Search Results (3)

Aglaia cucullata is a mangrove plant with a tropical Asian distribution. It is used as traditional medicine for the treatment of diarrhea, inflammation, skin diseases, and heart diseases. Several compounds isolated from A. cucullata have demonstrated cytotoxic activity against various human cancer cells. Cancer therapies such as surgery, chemo-, and radiotherapy have many side effects. However, the use of natural bioactive compounds such as triterpenoid in cancer treatment can be used as an alternative to reduce these side effects. Therefore, the discovery of bioactive compounds from plants is very important to improve aspects of discovery and development of sustainable new anticancer drug candidates. Here, we report the chemical structures of seven known dammarane-type triterpenoids (1–7) isolated from A. cucullata exocarp and evaluate their cytotoxicity against B16-F10 melanoma skin cancer cells. The isolated compounds included cabraleahydroxylactone 3α-acetate (1), (20S)-20-hydroxydammar,24-en-3α-ol (2), (20S)-20-hydroxydammar,24-en-3-on (3), methyl 20(S)-hydroxy-3,4-secodammar-4(28),24-diene-3-oic acid (4), 3-epi ocotillol II (5), cabraleone (6), and ocotillone (7). The n-hexane extract was found to be active against B16-F10 cells, exhibiting an IC₅₀ value of 7.85 ± 0.22 µg/mL. Fractionation of this extract subsequently identified the compound (20S)-20-hydroxydammar 24-en-3-on (3) as an active substance with an IC₅₀ value of 21.55 ± 0.25 µM, comparing favorably with the positive control cisplatin (12.90 µg/mL; 43.00 µM). These results provide further evidence of the genus Aglaia as a source of cytotoxic cancer drug leads. In addition, compound 3 has potential as a convincing therapeutic agent for further research in the context of sustainable drug development, especially the development of new safe cancer chemotherapeutic agents. Full article

Ginseng is one of the most widely consumed herbs in the world and plays an important role in counteracting fatigue and alleviating stress. The main active substances of ginseng are its ginsenosides. Ocotillol-type triterpenoid is a remarkably effective ginsenoside from Vietnamese ginseng that has received attention because of its potential antibacterial, anticancer and anti-inflammatory properties, among others. The semisynthesis, modification and biological activities of ocotillol-type compounds have been extensively studied in recent years. The aim of this review is to summarize semisynthesis, modification and pharmacological activities of ocotillol-type compounds. The structure–activity relationship studies of these compounds were reported. This summary should prove useful information for drug exploration of ocotillol-type derivatives. Full article

Antibiotic resistance has become a serious global problem that threatens public health. In our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial activity. Based on preliminary structure-activity relationship, novel serious C-3 substituted ocotillol-type derivatives 7–26 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5α, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 7–14, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 μg/mL against MRSA USA300 and 4 μg/mL against B. subtilis. The structure-activity relationships of all current ocotillol-type derivatives our team synthesised were summarized. In addition, the prediction of absorption, distribution, metabolism, and excretion (ADME) properties and the study of pharmacophores were also conducted. These results can provide a guide to further design and synthesis works. Full article