In the development of new drugs products,especially the development of traditional Chinese medicine active ingredients,solubility and oral bioavailability are the main factors which are restricting the development of ...In the development of new drugs products,especially the development of traditional Chinese medicine active ingredients,solubility and oral bioavailability are the main factors which are restricting the development of new drugs,whereas the physicochemical properties of active ingredients are the key element to affecting these factors.Pharmaceutical cocrystal provides an excellent opportunity to develop new drugs with excellent physical and chemical properties such as melting point,solubility,stability and bioavailability while retaining the pharmacological properties of individuals active pharmaceutical ingredients among pharmaceutical cocrystal compounds.Traditional Chinese herbal medicine has the characteristics of multiple pathways and multiple targets,mainly because it contains many active ingredients,like cocrystals thereof with many components.The active ingredients extracted from traditional Chinese herbal medicine have a wide range of pharmacological activities,but most of the active ingredients affect the development of traditional Chinese medicine active ingredients due to their physical and chemical properties such as solubility.Traditional Chinese medicine pharmaceutical cocrystals can not only improve the physical and chemical properties of drugs without changing the internal structure of drugs,so as to provide a new scheme for the development of traditional Chinese medicine active ingredients.This paper reviews the research progress of active ingredients of traditional Chinese medicine pharmaceutical cocrystal.The preparation methods of cocrystals are summarized and the advantages of cocrystals are illustrated with examples.展开更多
Flavonoids are natural organic compounds that are widely found in nature, their structural types are complex, and they mainly include flavonoids, flavonols, dihydroflavonols, isoflavones, dihydroisoflavones, chalcones...Flavonoids are natural organic compounds that are widely found in nature, their structural types are complex, and they mainly include flavonoids, flavonols, dihydroflavonols, isoflavones, dihydroisoflavones, chalcones, orange ketones, flavanoids, anthocyanidins, and biflavonoids. This review covers the plant distribution and pharmacological activities of flavonoids. Flavonoids are mainly distributed in angiosperms and gymnosperms, and they are abundant in plants such as Rutaceae, Labiatae, Zingiberaceae, Scrophulariaceae, and Leguminosae. Because of their wide distribution and variety, researchers have found that flavonoids have diverse biological activities, mainly focusing on anti-inflammatory, antibacterial and antitumor activities. Mechanistically, the anti-inflammatory effects are mainly related to the NF-κB and MAPK (mitogen-activated protein kinase) signaling pathway and then the inhibition of the production of inflammatory cytokines and mediators. The antibacterial activity is mainly manifested as inhibitory effects on many strains, including Escherichia coli, Cryptococcus neoformans, and Pseudomonas aeruginosa, via destroying the stability of the microbial membrane, inhibiting the invasion of virulent bacteria into host cells, promoting the apoptosis of bacteria, inhibiting bacterial fatty acid synthesis, etc. The antitumor activity of flavonoids is related to their inhibition of cell proliferation and induction of apoptosis via the mitochondria-mediated, endoplasmic reticulum-mediated, and death factor and its receptor-mediated signal transduction pathways. Understanding the plant distribution and pharmacological activity of flavonoids not only reveals the importance of identifying such valuable flavonoids in another genus or family but also provides a basis for fully exploiting the therapeutic potential of flavonoids.展开更多
目的：探讨苏铁双黄酮对非小细胞肺癌A549细胞内皮抑素（Endostatin）、转化生长因子-β（Transforming growth factor-β,TGF-β）、信号传导及转录激活因子3（Signal transducers and activators of transcription3,STAT3）、β-链蛋...目的：探讨苏铁双黄酮对非小细胞肺癌A549细胞内皮抑素（Endostatin）、转化生长因子-β（Transforming growth factor-β,TGF-β）、信号传导及转录激活因子3（Signal transducers and activators of transcription3,STAT3）、β-链蛋白和紧密连接蛋白1（Zonula occludens-1protein,ZO-1）表达的影响.方法：苏铁双黄酮作用于A549细胞24h后,采用免疫荧光法检测endostatin、TGF-β的定位及表达量,实时荧光定量PCR法检测STAT3、β-catenin、TGF-β和ZO-1mRNA的表达,westernblot法检测STAT3、β-catenin蛋白的表达.结果：与空白组比较,苏铁双黄酮显著下调TGF-β、STAT3和β-catenin的表达,上调endostatin和ZO-1的表达,且呈明显的浓度依赖性.结论：苏铁双黄酮治疗肺癌的作用机制可能为：通过抑制TGF-β、STAT3和β-catenin的表达,增加endostatin和ZO-1的表达,进而发挥抗肿瘤的作用.展开更多
基金The National Natural Science Foundation of China(No.81973977,No.81273872)the Fundamental Research Funds for the Central Universities(2021JCXK02)supported this study.
