Synthesis and antibacterial activity of a series novel 5,7-diisoprenyloxyflavone derivatives

In the present study, a series of novel 5,7-diisoprenyloxyflavone derivatives were designed, synthesized, and evaluated for their antibacterial activity. Most of these compounds displayed significant antibacterial effects against Gram-positive bacteria, especially against strains of multidrug-resistant clinical isolates. Compounds 4c, 4g, 4i, 4j, 4k, 4l, 4n, 4q and 4t showed high levels of antimicrobial activity against Staphylococcus aureus RN4220 with minimum inhibitory concentrations of 4.0-20 µM. Compound 4k showed the most potent activity among these compounds against all multidrug-resistant clinical isolates tested. Unfortunately, none of the compounds were active against Gram-negative bacteria at the doses of 24-164 µM.

Studies on chemical constituents from Isodon eriocalyx distributed in Hezhang / 中草药

Objective: To study the chemical constituents of Isodon eriocalyx. Methods The chemical constituents were isolated and purified by chromatography with silica gel, Sephadex LH-20 and semi-preparative HPLC, and their structures were identified by analysis of spectroscopic data and physicochemical properties as well as relevant references. Results :A total of 20 constituents were isolated from I. eriocalyx, plant material extracted with ethyl aceta, and they were elucidated as maoecrystal D (1), isothymusin (2), coetsoidin A (3), maoecrystal A (4), 5,4’-dihydroxy-6,7-dimethoxy flavone (5), vitexin (6), α-amyrin (7), β-daucosterol (8), odinicin (9), cirsimaritin (10), maoecrystal N (11), epi-macoecrystal P (12), pimaric acid (13), laxiflorin R (14), enmelol (15), maoecrystal B (16), pectolarigenin (17), neolaxiflorin V (18), eriocalyxin A (19), and neorabdosin (20). Conclusion: Compounds 2, 5-7, 13-15, 17, 18 are isolated from this plant for the first time, and compounds 5 and 6 are isolated from the plants of Isodon for the first time.

Chemical constituents from Rabdosia phyllopoda / 中草药

Objective: To investigate the chemical constituents of Rabdosia phyllopoda. Methods: The chemical constituents were isolated and purified by chromatography with silica gel, Sephadex LH-20 and by semi-preparative HPLC, and their structures were identified by analysis of spectroscopic evidences and physicochemical properties. Results: A total of 14 constituents were isolated from R. phyllopoda and elucidated as (Z)-1,1’-biindenyliden (1), β,β-carotene (2), germacrene B (3), 2α,3α,24-trihydrxyolean-12- en-28 oic acid (4), ferulic acid hexacosanyl ester (5), ergosterol peroxide (6), ursolic acid (7), α-amyrin acetate (8), obtusalin (9), betulinic acid (10), 2α,3α,19α-trihydroxy-12-en-28-urs acid (11), 2α,3α-dihydroxyl-12-ene-28 oic acid (12), 2α-hydroxyursolic acid (13), and lutein (14). Conclusion: The 14 compounds are isolated from this plant for first time, and compound 1, 3, 6, 9, 14 are isolated from the plants of R. phyllopoda for the first time.

Chemical constituents from Isodon coetsa distributed in Guizhou / 中草药

Objective: To investigate chemical constituents from Isodon coetsa distributed in Guizhou. Methods: Chemical constituents were isolated and purified by chromatography with silica gel, Sephadex LH-20, and semi-preparative HPLC, and their structures were identified by analysis of spectroscopic evidences and physicochemical properties as well as relevant references. Results: A total of 19 compounds were isolated from plant material extracted with 95% aqueous methanol, which were elucidated as β-sitosterol (1), stigmasterol (2), β-daucosterol (3), methyl linolenat (4), 9,12-octadecadienoic acid-2-hydroxy-1,3-propanedinyl ester (5), ursolic acid (6), oleanoic acid (7), 3β-hydroxy-urs-20-en-28-oic acid (8), betulinic acid (9), kurarinone (10), maslinic acid (11), 2α-hydroxy ursolic acid (12), 2α,3α-dihydroxy-urs-12-en-28-oic acid (13), 2α,3α,24-trihydrxyolean-12-en-28-oic acid (14), 2α,3β,24- trihydroxyolean-12-en-28-oic acid (15), formononetin (16), emodin (17), uracil (18), and sucrose (19). Conclusion: Compounds 2, 4, 5, 9, 11, 13-19 are isolated from this plant for first time, and compounds 11, 17, 19 are isolated from the genus of Isodon for the first time.

