Two new sesquiterpenes from the stems of Tripterygium wilfordii.

Two new ß-dihydroagarofuran-type sesquiterpenes 1ß,2α,6α,8ß,15- pentaacetoxy- 9α-benzoyloxy- ß-dihydroagarofuran (1) and 1ß,2ß,6α,15-tetraacetoxy-9ß-benzoyloxy- ß-dihydroagarofuran (2), together with five known abietane diterpenoids (3-7) were isolated from ethyl acetate extract of stems of Tripterygium wilfordii. Their structures were elucidated on the basis of detailed spectroscopic and physico-chemical analyses. All the isolates were evaluated for in vitro inhibitory activity against A549, HOS and MCF-7. Among them, compounds 4 and 5 exhibited manifest inhibition on A549, HOS and MCF-7 cancer cell lines.

Four new compounds isolated from Psoralea corylifolia and their diacylglycerol acyltransferase (DGAT) inhibitory activity.

A new bakuchiol compound Δ11-12-hydroxy-12-dimethyl bakuchiol (1), a new flavanone compound 2(S)-6-methoxy-7- hydroxymethylene-4'-hydroxyl-flavanone (8), and two new isoflavanone compounds 4',7-dihydroxy-3'-(6"ß-hydroxy-3″,7″-dimethyl-,2″,7″-dibutenyl)-geranylisoflavone (9) and 4',7-dihydroxy-3'-(7″-hydroxy-7″-methyl-2″,5″-dibutenyl)-geranylisoflavone (10) together with eight known compounds (2-7, 11, 12) were isolated from the P. corylifolia. Their structures were elucidated on the basis of spectroscopic and physico-chemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1/2. Among them, compounds 3, 9 and 10 were found to exhibit selective inhibitory activity on DGAT1 with IC50 values ranging from 93.7 ±â€¯1.3 to 96.2 ±â€¯1.1 µM. Compound 1 showed inhibition activity on DGAT1 with IC50 values 73.4 ±â€¯1.3 µM and inhibition of DGAT2 with IC50 value 121.1 ±â€¯1.3 µM.

Effect of Qi Kwai Granule particles on expression of TGF-β1 and MCP-1 in kidney of diabetic nephropathy rats / 中国药理学与毒理学杂志

OBJECTIVE To observe the effect of Qi Kwai Granule particles on the expression of in-terleukin 6 (IL-6), monocyte chemotactic protein 1(MCP-1) and transforming growth factor-β1(TGF-β1) in diabetic nephropathy(DN)rats and evaluate the protective effect of Qi Kwai Granule particles against renal injury of diabetic nephropathy. METHODS This experiment adopts adopted the high-sugar-high-fat diet and intraperitoneal injection of 2％ STZ+unilateral renal ligation to establish rat model of diabet-ic nephropathy.50 model rats were then randomly divided into model group,Irbesartan group,Qi Kwai Granule particles of high, medium, low dose group, 10 rats in each group. 10 normal rats were set as the sham operation group.Intragastric administration for 8 weeks were measured in rats.Measure the value of rat blood glucose by blood glucose meter,the determination of serum interleukin 6(IL-6)con-tent by ELISA, the expression of MCP-1 and TGF-β1by immunohistochemistry method. The value of rat blood glucose were measured by blood glucose meter.Serum interleukin 6(IL-6)were determinat-ed by ELISA.Expression of MCP-1 and TGF-β1were evaluated by immunohistochemistry method.RE-SULTS The blood glucose of Qi Kwai Granule particles of high,medium groups were decreased com-pared with those of the model group(P<0.05).The content of IL-6 of Qi Kwai Granule particles of high, medium groups were reduced(P<0.01). The content of MCP-1, TGF-β1in kidney of Qi Kwai Granule particles of high, medium, low dose groups were decreased (P<0.01). CONCLUSION Qi Kwai parti-cles have protective effect on renal tissue of diabetic nephropathy rats.Its mechanism might be related to the decrease of blood glucose value and IL-6,the inhibition of the expression of MCP-1 and TGF-β1.

