Phyllanthacidoid U: a new N-glycosyl norbisabolane sesquiterpene from Phyllanthus acidus (L.) skeels.

A novel highly oxygenated norbisabolane sesquiterpene, namely phyllanthacidoid U (1), along with nine known sesquiterpenes (2-10) was isolated from the roots and stems of Phyllanthus acidus (L.) Skeels (Phyllanthaceae), collected from Xishuangbanna, Yunnan province, China. Their structures were elucidated by means of extensive spectroscopic analysis and by comparison of their data with reported values in literatures. Instead of the C-13 ester O-glycosyl found mostly in the titled plant growing in Thailand, compound 1 possessed a rare N-ß-glucosamine-2-N-acetate moiety linked directly to the carbonyl at C-13 through an amido bond. Moreover, the acyl group at C-10 in 1 was (Z)-2-(2-hydroxyethyl)-pent-2-enedioyl group, instead of benzoic or p-hydroxybenzoic moieties found commonly in the reported norbisabolane sesquiterpenes. The known sesquiterpene 5 displayed stronger anti hepatitis B virus (HBV) activity with IC50 values of 1.69 ± 0.22 and 2.79 ± 0.69 µM towards HBV surface antigen (HBsAg) and HBV excreted antigen (HBeAg) secretion, respectively.

Phyllaciduloids A-D: Four new cleistanthane diterpenoids from Phyllanthus acidus (L.) Skeels.

Four new cleistanthane diterpenoids, phyllaciduloids A-D (1-4), were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels (Phyllanthaceae). Their structures were elucidated on the basis of extensive spectroscopic analysis. Phyllaciduloids B-D (2-4) present in their structures with ether bond between C-7 and C-16, which were rarely reported. All the isolates were evaluated for their cytotoxic activities against five human cancer cell lines.

Bioassay-guided isolation of saikosaponins with agonistic activity on 5-hydroxytryptamine 2C receptor from Bupleurum chinense and their potential use for the treatment of obesity.

5-Hydroxytryptamine 2C (5-HT2C) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtOH extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT2C receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT2C receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d (1), was determined by extensive spectroscopic analyses (HR-ESI-MS, IR, and 1D and 2D NMR). The primary structure-activity relationship study suggested that the intramolecular ether bond between C-13 and C-28 and the number of sugars at C-3 position were closely related to the 5-HT2C receptor agonistic activity. Saikosaponin a (3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT2C receptor with an EC50 value of 21.08 ± 0.33 µmol·L-1in vitro and could reduce food intake by 39.1% and 69.2%, and weight gain by 13.6% and 16.4%, respectively, at 3.0 and 6.0 mg·kg-1in vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.

[Effect of scalp acupuncture drawing method on motor function in hemiplegic patients following cerebral thrombosis at convalescent period].

OBJECTIVE: To observe the effect of scalp-acupuncture drawing method (SADM) on recovering motor function in hemiplegic patients following cerebral thrombosis at convalescent period. METHODS: Adopting randomized, single-blinded, controlled method, 93 patients suffering from hemiplegia following cerebral thrombosis were randomly assigned to 3 groups, 31 in each group. All patients were treated based on neurological routine therapy, those in the treated group and the control group I were treated respectively with SADM and scalp-acupuncture twirling method (SATM) additionally, but for those in the control group II, no additional treatment was given. The treatment course for all was 4 weeks. RESULTS: Before treatment, there were insignificant difference among 3 groups in the score of neural motor function deficits (NFDS) of limbs and activity of daily life (ADL) score (P > 0.05). After being treated for 4 weeks, the NFDS was significantly lower and in the control group II (P < 0.01, P < 0.05) and the change of the scores in the treated group was more than that in the control group I (P < 0.05). CONCLUSION: SADM was superior to scalp-acupuncture twisting prove the ADL score and motor function of hemiplegia patients following cerebral thrombosis in the convalescent stage.