Double-balloon enteroscopy in diagnosis of small intestinal disease / 中国内镜杂志

Objective To explore the clinical value of double-balloon enterocopy (DBE) in diagnosis of small intestinal diseases. Methods The clinical and endoscope image data of 231 patients with suspected small bowel disease who underwent DBE from January 2008 to May 2016 were analyzed. Result 231 patients received 257 times of DBE examination, 112 of them were performed by oral and 93 by anal route, 26 patients were underwent by both approaches. The detection rate of intestine diseases was 64.9% (150/231), include 33 cases (14.3%) of nonspecific enteritis, 27 cases (11.7%) of crohn's disease, 19 cases (8.2%) of ulcer, 13 cases (5.6%) of intestinal vascular malformation, 12 cases (5.2%) of small intestinal stromal tumor. The lesion detection rate in obscure abdominal pain and obscure gastrointestinal bleeding were 59.6% (62/104) and 67.0% (63/94). In all patients, there were 1 case of small bowel perforation, the remaining patients had no serious complications such as bleeding and perforation. Conclusion The positive detection rate of double-balloon enteroscopy examination is high, and the double-balloon enteroscopy examination is relatively safe. So, double-balloon enterscopy examination has high diagnostic value for detecting small intestine diseases.

Effect of grape seed proanthocyanidins on phenotype marker protein of renal cells in db/db mice / 临床与实验病理学杂志

Purpose To investigate the effect of grape seed proanthocyanidins on the phenotype-transforming marker protein expression of db/db renal cells in mice model of type 2 diabetes,and to explore the protective mechanism of grape seed extract on diabetic renal injury in db/db mice.Methods Male db/db diabetic mice were randomly divided into two groups:diabetic group (db/db group) and diabetic + grape seed proanthocyanidin extract group (db/db + GSPE).The same week-old male db/m mice was used as normal controls (db/m) and grape seed proanthocyanidin extract gavage treatment group (db/m +grape seed proanthocyanidin extract group,db/m + GSPE).The mice of db/db + GSPE group and db/m + GSPE group were administered daily with grape seed proanthocyanidin extract (5mg/kg) by gavage.Results Renal tissues of db/db diabetic mice showed increased expression of α-SMA,p-p38MAPK,pERK1/2 and 8-OHdG level,and down-regulation in E-cadherin expression compared with db/m group (P ＜ 0.05).However,the alternations of α-SMA,p-p38,p-ERK1/2,E-cadherin protein levels,and 8-OHdG level,in db/db group were reversed by addition of grape seed proanthocyanidin extract (P ＜ 0.05).Conclusion Grape seed proanthocyanidin extract inhibits the epithelial to mesenchymal transition (EMT) associated protein,by decreasing ROS production,and activating p38 MAPK and ERK1/2.These findings suggest that grape seed proanthocyanidin extract provides a treatment option for diabetic nephropathy.

Double-balloon enteroscopy in diagnosis of small intestinal disease / 中国内镜杂志

Objective To explore the clinical value of double-balloon enterocopy (DBE) in diagnosis of small intestinal diseases. Methods The clinical and endoscope image data of 231 patients with suspected small bowel disease who underwent DBE from January 2008 to May 2016 were analyzed. Result 231 patients received 257 times of DBE examination, 112 of them were performed by oral and 93 by anal route, 26 patients were underwent by both approaches. The detection rate of intestine diseases was 64.9% (150/231), include 33 cases (14.3%) of nonspecific enteritis, 27 cases (11.7%) of crohn's disease, 19 cases (8.2%) of ulcer, 13 cases (5.6%) of intestinal vascular malformation, 12 cases (5.2%) of small intestinal stromal tumor. The lesion detection rate in obscure abdominal pain and obscure gastrointestinal bleeding were 59.6% (62/104) and 67.0% (63/94). In all patients, there were 1 case of small bowel perforation, the remaining patients had no serious complications such as bleeding and perforation. Conclusion The positive detection rate of double-balloon enteroscopy examination is high, and the double-balloon enteroscopy examination is relatively safe. So, double-balloon enterscopy examination has high diagnostic value for detecting small intestine diseases.

