Targets and underlying mechanisms related to the sedative and hypnotic activities of saponins from Rhodiola rosea L. (crassulaceae).

Rhodiola rosea L. (Crassulaceae) are popularly used as a natural supplement for the treatment of insomnia and anxiety. Here, saponin extracts from R. rosea were investigated for their roles on relieving sleeplessness. The levels of neurotransmitters, hormones, and inflammation cytokines in plasma, and the expression of 5-hydroxytryptamine (5-HT), γ-aminobutyric acid (GABA), prostaglandin D2 (PGD2), interleukin-1ß (IL-1ß) and interleukin-6 (IL-6) in the hypothalamus and hippocampus were detected using ELISA, RT-PCR, and western blotting. First, the butanol fraction extracted from R. rosea was collected as the total saponins (HJT-I), then a saponin-rich fraction (HJT-II) was obtained after the further purification of HJT-I. The saponin contents of HJT-I and HJT-II were 28.92% and 65.69%, respectively. Second, behavioral tests were performed and showed that both HJT-I and HJT-II could effectively reduce the duration of immobility in the tail suspension test, and shorten sleep latency and prolong the sleep duration time in the sodium barbital-induced sleeping test, with HJT-II better than HJT-I. Third, ELLISA results showed that the concentrations of GABA, 5-HT, norepinephrine (NA), PGD2, and IL-1ß in plasma were significantly increased after HJT-I and HJT-II administration, while IL-6 was decreased. HJT-I and HJT-II also exhibited differential modulation of the receptors of 5-HT, GABA, PGD2, and IL-1ß expression. In hypothalamus, HJT-II was more powerful than HJT-I in regulation of the GABAARα2, GABAARα3, and glutamic acid decarboxylase (GAD) 65/67 expression, as well as 5-HT2A and IL-1ß. As for DPR and PGD2, HJT-II was more effective in the hippocampus. The efficacy of HJT-I was better than HJT-II at stimulating GABAARα2, GAD 65/67, 5-HT1A, and IL-1ß expression in the hippocampus. In conclusion, the potential sedative and hypnotic effects of HJT-I and HJT-II may possibly be related to the serotonergic, GABAAergic, and immune systems, while the underlying mechanism of HJT-I and HJT-II differed from each other.

Inhibitory effect of chloroform extracts from Citrus aurantium L. var. amara Engl. on fat accumulation.

BACKGROUND: Excess lipid accumulation can accelerate the development of various metabolic diseases. Blossoms of Citrus aurantium L. var. amara Engl. (CAVA) have been reported to possess inhibitory capacities on lipid deposition. However, the constituents responsible for the observed bioactivity and the underlying mechanisms are still not clearly understood. PURPOSE: To screen constituents from blossoms of CAVA with inhibitory effects on lipid accumulation and to explore the action mechanism. METHODS: The chloroform (CHL) extracts are prepared from blossoms of CAVA by fractional extraction and are characterized using LC-MS assay. 3T3-L1 preadipocytes are induced with differentiation medium (DMI) and treated with CHL extracts. High fat diet (HFD)-induced obese mice are further established and administrated with CHL extracts for 12 weeks. Hematoxylin and eosin (HE) staining, Oil Red O staining, ELISA, RT-qPCR, western blot and 16S rRNA gene sequence methods are employed. RESULTS: 14 compounds are identified in CHL extracts and trigonelline hydrochloride, nobiletin and 7-demethylsuberosin are most abundant. CHL extracts treatment significantly inhibit differentiation of 3T3-L1 cells by regulating expression of preadipocyte factor-1 (Pref-1), fatty acid synthase (FAS) and CCAAT/enhancer binding protein α (C/EBPα). CHL extracts intervention also significantly attenuate features of obesity and improved plasma biochemical profiles in HFD-fed mice. HFD-triggered hepatic steatosis and epididymal adipose tissues (EATs) hypertrophy are also reversed by CHL extracts administration through enhancing antioxidant responses and modulating lipogenesis and energy expenditure-related genes and proteins. 16S rRNA gene sequence data further show that CHL extracts enhance the diversity of gut microbiota. CHL extracts at lower concentrations reduce the ratio of Firmicutes to Bacteroidetes and the abundance of Erysipelotrichaceae. CHL extracts at higher doses markedly increase the abundance of Lachnospiraceae. CONCLUSION: These findings suggest that CHL extracts probably suppress lipid accumulation through inhibiting differentiation of 3T3-L1 cells and attenuating metabolic syndromes in HFD-fed mice.

Origin and evolution of China Pharmacopoeia and its implication for traditional medicines.

Traditional Chinese Medicine (TCM) has a history that can be dated back to several thousand years ago. The extant earliest medical book is Huangdi Neijing (Canon of Internal Medicine, 770 BC~221 BC), and the earliest pharmacy monograph is Shengnong Bencao Jing (Shengnong Materia Medica, AD25~AD220). The most influential pharmacy monograph is the Bencao Gangmu (Compendium of Materia Medica, AD1368~AD1644). There were also many other far-reaching influencial monographs, which become the main and the most important derived resources of modern China pharmacopoeia for TCM. In this paper, we try to introduce some representative medicine and pharmacy works of ancient China, and elaborate the origin, development and improvement process of modern China pharmacopoeia, which may have referential significance for traditional and natural drugs. China Pharmacopoeia and TCM still have to face many problems in authenticity discrimination, action mechanism, and adverse reaction, etc. The improvement of China Pharmacopoeia still has room for progress with the solutions of modern analytical methods to the problems. The start-up and development of Herbalomics project will be helpful to further improve the China Pharmacopoeia, especially Chinese patented medicine and compound prescription.

Protective effects of diphenylheptanes from Curcuma phaeocaulis Val. on H2O2 induced cell injury.

Curcuma phaeocaulis Val. has been used as a health food in China for a long time. This research aimed to isolate and identify its active compounds with protective effects against hydrogen peroxide-induced PC12 cell death. 70% ethanol extracts of C. phaeocaulis were re-extracted and three fractions of water, petroleum ether and ethyl acetate were obtained. Three diphenylheptane compounds from the ethyl acetate fraction were identified for the first time from C. phaeocaulis, and compound III was considered to be a new structure. All of the three compounds displayed certain protective effects against toxicity in PC12 cells. For all concentrations, compound III displayed a more significant protective effect than ethanol extracts, the ethyl acetate fraction, and the other two compounds. At a concentration of 50 µg mL(-1), the survival rate of damaged PC-12 cells treated with compound III reached 84.7%. Diphenylheptanes were concluded to be the main compounds responsible for the health effects of C. phaeocaulis.