Nine pairs of undescribed enantiomers from the resin of Styrax tonkinensis (Pierre) Craib ex Hart with anti-inflammatory activity.

Nine pairs of undescribed enantiomers, (±)-styraxoids A-I (1-9), were isolated from the resin of Styrax tonkinensis, and their structures were assigned by spectroscopic and computational methods. Compounds (±)-1 are a pair of degraded lignans, and the remaining compounds (±)-(2-9) are phenylpropanoid skeletons. Compounds (±)-8 and (±)-9 feature a 1,3-dioxolane moiety. The biological evaluation showed that both enantiomers of 1 could inhibit LPS-induced INOS and COX-2 in RAW264.7 cells in a dose-dependent manner.

Eight new 2-(2-phenylethyl)chromone derivatives from agarwood of Aquilaria sinensis with anti-inflammatory activity.

Eight previously unknown 2-(2-phenylethyl)chromone derivatives, called aquichromones A - E (1-3, 5 and 6) and 8-epi-aquichromone C (4), including two pairs of enantiomers [(±)-1 and (±)-2] were isolated from the agarwood of Aquilaria sinensis. The structures and absolute stereochemistry of these natural products were elucidated by using spectroscopic and computational methods. The result of biological assay showed that two members of this group, 4 and 5, have significant dose-dependent anti-inflammatory activity.

Six new diterpenoids from the resins of Populus euphratica and their anti-inflammatory activities.

Six new diterpenoids, identified as two abietane derivatives, euphraticanoids J and K (1 and 2), two pimarane derivatives, euphraticanoids L and M (3 and 4), and two 9,10-seco-abietane derivatives, euphraticanoids N and O (5 and 6) were isolated from Populus euphratica resins. Their structures including absolute configurations were characterized using spectroscopic, quantum chemical NMR, and ECD calculation methods. The anti-inflammatory activity of the compounds was tested and the results revealed that compounds 4 and 6 inhibited the production of iNOS and COX-2 in a dose-dependent manner in lipopolysaccharide (LPS)-induced RAW 264.7 cells.

Antifungal and wound healing promotive compounds from the resins of Dracaena cochinchinensis.

Five new compounds (xuejieins A-E), including three new phenolic glycosides (1, 2, and 5) and two new flavonoids (10 and 11), together with six known compounds were isolated from the resins of Dracaena cochinchinensis (Chinese dragon's blood). The structures of the new compounds were confirmed by extensive spectroscopic methods and electronic circular dichroism (ECD) data analysis. Especially, the absolute configurations of the sugar moieties in compounds 1, 2, and 5 were clarified by GC analysis after acid hydrolysis. All isolated compounds have been tested for antifungal and wound healing promoting activities, The results showed that compound 9 shows significant antifungal activities against Botrytis cinerea, Magnaporthe grisea, Penicillium digitatum, and Sclerotinia sclerotiorum. In addition, compound 4 could significantly stimulate human keratinocytes (HaCAT) proliferation, mobility, and human umbilical vein vascular endothelial cells (HUVECs) tube formation at 40 µM.

Populeuphrines A and B, two new cembrane diterpenoids from the resins of Populus euphratica.

Two new cembrane diterpenoids, named populeuphrines A and B (1 and 2), together with three known analogues (3-5) were isolated from the resins of Populus euphratica. The planar structures and relative configurations of 1 and 2 were elucidated by detailed 1 D and 2 D NMR spectroscopic analyses. The absolute configurations of 1 and 2 were determined by X-ray diffraction analysis and quantum chemical computation. Biological activities of all the isolates against proliferation of human cancer cells and umbilical cord mesenchymal stem cells were evaluated.

Discovery of Populusone, a Skeletal Stimulator of Umbilical Cord Mesenchymal Stem Cells from Populus euphratica Exudates.