Study on lateral buds induction and culture of Huperzia serrata / 中草药

Objective: Due to the low reproductive capacity and scarce resources of Huperzia serrata, and in vitro culture of H. serrata has not been really successful, we wish to make a good progress in rapid propagation in this study. Methods: Living shoot tips were used as the materials, after a variety of surface sterilization, malachite green and AAS were used to eliminate the endophytic fungi of the seedling. Then, the aseptic seedlings were transplanted to the medium with 1/2 MS + 25 g/L sucrose to be cultured. After the new dichotomous branching occurred, and the branches grew to 4-5 cm high, we cut it and subcultured for the new dichotomous branching. Results: After four times of subculture of dichotomous branching, the aseptic seedlings got the different number of proliferating lateral buds, which came from the middle or top of the stem. Comparing the structure of lateral buds with the gemma, we found it was significantly different from the gemma. The number of lateral buds from different individuals was different, the most lateral buds could get to 14 in one seedling, some lateral bud generating point can produce two or more lateral buds. After removing the apical dominance of stem tip, the lateral buds in the middle of the stem grew faster. The surviving rate of different height lateral buds was different when they separated from the stock plant. Lateral buds which beyond 5 mm, the surviving rate could get 90%, while cultured in medium of 1/2 MS + 30 g/L sucrose, after 120 d, it grew into seedling about 2-3 cm high, lateral buds less 5 mm had high mortality with the same cultured medium. Conclusion: Though in vitro culture, H. serrata can break the reproductive way by which the leaf axil could generate spore only but no lateral bud naturally, and can produce the multiple lateral bud proliferation. The lateral buds can easily produce adventitious roots by stripping, which could provide an important view for rapid reproduction of H. serrata.

Comparison of effect between early and delayed in primary intramedullary nailing combined with locked plate fixation for the treatment of multi-segments tibial fractures of type / 中国骨伤

<p><b>OBJECTIVE</b>To compare the clinical results of early and delayed intramedullary nailing and locked plating for the treatment of multi-segments tibial fractures of type AO/ASIF-42C2.</p><p><b>METHODS</b>Between January 2010 and January 2013,45 patients with multi-segments closed tibial fractures of AO/ASIF-42C2 were treated by early primary intramedullary nailing and locked plating in 20 cases as early group and delayed in 25 cases as delayed group. In early group,20 cases included 13 males and 7 females with an average age of (37.9±14.3) years old ranging from 20 to 56 years;according to soft tissue injury Tscherne classification, 8 fractures were frade I,12 were grade II. In delayed group, 25 cases included 17 males and 8 females with an average age of (38.7±17.2) years old ranging from 24 to 55 years,4 fractures were grade I ,19 were grade II ,2 were grade III. The operative time, blood loss, hospital stay,fracture healing time and complications were recorded. At final follow-up, the Johner-Wruhs score were used to evaluate functional efficacy, and the posterior-anterior and lateral X-ray to evaluate fracture reduction and alignment.</p><p><b>RESULTS</b>All the patients were followed up for (12.5±2.5) months in early group and (13.2±2.8) months in delayed group (P>0.05). No wounds infections were happened. At the last follow-up, the mean range of knee joint was 10°-0°-120°. According to Johner-Wruhs scoring,there were 15 cases in excellent,3 in good,fair in 2 in early group; 21 in excellent,2 in good,2 in fair. The average operative time,blood loss had no significant differences between two groups (P>0.05), but hospital stay in early group was significantly shorter than those in delayed group(P<0.05). Average fracture healing time of early group and delayed group were (5.3±2.6) months and (6.0±2.9) months, respectively (P>0.05).</p><p><b>CONCLUSION</b>For multi-segments tibial fractures of type AO/ASIF-42C2 with preoperative minor soft tissue injuries lighter of Tscherne grade I or II, early primary intramedullary nailing and locked plating does not significantly increase the postoperative incidence of soft tissue complications for patients. The early and delayed primary intramedullary nailing and locked plating for treatment of AO/ASIF-42C2 proximal third tibial fractures can get similar curative effect.</p>

