Two new pentacyclic triterpene acids, 1a, 3b-dihydroxyl-olean-12-en-28-oic acid and 1a, 2a, 3b-trihydroxyl-olean-12-en-28-oic acid, were isolated from the arial parts of Sabia parviflora.
Botanical pentacyclic triterpenes possessed a broad range of pharmacological activities such as antioxidant,anti-tumor,anti-microbial and anti-inflammatory activities.It is believed that the mechanisms involved in the...Botanical pentacyclic triterpenes possessed a broad range of pharmacological activities such as antioxidant,anti-tumor,anti-microbial and anti-inflammatory activities.It is believed that the mechanisms involved in these bioactivities are due to the modulation of immune system.Recently,the pharmacological validation on immunomodulatory of pentacyclic triterpenes derived from higher plants is very limited and several existence review papers related for this group of compound have not been focused for this activity.In this review,we have highlighted several studies on immunomodulatory potential of botanical pentacyclic triterpenes isolated from wide array of different species of medicinal plants and herbs based on various preclinical in vitro and animal models.This review also attempts to discuss on bioactivities of compouns related with their structure-activity relationship.Hence,the evaluation of pentacyclic triterpenes offers a great opportunity to discover adjuvants and novel therapeutic agents that presented beneficial immunomodulatory properties.展开更多
A series of triterpene dimers bearing different scaffold were designed and synthesized via CuAAC reaction. Their anti-HCV entry activities were evaluated by HCVpp and VSVpp entry assays. It was found that echinocystic...A series of triterpene dimers bearing different scaffold were designed and synthesized via CuAAC reaction. Their anti-HCV entry activities were evaluated by HCVpp and VSVpp entry assays. It was found that echinocystic acid （EA） and its dimer were still necessary for maintaining anti-HCV entry activity, and replacement of EA by other triterpenes might significantly decrease its anti-viral activities. Using a linker bearing a piperazine group, compound 14 dramatically increased its potency with IC50 at 2.87 nmol/L. In addition, the undesired hemolytic effect of all these compounds was removed.展开更多
文摘Two new pentacyclic triterpene acids, 1a, 3b-dihydroxyl-olean-12-en-28-oic acid and 1a, 2a, 3b-trihydroxyl-olean-12-en-28-oic acid, were isolated from the arial parts of Sabia parviflora.
文摘Botanical pentacyclic triterpenes possessed a broad range of pharmacological activities such as antioxidant,anti-tumor,anti-microbial and anti-inflammatory activities.It is believed that the mechanisms involved in these bioactivities are due to the modulation of immune system.Recently,the pharmacological validation on immunomodulatory of pentacyclic triterpenes derived from higher plants is very limited and several existence review papers related for this group of compound have not been focused for this activity.In this review,we have highlighted several studies on immunomodulatory potential of botanical pentacyclic triterpenes isolated from wide array of different species of medicinal plants and herbs based on various preclinical in vitro and animal models.This review also attempts to discuss on bioactivities of compouns related with their structure-activity relationship.Hence,the evaluation of pentacyclic triterpenes offers a great opportunity to discover adjuvants and novel therapeutic agents that presented beneficial immunomodulatory properties.
基金Acknowledgement This work was supported by the National Natural Science Foundation of China （No. 81560560）, Open-Fund Program of the State Key Laboratory of Natural and Biomimetic Drugs （No. K20160209） and Yunnan Basic Research Project （No. 14051789）.
文摘A series of triterpene dimers bearing different scaffold were designed and synthesized via CuAAC reaction. Their anti-HCV entry activities were evaluated by HCVpp and VSVpp entry assays. It was found that echinocystic acid （EA） and its dimer were still necessary for maintaining anti-HCV entry activity, and replacement of EA by other triterpenes might significantly decrease its anti-viral activities. Using a linker bearing a piperazine group, compound 14 dramatically increased its potency with IC50 at 2.87 nmol/L. In addition, the undesired hemolytic effect of all these compounds was removed.