Populusone (1), a cembrane-type macrocyclic trinorditerpenoid, was isolated from the exudates of Populus euphratica and shown to have an unprecedented carbon skeleton, The structure was identified using spectroscopic methods and X-ray crystallography. A possible pathway for the biosynthesis of 1 was proposed. Populusone (10 µM) was found to promote proliferation and differentiation of umbilical cord derived mesenchymal stem cells into keratinocyte like cells.

[Comparative effects of Roux-en-Y gastric bypass procedures preserving different gastric volume on blood glucose in Goto-Kakizaki rats].

OBJECTIVE: To compare the effects of Roux-en-Y gastric bypass (RYGBP)procedures preserving different gastric volume on blood glucose of rats with non-obese type 2 diabetes. METHODS: A total of 36 Goto-Kakizaki rats randomly underwent one of the following procedures: gastric bypass with different types of anastomosis including the Roux-en-Y of total stomach excision(n=12), the Roux-en-Y of partial stomach excision(n=12) and the Roux-en-Y of stomach preservation(n=12). Rats were observed for 24 weeks after surgery. Body weight, food intake and fasting blood glucose level were tested at 0(preoperative), 1, 3, 6, 12, 24 weeks. Hemoglobin A1c(HbA1c) level was measured at 0, 12, 24 weeks and glucose tolerance test (OGTT) was performed in conscious rats before (baseline) and then 30, 60, 120, and 180 minutes. Change of blood glucose over time was depicted. Area under curve(AUC) of glucose tolerance were calculated. RESULTS: Compared with preoperative levels, the weight and food intake of all the rats were significantly decreased at 1 week after surgery(P<0.01). At 3 weeks after operation, the weight and food intake were significantly increased compared with 1 week after operation in the Roux-en-Y of partial stomach excision and the Roux-en-Y of stomach retention(P<0.01). In the Roux-en-Y of total stomach excision, the weight and food intake were significantly lower compared with other two groups(P<0.05). At 24 weeks after operation, the levels of fasting blood glucose were (7.3 ± 1.5), (7.5 ± 2.0) and (8.3 ± 1.3) mmol/L, which were lower than the preoperative levels [(13.2 ± 1.6), (13.6 ± 2.5) and (12.9 ± 2.0) mmol/L, P<0.01] in the three groups. There were no significant differences among the three groups(P>0.05). At 24 weeks after operation, the HbA1c levels were(6.3 ± 1.3)%, (6.4 ± 2.0)% and (7.0 ± 1.3)%, which were lower than the preoperative level[(10.2 ± 2.6)%, (9.6 ± 2.5) and (9.9 ± 2.0)%, P<0.01]. There were no significant differences among the three groups(P>0.05). The trend of the glucose tolerance test and AUC were similar in the three groups after operation. CONCLUSION: Roux-en-Y gastric bypass in non-obese diabetic rats is effective in terms of glucose control and the efficacy of gastric bypass has no obvious association with the stomach volume.

[Effect of blood glucose control after small intestine exclusion surgery in Goto-Kakizaki rat with type 2 diabetes mellitus].

