱导骨肉瘤细胞自噬。Western印迹显示，MI组细胞的自噬和凋亡蛋白明显升高。Transwell侵袭试验、伤口愈合试验和集落形成试验证实，MI能抑制骨肉瘤细胞的侵袭、迁移和克隆能力。总之，我们的研究证实，MI可通过诱导骨肉瘤细胞凋亡和自噬发挥抗肿瘤作用。
{"title":"Momordin Ic Inhibits the Partially Malignant Phenotype of Osteosarcoma Cells by Inducing Apoptosis and Autophagy","authors":"Ruiqing Xu, Rui Huang, Jiandang Shi, Dawei Chu, Pengyu Yang","doi":"10.1177/1934578x241228966","DOIUrl":"https://doi.org/10.1177/1934578x241228966","url":null,"abstract":"Studies have shown that Momordin Ic (MI) has an antitumor effect on liver cancer, gastric cancer, and colorectal cancer. However, its effect on osteosarcoma has not yet been reported. The purpose of this study was to explore the effect of MI on several malignant phenotypes of osteosarcoma cells. CCK-8 and EdU were used to evaluate the effect of MI on the proliferation of osteosarcoma cells. Apoptosis and cell cycle were observed by flow cytometry. Monodansycadaverine (MDC) staining was used to detect autophagy. Western blot was used to evaluate apoptosis, cell cycle, autophagy, and ferroptosis. Evaluation of osteosarcoma cell migration ability by wound healing assay. Colony formation assay was used to test the ability of cloning. Transwell invasion assay was used to detect the invasion level of osteosarcoma cells. The results showed that MI significantly inhibited the proliferative activity of osteosarcoma cells. Z-VAD-FMK, 3-MA, and Fer-1 were administered separately, and the results showed that except for Fer-1, the other two inhibitors could reverse cell activity to different degrees. Flow cytometry showed that MI induced G0/1 cell cycle arrest and increased apoptosis. MDC showed that MI induced autophagy in osteosarcoma cells. Western blot showed that autophagy and apoptosis proteins were significantly higher in MI group. Transwell invasion assay, wound healing assay, and colony formation assay confirmed that MI could inhibit the invasion, migration, and cloning ability of osteosarcoma cells. In conclusion, our study confirmed that MI may exert antitumor effects by inducing apoptosis and autophagy in osteosarcoma cells.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139877911","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-01DOI: 10.1177/1934578x231224988
Zhimin Zhang, Qian Su, Yan Lin, Bohou Xia, Yamei Li, Jingchen Xie, Ping Wu, Duanfang Liao, Limei Lin
To investigate the scientific connotation of harvest period for Prunella vulgaris L. ( P vulgaris, known as Prunellae Spica), the triterpenoids and phenols of Prunellae Spica in developmental stages were quantified by high performance liquid chromatography, and the anti-inflammatory and anti-breast cancer properties of which were investigated. Furthermore, Grey correlation and Pearson correlation analysis were used to screen the anti-inflammatory and anti-breast cancer–related effective ingredients, and a multidimensional network of “ingredient-target-pathway” through network pharmacology was constructed. The results showed that the harvest time of Prunellae Spica was closely related to its chemical composition and pharmacological activity. Phenols, such as salvianic acid A, caffeic acid, and salviaflaside, mainly accumulated in late development, while rosmarinic acid showed the opposite. Triterpenes, such as oleanolic acid and ursolic acid, mainly accumulated in early development, while betulinic acid accumulated during ripening. The anti-breast cancer activity of Prunellae Spica in early development was stronger than that in the later, but the anti-inflammatory activity in late development was stronger than that in the early stage. Significantly associated with anti-inflammatory activity in Prunellae Spica was salviaflaside, which may regulate TNF and NOD-like receptor signaling pathways by acting on targets such as CASP7, CASP8, CASP3, NOD2, and CASP1. Significantly associated with anti-breast cancer activity were oleanolic acid and ursolic acid, which may regulate Ovarian steroidogenesis and Prolactin signaling pathways on targets such as PTGS2, CYP19A1, ESR2, CYP17A1, and MAPK3. These results suggest that P vulgaris could be harvested before ripening for its anti-breast cancer use, and after ripening for its anti-inflammatory use.
{"title":"The Dynamics of Bioactive Ingredients With Anti-Inflammatory and Anti-Breast Cancer Activity During Prunellae Spica Development","authors":"Zhimin Zhang, Qian Su, Yan Lin, Bohou Xia, Yamei Li, Jingchen Xie, Ping Wu, Duanfang Liao, Limei Lin","doi":"10.1177/1934578x231224988","DOIUrl":"https://doi.org/10.1177/1934578x231224988","url":null,"abstract":"To investigate the scientific connotation of harvest period for Prunella vulgaris L. ( P vulgaris, known as Prunellae Spica), the triterpenoids and phenols of Prunellae Spica in developmental stages were quantified by high performance liquid chromatography, and the anti-inflammatory and anti-breast cancer properties of which were investigated. Furthermore, Grey correlation and Pearson correlation analysis were used to screen the anti-inflammatory and anti-breast cancer–related effective ingredients, and a multidimensional network of “ingredient-target-pathway” through network pharmacology was constructed. The results showed that the harvest time of Prunellae Spica was closely related to its chemical composition and pharmacological activity. Phenols, such as salvianic acid A, caffeic acid, and salviaflaside, mainly accumulated in late development, while rosmarinic acid showed the opposite. Triterpenes, such as oleanolic acid and ursolic acid, mainly accumulated in early development, while betulinic acid accumulated during ripening. The anti-breast cancer activity of Prunellae Spica in early development was stronger than that in the later, but the anti-inflammatory activity in late development was stronger than that in the early stage. Significantly associated with anti-inflammatory activity in Prunellae Spica was salviaflaside, which may regulate TNF and NOD-like receptor signaling pathways by acting on targets such as CASP7, CASP8, CASP3, NOD2, and CASP1. Significantly associated with anti-breast cancer activity were oleanolic acid and ursolic acid, which may regulate Ovarian steroidogenesis and Prolactin signaling pathways on targets such as PTGS2, CYP19A1, ESR2, CYP17A1, and MAPK3. These results suggest that P vulgaris could be harvested before ripening for its anti-breast cancer use, and after ripening for its anti-inflammatory use.","PeriodicalId":509851,"journal":{"name":"Natural Product Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139880530","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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