Notoginsenoside Ft1 acts as a TGR5 agonist but FXR antagonist to alleviate high fat diet-induced obesity and insulin resistance in mice

Obesity and its associated complications are highly related to a current public health crisis around the world. A growing body of evidence has indicated that G-protein coupled bile acid (BA) receptor TGR5 (also known as Gpbar-1) is a potential drug target to treat obesity and associated metabolic disorders. We have identified notoginsenoside Ft1 (Ft1) from

Probing the new strategy for the oral formulations of taxanes: changing the method with the situation / 中国天然药物

The first-generation taxanes (including paclitaxel and docetaxel) are widely used for the treatment of various cancers in clinical settings. In the past decade, a series of new-generation taxanes have been developed which are effective in the inhibition of tumor resistance. However, intravenous (i.v.) infusion is still the only route of administration, and may result in serious adverse reactions with respect to the utilization of Cremophor EL or Tween-80 as solvent. Besides, the dosing schedule is also limited. Therefore, oral administration of taxanes is urgently needed to avoid the adverse reactionss and increase dosing frequency. In this review, we first outlined the discovery and development of taxane-based anticancer agents. Furthermore, we summarized the research progress on the oral formulations of taxanes and proposed some thoughts on the future development of oral taxane formulations.

Chemical constituents and hypoglycemic activity of Phlomis tuberosa / 中草药

Objective: To study the chemical constituents and hypoglycemic activity of Phlomis tuberosa. Methods: The db/db diabetic mice was used to screen the hypoglycemic active site of P. tuberosa. The chemical constituents were isolated and purified by various separation and analysis techniques. The structures of these compounds were identified by spectroscopic analysis (1H-, 13C-NMR and MS). The hypoglycemic activities of these compounds were verified by the DPP-4 inhibitory activity in vitro. Results: Ethyl acetate extract of P. tuberosa showed significant hypoglycemic effect. Twenty-five compounds were isolated from the active site, containing β-stiosterol (1), stigmasterol (2), daucosterol (3), clerosterol-stigmast-4-ene-3,6-dione (4), 22-dehydro- stigmast-4-ene-3,6-dione (5), ellagic acid (6), ethyl gallate (7), gllagic acid (8), 4-hydroxybenzoic acid (9), 3,4-diohydroxybenzoic acid (10), cinnamic acid (11), p-hydroxy-cinnamic acid (12), caffeic acid (13), 5-hydromethylfuraldehyde (14), quinic acid (15), chlorogenic acid (16), ferulic (17), 2,3-dimethoxy-5-methyl-6-(3,7,11,15,19-pentamethyl-2,6,10,14,18-eicosapentaen-1- yl)-2,5-cyclohexadiene-1,4-dione (18), 1-O-caffeoyl- quinic acid (19), 3,5-dimethoxy-4-hydroxy-benzene carbonic-1-O-β-D-glucoside (20), 2-O-butyl-α-D-fructofuranoside (21), n-octadecanoic acid (22), stearic acid (23), methyl-5-(hydroxymethyl) furan-2-carboxylate (24) and 4-hydroxy-3-methoxy-benzaldehyde(25). Nine compounds were obtained from the genus Phlomis for the first time, in which ellagic acid (6), quinic acid (15), and 1-O- caffeoylquinic acid (19) showed strong DPP-4 inhibitory activity with IC50 of 72.3, 89.2, and 103.4 μmol/L, respectively. The IC50 of the positive drug diprotin A was 50 μmol/L. Conclusion: Compounds (3-7 and 18-21) are obtained from the genus Phlomis for the first time. Compound 6, 15, and 19 show DPP-4 inhibitory activities.

Non-operative treatment for patients with acute uncomplicated appendicitis / 中华全科医师杂志

Total 786 cases of acute uncomplicated appendicitis(UCAA) were included for analysis.All the cases were given antibiotics as a main treatment.Clinical cure rate and the number of cases requiring surgery were observed.Patients with conservative treatment were followed up and the recurrence was observed.Logistic regression was applied to analyze the risk factors of recurrence.Among 786 cases,774 (98.5％) were treated conservatively and achieved clinical cure;68 cases (9.0％) had recurrence during follow-up,the median time to recurrence was 11 months (1-33 months).Logistic regression analysis showed that age(OR =1.124,95％ CI:1.067-3.790,x2 =2.767,P =0.041) and appendix bezoar (OR =1.649,95％ CI:1.281-4.055,x2 =3.935,P =0.027) were independent risk factors for recurrence.Non-operative treatment for acute uncomplicated appendicitis shows a good short and long term effects.Surgical excision may be a better choice for the patients with high risks of recurrence.