OBJECTIVE: To evaluate the effect of diabetic control after small intestine exclusion surgery in Goto-Kakizaki (GK) rat with type 2 diabetes mellitus. METHODS: GK type 2 diabetic rats underwent duodenal bypass (Group A, n = 8) creating a shortcut for ingested nutrients with bypassing duodenum alone, or duodenal-jejunal bypass (Group B, n = 8), a stomach-preserving RYGB excluding duodenum and proximal jejunum, or duodenum and total jejunum exclusion (Group C, n = 8), or sub-total small intestine exclusion (Group D, n = 8) creating a shortcut for ingested nutrients with bypassing duodenum, jejunum and sub-total ileum. Controls were pair-fed (PF) sham-operated and untreated GK rats (Group SO, n = 8). Rats were observed for 24 weeks after surgery. Fasting blood glucose (FBG) level was determined on a Surestep plus blood glucose meter (Lifescan) at 0, 1, 3, 6, 12, 24 week. Hemoglobin A1c (HbA1c) level was measured at 0, 12, 24 week on VARIANT Hemoglobin A1c Program (Bio-Ray) with high performance liquid chromatography (HPLC) method. RESULTS: The fasting blood glucose and HbA1c levels significantly decreased after surgery in all the operative groups through the entire follow-up period [Group B (FBG before surgery and 1 week after: (162 +/- 44) mg/dl vs (80 +/- 19) mg/dl; HbAlc before surgery and 12 week after: (8.2 +/- 2.2)% vs (5.1 +/- 1.5)%, P < 0.05 or P < 0.01]; while FBG had no differences before 12 week and significantly increased at 12 week (164 +/- 44) mg/dl and 24 week (180 +/- 42) mg/dl in group SO [preoperative (145 +/- 35) mg/dl, P < 0.01]. As compared with sham-operated rats, all the operative groups showed reduced blood-glucose and HbA1c levels through the entire follow-up period (P < 0.05 or P < 0.01). The FBG and HbA1c levels in Group B significantly decreased versus Group A [24 week (FBG: (82 +/- 21) mg/dl vs (111 +/- 27) mg/dl; HbA1c: (3.9 +/- 0.9)% vs (5.4 +/- 1.2)%, P < 0.05], indicating that duodenal-jejunal bypass had markedly a better effect of diabetic control. But Groups B, C and D were similar to one another (P > 0.05), suggesting that a potential role of proximal gut in the pathogenesis of disease. CONCLUSION: In spontaneous type 2 diabetes mellitus rats, all the small intestinal exclusion including proximal gut are effective in glucose control. In terms of intestinal nutrient absorption, duodenal-jejunal bypass may be an ideal surgery for clinical diabetic control. These findings suggest a potential role of proximal intestine in pathogenesis of type 2 diabetes mellitus.

[Effect of diabetes control after small intestine exclusion surgery in Goto-Kakizaki rat with non-obese type 2 diabetes mellitus].

OBJECTIVE: To evaluate the effect and possible mechanisms of diabetes control after small intestine exclusion surgery in Goto-Kakizaki (GK) rat with non-obese type 2 diabetes mellitus. METHODS: Forty GK rats with non-obese type 2 diabetes mellitus underwent duodenal bypass (Group A, n = 8), which creates a shortcut for ingested nutrients bypassing duodenum alone; duodenal-jejunal bypass (Group B, n = 8), a stomach-preserving RYGB that excludes the duodenum and proximal jejunum; duodenum and total jejunum exclusion (Group C, n = 8); sub-total small intestine exclusion (Group D, n = 8), which creates a shortcut for ingested nutrients bypassing duodenum, jejunum and sub-total ileum; controls were pair-fed (PF) sham-operated and untreated GK rats (Group SO, n = 8). The rats were observed for 24 weeks after surgery. Body weight, food intake and fasting blood glucose level were tested at 0, 1, 3, 6, 12, 24 weeks after the operation in those groups. The concentrations of insulin and glucagon-like peptide-1 (GLP-1) concentrations were measured before (baseline) and then 30, 60, 120, and 180 minutes after OGTT at 0, 12, 24 weeks after the operation. RESULTS: Mean operating time of all groups was similar. The mean body weight and food intake decreased significantly at 1 week after surgery (P < 0.01) and with no differences among the groups. Fasting blood glucose level decreased significantly after surgery in all the operation groups through the entire follow-up period (P < 0.05). No significant changes in fasting blood glucose level in SO group was found in 12 weeks after the operation, and it increased at 12 and 24 weeks after. Fasting blood glucose levels in group B decreased significantly compared with group A (P < 0.05), but no difference was found among group B, C and D (P > 0.05). Oral glucose-stimulated peak (30 min) levels of blood insulin and GLP-1 increased markedly in operation groups (A, B, C and D) after surgery (P < 0.01). Compared with group A, peak levels of blood insulin and GLP-1 in group B were strikingly higher (P < 0.05), but no difference was found when compared with group C or D (P > 0.05). CONCLUSIONS: In spontaneously non-obese type 2 diabetes mellitus rats, small intestinal exclusion including proximal gut is effective in terms of glucose control and has no direct relation with body weight and food intake loss. Restoration of the first-phase insulin secretion and high secretion of GLP-1 in type 2 diabetic subjects after gastrointestinal bypass surgery seem to be helpful to diabetes control. Taking intestinal nutrient absorption into consideration, duodenal-jejunal bypass may be a better surgery for diabetes control.

