Chemical Constituents from the Roots of Jasminum sambac (L.) Ait. and their Cytotoxicity to the Cancer Cell Lines.

BACKGROUND: The roots of J. sambac is the Traditional Chinese Medicine (TCM) with analgesic and anesthetic effects. However, relatively fewer studies on the chemical compositions and the biological activities of the roots of J. sambac have been carried out till now. We studied the chemical compositions of the roots of J. sambac planted in Fujian Province to discover new compounds from this TCM to develop new drugs or drug candidates. AIM: This work aims to find the new compounds from the roots of Jasminum sambac (L.) Ait. (J. sambac) for the development of new drugs or drug candidates. METHODS: The dichloromethane (DCM) extract was selected to isolate over silica gel column chromatography to obtain different polar fractions. Several similar fractions were combined according to Thin Layer Chemotherapy (TLC) or High-Performance Liquid Chromatography (HPLC) analysis. The combined fractions were reisolated by silica gel column chromatography, preparative TLC or HPLC to obtain nine pure compounds (1-9). The purity of the isolated compounds was detected by HPLC, and their structures were determined by 1D, 2D NMR, and HRESIMS analysis. The in vitro anticancer activity was evaluated using Cell Counting Kit-8 (CCK8) method. RESULTS: Nine compounds were isolated in this work. Compounds (1-3) are new compounds, while compounds (4-9) were isolated for the first time from the roots of J. sambac. Their structures were elucidated by 1D, 2D NMR, and HRESIMS analysis. The biological evaluation showed that compound 7 exhibited potent cytotoxic efficacy against MCF-7 cell lines with IC50 values of 148.3 µM for 24 hs and 35.94 µM for 48 hs, respectively; compound 1 displayed significant cytotoxic potential against MCF-7 cell lines with IC50 value of 38.5 µM for 24 hs; while compound 3 and 4 displayed potent cytotoxic effects against MCF-7 cell lines with IC50 values of 161.1 µM and 243.7 µM for 48 hs, respectively. CONCLUSION: We discovered new compounds from the roots of J. sambac. and several compounds exhibited potent cytotoxity to MCF-7 cell lines. This work encourages us to further study the chemical constituents and their biological activities from the roots of J. sambac.

New neo-Clerodane Diterpenoids Isolated from Ajuga decumbens Thunb., Planted at Pingtan Island of Fujian Province with the Potent Anticancer Activity.

AIMS: The aim of this study is to find the anticancer lead compounds or drug candidates from Chinese Traditional Plant Medicine of Ajuga decumbens Thunb. BACKGROUND: Ajuga decumbens Thunb. has been used in clinical for a long time in China and was selected in "Chinses Pharmacopoeia" (part I in 1977) for its wide spectrum biological activities: such as anticancer, antioxidant, antifeedant, antibacterial, anti-inflammatory, antihyperlipidemic, anti-cholinesterase and cytotoxicity activities. However, there are relatively fewer studies of Ajuga decumbens Thunb. that have been carried out till now. For some years, our research group focused on the discovery of new anticancer agents, so we studied the chemical compositions of Ajuga decumbens Thunb., planted in Pingtan island of Fujian Province, to discover new anticancer lead compounds or candidates from this Chinese Traditional Plant Medicine. METHODS: The dichloromethane (DCM) extract was obtained in this work, and then this extract was used for silica gel column chromatography to obtain different polar fractions. Several similar fractions were combined according to TLC or HPLC analysis. The combined fractions were isolated by preparative TLC or preparative HPLC to obtain the pure compounds and HPLC was used to detect the purity. All isolated compounds were determined by NMR (1HNMR, 13CNMR, DEPT, HMBC, HSQC, 1H-1H COSY and NOESY), HRESIMS and single crystal X-ray diffraction methods. The in vitro anticancer activity was evaluated using CCK8 method. RESULTS: Seven compounds [three new compounds 1-3; and four known compounds (Ajugacumbins A, Ajugacumbin B, Ajugamarin A2 and Ajugamarin A1)] were isolated from Ajuga decumbens Thunb. in this work, and their structures were confirmed. The biological evaluation showed that 3 and Ajugamarin A1 exhibited potent in vitro anticancer activity both against A549 cell lines with IC50s=71.4 µM and 76.7 µM; and against Hela cell lines with IC50s=71.6 mM and 5.39×10-7 µM, respectively. CONCLUSION: Compounds (3 and Ajugamarin A1) can be regarded as the lead compounds for the development of anticancer agents.

Advances in studies on the rupestonic acid derivatives as anti-influenza agents.

Rupestonic acid (isolated from the Chinese traditional medicine Artemisia rupestris L.) is a sesquiterpene with multifunctional groups and possess higher activity against influenza virus B. In order to improve the biological activity of rupestonic acid, many derivatives have been synthesized and their anti-influenza activity was screened. This review describes the rupestonic acid derivatives and their anti-influenza activity studied by our researching group.