Effect of different durations of overdistention on rat bladder function and morphology

We investigated the contribution of the duration of overdistention (DOD) to rat bladder function and morphology and explored its possible molecular mechanisms. Bladder overdistention was induced in male Sprague-Dawley rats (200-250 g) by an infusion of saline. Forty rats were divided into 5 groups submitted to different DOD, i.e., 1, 2, 4, and 8 h, and control. Bladder function was evaluated by cystometry. Morphological changes were observed by light and transmission electron microscopy. Compared to control (44.567 ± 3.472 cmH2O), the maximum detrusor pressure of groups with 2-, 4- and 8-h DOD decreased significantly (means ± SEM): 32.774 ± 3.726, 31.321 ± 2.847, and 29.238 ± 3.724 cmH2O. With the increase of DOD, inflammatory infiltration and impairment of ultrastructure were more obvious in bladder tissue. Compared to control (1.90 ± 0.77), the apoptotic indexes of groups with 1-, 2-, 4-, and 8-h DOD increased significantly (6.47 ± 2.10, 10.66 ± 1.97, 13.91 ± 2.69, and 18.33 ± 3.28%). Compared to control (0.147 ± 0.031/0.234 ± 0.038 caspase 3/β-actin and Bax/Bcl-2 ratios), both caspase 3/β-actin and Bax/Bcl-2 ratios of 1-, 2-, 4-, and 8-h DOD increased significantly (0.292 ± 0.037/0.508 ± 0.174, 0.723 ± 0.173/1.745 ± 0.471, 1.104 ± 0.245/4.000 ± 1.048, and 1.345 ± 0.409/8.398 ± 3.332). DOD plays an important role in impairment of vesical function and structure. With DOD, pro-apoptotic factors increase and anti-apoptotic factors decrease, possibly contributing to the functional deterioration and morphological changes of the bladder.

Effects of deltamethrin on neurobehavioral development of offspring of intoxicated rats / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To investigate the effects of deltamethrin on the filial brain nitric oxide synthase (NOS) activity and neurobehavioral development of the exposed lactational rats.</p><p><b>METHODS</b>Pregnant rats were randomizedly divided into the treated group and the control group. The treated group was administered orally with 3.35, 6.70 mg/kg deltamethrin every other day from postnatal day (PND) 1 to PND 19 while the control group was administered with the corn oil of same amount in the same period. The activity of NOS of filial brain and neurobehavioral functions of the filial rats were observed.</p><p><b>RESULTS</b>The lactational survival rate (81.80%:78.60%) in both treated groups was decreased significantly (P < 0.01) compared with that in the control group. The body weight of filial rats on PND 10, 21 in 6.70 mg/kg DM treated group [(16.62 +/- 2.2 8), (31.34 +/- 6.94) g] was less than those in the control group (P < 0.05). The delayed time in the filial rats in 6.70 mg/kg group was (3.05 +/- 1.20) s and the positive rates of passive escaping response in 3.35 and 6.70 mg/kg DM treated group were 22.5% and 21.5% respectively. There was the trend of the developmental increase of the activity of filial brain NOS between PND 5 and PND 21 and the NOS activity of rat brain on PND 5 in 6.70 mg/kg group [(0.60 +/- 0.07) U.mg pro(-1).h(-1)] was lower than that in the control group (P < 0.05).</p><p><b>CONCLUSION</b>Exposure to high dose of deltamethrin in lactational female rats will decrease the activity of NOS of brain and retard the neurobehavioral development of their filial rats.</p>

Lignan: an important natural estrogen from plants / 中国中药杂志

Lignan is an important phytoestrogen with weakly estrogenic and anti-estrogenic properties, and possesses diverse bioactivities, including antioxidation, antitumor and antivirus etc. In particular, it may prevent hormone-dependent diseases, such as breast cancer, prostate cancer and benign prostatic hyperplasia. However, many important scientific problems have not been constrained, whether do the metabolites of lignans from foods have their potential genic toxicity? What are the anticancer mechanisms of lignans? What is the dosage of lignans to achieve the desired biological effect? In this paper, the references on lignans have systematically been reviewed in the following aspects: classification, distribution, metabolism, pharmacological activities and analytical methods, and a prospective of future studies on lignans is also elucidated.