文摘In the development of new drugs products,especially the development of traditional Chinese medicine active ingredients,solubility and oral bioavailability are the main factors which are restricting the development of new drugs,whereas the physicochemical properties of active ingredients are the key element to affecting these factors.Pharmaceutical cocrystal provides an excellent opportunity to develop new drugs with excellent physical and chemical properties such as melting point,solubility,stability and bioavailability while retaining the pharmacological properties of individuals active pharmaceutical ingredients among pharmaceutical cocrystal compounds.Traditional Chinese herbal medicine has the characteristics of multiple pathways and multiple targets,mainly because it contains many active ingredients,like cocrystals thereof with many components.The active ingredients extracted from traditional Chinese herbal medicine have a wide range of pharmacological activities,but most of the active ingredients affect the development of traditional Chinese medicine active ingredients due to their physical and chemical properties such as solubility.Traditional Chinese medicine pharmaceutical cocrystals can not only improve the physical and chemical properties of drugs without changing the internal structure of drugs,so as to provide a new scheme for the development of traditional Chinese medicine active ingredients.This paper reviews the research progress of active ingredients of traditional Chinese medicine pharmaceutical cocrystal.The preparation methods of cocrystals are summarized and the advantages of cocrystals are illustrated with examples.
基金This study was financially supported by the Autonomous Foundation of Key Laboratory of Ethnomedicine (Minzu University of China), Ministry of Education (No. KLEM-ZZ201902)the National Natural Science Foundation of China Grants (No. 81973977)the National Training Programs of Innovation and Entrepreneurship for Undergraduates (No. GCYS2018110001).
文摘Flavonoids are natural organic compounds that are widely found in nature, their structural types are complex, and they mainly include flavonoids, flavonols, dihydroflavonols, isoflavones, dihydroisoflavones, chalcones, orange ketones, flavanoids, anthocyanidins, and biflavonoids. This review covers the plant distribution and pharmacological activities of flavonoids. Flavonoids are mainly distributed in angiosperms and gymnosperms, and they are abundant in plants such as Rutaceae, Labiatae, Zingiberaceae, Scrophulariaceae, and Leguminosae. Because of their wide distribution and variety, researchers have found that flavonoids have diverse biological activities, mainly focusing on anti-inflammatory, antibacterial and antitumor activities. Mechanistically, the anti-inflammatory effects are mainly related to the NF-κB and MAPK (mitogen-activated protein kinase) signaling pathway and then the inhibition of the production of inflammatory cytokines and mediators. The antibacterial activity is mainly manifested as inhibitory effects on many strains, including Escherichia coli, Cryptococcus neoformans, and Pseudomonas aeruginosa, via destroying the stability of the microbial membrane, inhibiting the invasion of virulent bacteria into host cells, promoting the apoptosis of bacteria, inhibiting bacterial fatty acid synthesis, etc. The antitumor activity of flavonoids is related to their inhibition of cell proliferation and induction of apoptosis via the mitochondria-mediated, endoplasmic reticulum-mediated, and death factor and its receptor-mediated signal transduction pathways. Understanding the plant distribution and pharmacological activity of flavonoids not only reveals the importance of identifying such valuable flavonoids in another genus or family but also provides a basis for fully exploiting the therapeutic potential of flavonoids.
文摘目的：探讨苏铁双黄酮对非小细胞肺癌A549细胞内皮抑素（Endostatin）、转化生长因子-β（Transforming growth factor-β,TGF-β）、信号传导及转录激活因子3（Signal transducers and activators of transcription3,STAT3）、β-链蛋白和紧密连接蛋白1（Zonula occludens-1protein,ZO-1）表达的影响.方法：苏铁双黄酮作用于A549细胞24h后,采用免疫荧光法检测endostatin、TGF-β的定位及表达量,实时荧光定量PCR法检测STAT3、β-catenin、TGF-β和ZO-1mRNA的表达,westernblot法检测STAT3、β-catenin蛋白的表达.结果：与空白组比较,苏铁双黄酮显著下调TGF-β、STAT3和β-catenin的表达,上调endostatin和ZO-1的表达,且呈明显的浓度依赖性.结论：苏铁双黄酮治疗肺癌的作用机制可能为：通过抑制TGF-β、STAT3和β-catenin的表达,增加endostatin和ZO-1的表达,进而发挥抗肿瘤的作用.