Effects of Ginkgo biloba extract on expressions of IL-1beta, TNF-alpha, and IL-10 in U937 foam cells.

This study is to investigate the protein and mRNA expressions of pro-inflammatory and anti-inflammatory cytokines in U937 foam cells and effects of Ginkgo biloba extract (GbE) on the cytokines. U937 cells were cultured with different concentrations of GbE (0.1, 1, and 10 microg x L(-1)), and stimulated by 100 mg x L(-1) oxidized low density lipoprotein (ox-LDL) for 24 h. The expressions of interleukin-1beta (IL-1beta), tumor necrosis factor-alpha (TNF-alpha) and interleukin-10 (IL-10) in culture solution were detected by enzyme-linked immunosorbant assay (ELISA) and reverse transcriptase polymerase chain reaction (RT-PCR). The results showed that incubated with 100 mg x L(-1) ox-LDL for 24 h, the U937 cells became foam cells, the protein or mRNA expressions of IL-1beta, TNF-alpha, IL-10, and its receptor IL-10R in U937 foam cells were higher markedly than those in normal U937 cells. When the cells were pretreated with GbE (0.1, 1, and 10 microg x L(-1)), the increases of IL-1beta and TNF-alpha in U937 foam cells were remarkably inhibited, but IL-10 expression increased greatly. Especially when cells were pretreated with 10 microg x L(-1) GbE, the protein and mRNA expressions of IL-1beta and TNF-alpha were markedly lower than those in U937 foam cells. The protein expression of IL-10 and mRNA expressions of IL-10 and its receptor IL-10R were markedly higher than those in U937 foam cells. GbE inhibited production of pro-inflammatory cytokines IL-1beta and TNF-alpha, but up-regulated the production of anti-inflammatory cytokine IL-10 and its receptor IL-10R in U937 foam cells, which might be related with its anti-atherosclerotic actions.

Expression of pro-inflammatory and anti-inflammatory cytokines in brain of atherosclerotic rats and effects of Ginkgo biloba extract.

AIM: To study the protein and mRNA expressions of pro-inflammatory and anti-inflammatory cytokines in the brain of rats with atherosclerosis (AS) and the effects of Ginkgo biloba extract (GbE) on expressions of cytokines. METHODS: The experimental model of AS in rats were established by intraperitioneal injection of vitamin D3 with high fat/cholesterol diet. GbE 100 mg/kg was administered to rats by ig. After 8 weeks, the expressions of IL-1beta, TNF-alpha, IL-10, and IL-10R in the brain tissues of AS rats were detected by enzyme-linked immunosorbant assay, immunohistochemistry, Western blotting, and reverse transcriptase polymerase chain reaction. RESULTS: The protein and mRNA expressions of IL-1beta, TNF-alpha, and IL-10 in the brains were markedly higher in AS groups than that in control groups (6.11+/-0.15, 1.55+/-0.14, 0.54+/-0.04 ng/g wet weight vs 0.80+/-0.14, 0.33+/-0.09, and 0.33+/-0.02 ng/g wet weight, respectively). The protein and mRNA expressions of IL-1beta and TNF-alpha in the brains were markedly lower in GbE groups (3.82+/-0.54, 0.95+/-0.08 ng/g wet weight) than that in AS groups, the protein and mRNA expressions of IL-10 and IL-10R in the brains were markedly higher in GbE groups (0.85+/-0.06 ng/g wet weight) than that in AS groups. CONCLUSION: GbE inhibited production of pro-inflammatory cytokines IL-1beta and TNF-alpha, but up-regulated the production of anti-inflammatory cytokines, IL-10 and IL-10R in brain, which might be related with its anti-AS actions.