Four new neolignans isolated from Eleutherococcus senticosus and their protein tyrosine phosphatase 1B inhibitory activity (PTP1B).

Four new compounds, erythro-7'E-4-hydroxy-3,3'-dimethoxy-8,5'-oxyneoligna-7'-ene-7,9-diol-9'-al (1), (7S,8S)-4-hydroxy-3,1',3'-trimethoxy-4',7-epoxy-8,5'-neolign-9-ol (5), (7S,8S,7'E)-5-hydroxy-3,3'-dimethoxy-4',7-epoxy-8,5'-neolign-7'-ene-9,9'-diol (6) and (7S,8S,7'E)-5-hydroxy-3,3',9'-trimethoxy-4'-7-epoxy-8,5'-neolign-7'-ene-9-ol (7). Along with four known compounds (2-4, 8) were isolated from the EtOAc-soluble extract of Eleutherococcus senticosus. Their structures were elucidated on the basis of spectroscopic and physicochemical analyses. All the compounds were evaluated for in vitro inhibitory activity against PTP1B, VHR and PP1. Among them, compounds 1-4 and 6-8 were found to exhibit selective inhibitory activity on PTP1B with IC50 values ranging from 17.2±1.6 to 32.7±1.2µM.

Treatment of Early Diabetic Retinopathy by Liuwei Dihuang Pill Combined Ginkao Leaf Tablet / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To observe the prevention and clinical efficacy of combination of Liuwei Dihuang Pill (LDP) and Ginkgo Leaf Tablet (GLT) for early diabetic retinopathy (DR).</p><p><b>METHODS</b>Using randomized, double-blind, double simulation, parallel controlled clinical trial, 140 type 2 diabetes mellitus (T2DM) outpatients were recruited and assigned to the treatment group and the control group, 70 in each group. All patients received basic Western medicine treatment (such as blood glucose and pressure control). Patients in the treatment group took LDP (8 pills each time, 3 times per day) and GLT (19.2 mg each time, 3 times per day), while those in the control group took LDP placebos and GLT placebos. All treatment lasted for 24 consecutive months. All subjects were followed-up every month. The general clinical data as sex, age, and metabolic data such as blood glucose, blood pressure, blood lipid, and DR prevalence rate were collected and statistically analyzed.</p><p><b>RESULTS</b>There was no significant difference in levels of blood glucose, blood pressure, or blood lipid between the two groups (P > 0.05). After treatment the DR incidence rate was significantly lower in the treatment group than in the control group [3.1% (2/64) vs 18.6% (11/59), P < 0.05)]. Meanwhile, the DR prevalence rate of the treatment group was also significantly lower than that of the control group [6.3% (4/64) vs 20.0% (13/59), P < 0.05].</p><p><b>CONCLUSION</b>Combination of LDP and GLT could effectively prevent and treat the development of DR in T2DM patients.</p>

Effect of Liuwei Dihuang soft capsule and Ginkgo leaf tablet on serum regulated upon activation, normal T cell expressed and secreted in patients with diabetes mellitus type 2 / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To investigate the effect of Liuwei Dihuang Soft Capsule(LDSC) and Ginkgo Leaf Tablet (GLT) on serum regulated upon activation, normal T cell expressed and secreted (RANTES) in the patients with diabetes mellitus type 2 (DM2).</p><p><b>METHODS</b>Forty patients with early stage DM2 were randomly assigned to two groups, 20 in each group. Based on the conventional treatment with hypoglycemic agents, patients in the treated group were treated with LDSC plus GLT additionally, and those in the placebo group with placebo for 6 months, respectively. The levels of serum RANTES, blood glucose, blood lipids and glycosylated hemoglobin, as well as micro-content of albumin in urine were measured before and after treatment.</p><p><b>RESULTS</b>In the treated group, the serum level of RANTES decreased significantly after treatment, and it was significantly lower as compared with that in the control group (P < 0.05).</p><p><b>CONCLUSIONS</b>LDSC and GLT can decrease serum RANTES level in patients with DM2. They play a preventive and therapeutic role on diabetic complications by their anti-inflammatory effect.</p>