Effects of deltamethrin on cell survival rate and intracellular free Ca2+ concentration in primary cultured astrocytes of rat / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To study the effects of deltamethrin (DM) on cell survival rate and intracellular Ca(2+) ([Ca(2+)]i) concentration in primary cultured astrocytes of rat.</p><p><b>METHODS</b>The cell survival rate was measured by Typan Blue assay; the intracellular [Ca(2+)]i concentration was determined by the fluorescent Ca(2+) indicator Fura-2/AM.</p><p><b>RESULTS</b>The survival rate of astrocytes was decreased to 91.9% after astrocytes were incubated with 1 x 10(-5) mol/L DM for 72 h (P < 0.05). The cell survival rates were 89.0%, 84.8%, 81.2% and 79.2% respectively when astrocytes were administered with 1 x 10(-4) mol/L DM for 4, 12, 24 and 72 h, which were remarkably lower than control groups (P < 0.01). Comparing with controls and before DM treatment, sharp increases in [Ca(2+)]i concentration [(451.4 +/- 42.3), (536.9 +/- 47.5) and (870.9 +/- 100.5) nmol/L respectively] were observed when astrocytes were incubated with 1 x 10(-7), 1 x 10(-6) and 1 x 10(-5) mol/L DM for 5 minutes (P < 0.01). After astrocytes were treated with 1 x 10(-8), 1 x 10(-7), 1 x 10(-6), 1 x 10(-5) mol/L DM for 15 minutes, the [Ca(2+)]i concentrations were decreased to (124.3 +/- 6.0), (131.3 +/- 19.1), (118.9 +/- 1.4), (136.6 +/- 3.8) nmol/L respectively, which were significantly different from those of controls and before treatment. And this situation was almost keeping stable to 30 min.</p><p><b>CONCLUSION</b>The cell survival rate was decreased and the [Ca(2+)]i concentration was temporarily increased when astrocytes were treated with DM.</p>

Association of HLA-DPB1 alleles with chronic myelogenous leukemia in southern Chinese Hans / 中国实验血液学杂志

To clarify the association between HLA-DPB1 alleles and chronic myelogenous leukemia (CML) in South Chinese, the allelic types of HLA-DPB1 were detected by sequence based typing (SBT) in 86 patients with CML and 82 healthy individuals from Southern China. The results showed that the frequencies of HLA-DPB1 * 1301 and DPB1 * 20011 were higher in patients with CML in comparison with those of healthy individuals. It is concluded that positive association may exist between certain HLA-DPB1 alleles and CML.

A pilot study of repair of periodontal bone defects with carbonated phosphate bone cement modified with synthesized peptides in dogs / 中华口腔医学杂志

<p><b>OBJECTIVE</b>To explore the possibility of repairing periodontal defects with carbonated calcium phosphate bone cement (CCPBC) modified with synthesized peptides.</p><p><b>METHODS</b>Periodontal bone defects in 4 dogs were surgically created and then restored directly with hydroxyapatite (HA), Perioglass, CCPBC and CCPBC modified with peptides. The results were compared at different levels.</p><p><b>RESULTS</b>Bone replacement materials were lost in HA and Perioglass groups. In the HA group defects were restored with connective tissue. Perioglass group had only a little new bone around materials by alveolar bone. CCPBC could firmly stay in bone defects to maintain the space of bone defects even without membrane use. CCPBC modified with peptides was superior to HA, Perioglass, and CCPBC, surrounded by a great deal of new bone.</p><p><b>CONCLUSION</b>Under limitation of this study, CCPBC modified with peptides has some osteoinuctive activity and may have good prospect for the clinical application in periodontal defect repair.</p>