Mogroside V, a component with high content and sweetness in mogrosides, has many pharmacological activities such as relieving cough, reducing sputum, anti-cancer, anti-oxidation, regulating blood sugar, making it a natural nonsugar sweetener with therapeutic functions, and showing a broad market prospect. However, the limited resources and high extraction costs have restricted its widespread use. The rapid development of synthetic biology has provided a new idea for the production of plant natural products. The low-cost and large-scale production will be realized through the construction of a microbial cell factory for mogroside V. Here, we briefly introduce the structure and pharmacological activity of mogroside V, and review progress in applying synthetic biology for its synthesis, and also discuss the challenges faced by the current research, to provide a reference for further studies on the biosynthesis of mogroside V.
Biological Products/chemistry* ; Sweetening Agents/chemical synthesis* ; Synthetic Biology ; Triterpenes/chemical synthesis*

We think the strategy of classic natural product-based drug discovery will be an effective way for us to develop new drugs with independent intellectual property. The strategy includes: to study the molecular mechanism of action of classic natural product with chemical genetics and chemical biology approaches firstly; then establish the proper in vitro bioassay or bioassay system based on its molecular mechanism for their pharmacodynamic evaluation; finally, study their structure-activity, structure-toxicity and structure-ADME properties with medicinal chemistry.
Animals ; Anti-HIV Agents ; chemical synthesis ; pharmacology ; Antineoplastic Agents, Phytogenic ; chemical synthesis ; pharmacology ; Berberine ; analogs & derivatives ; chemical synthesis ; pharmacology ; Biological Products ; chemical synthesis ; chemistry ; pharmacology ; Camptothecin ; analogs & derivatives ; chemical synthesis ; pharmacology ; Drug Discovery ; Humans ; Hypoglycemic Agents ; chemical synthesis ; pharmacology ; Oleanolic Acid ; analogs & derivatives ; chemical synthesis ; pharmacology ; Triterpenes ; chemical synthesis ; pharmacology ; Vinblastine ; analogs & derivatives ; chemical synthesis ; pharmacology

Structure of natural product-ursolic acid was modified for increasing its antitumor activity. Ursolic acid was acylated, esterified, hydrolized or oxidized to obtain target pentacyclic triterpenoid compounds with different substitutes. Sixteen derivatives of ursolic acid were designed and synthesized including eleven new compounds. Anti-tumor activities of ursolic acid and these derivatives against HeLa, SKOV3 and BGC-823 cells in vitro were investigated by MTT assay. The results indicated that compounds 7a and 8a were found to have stronger cell growth inhibitory than ursolic acid on HeLa cells and SKOV3 cells separately, and are worth to be intensively studied further.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; HeLa Cells ; Humans ; Triterpenes ; chemical synthesis ; chemistry ; pharmacology

Chemical modification was performed for improving the antioxidant activity of lead compound glycyrrhetinic acid (Ib). Two conjugated diene derivatives were prepared by reduction and dehydration reactions. Their in vitro antioxidant activities were studied using a cytochrome P450/NADPH reductase system from rat liver microsomes. The generation of microsomal free radicals was followed by oxidation of the DCFH-DA probe, while evaluating the capacity to inhibit reactive oxygen species (ROS) formation. The initial result showed that the two homo- and heterocyclic diene derivatives--18beta-olean-11,13(18)-diene-3beta, 30-diol (IV) and 18beta-olean-9 (11), 12-diene-3beta, 30-diol (V) exhibited strong antioxidant activities, at a concentration of 1.0 mg x mL(-1), they inhibited free radical (ROS) formation by 45% and 41%, respectively. In the same conditions, the lead compound (Ib) and the reference vitamin E inhibited ROS activity by 31% and 32%. Our results suggest that the elimination of the 11-keto group and the chemical reduction of 30-carboxylic group into hydroxyl function can increase the antioxidant activity of Ib significantly.
Animals ; Antioxidants ; chemical synthesis ; pharmacology ; Glycyrrhetinic Acid ; analogs & derivatives ; Male ; Microsomes, Liver ; metabolism ; Rats ; Reactive Oxygen Species ; metabolism ; Triterpenes ; chemical synthesis ; pharmacology

Betulinic acids are lupine-type pentacyclic triterpenoid saponins commonly found in some plants of Betulaceae family, especially in the bark of betula alba (birch). The potent anti-HIV and anti-tumor activities of betulinic acids have been greatly concerned. The natural betulinic acids include betulinic acid, 23-hydroxy betulinic acid, betulin and so on. Some investigations on the structural modifications of betulinic acids were carried out, and many derivatives with excellent biological activity have been obtained nowadays. In this paper, the research advances of the structural modification of betulinic acids, as well as their anti-HIV and anti-tumor activities are reviewed.
Anti-HIV Agents ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology ; Antineoplastic Agents, Phytogenic ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology ; Betula ; chemistry ; Cell Line, Tumor ; HIV ; drug effects ; Humans ; Plant Bark ; chemistry ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Triterpenes ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology ; therapeutic use