Identification of antibacterial principles against Streptococcus mutans and inhibitory principles against glucosyltransferase from the seed of Areca catechu L

During the course of our studies on dental caries prevention by traditional medicines, fatty acids (myristic and oleic acids etc.) and procyanidins from betel nuts (the seed of Areca catechu L.) were respectively revealed to be the major antibacterial principles against a primary cariogenic bacterium, Streptococcus mutans, and the major inhibitory principles against glucosyltransferase from S. mutans.     

海风藤及其代用品药理作用的比较研究

选择经典的实验指标，对海风藤及其３种代用品山Ｊｕ，石楠藤有毛Ｊｕ的药理作用进行了比较研究，结果表明海风藤，山Ｊｕ和毛Ｊｕ在抗炎，镇痛和抗血小板聚集方面均有效，其中海风藤作用最强，其次为山Ｊｕ，毛Ｊｕ石楠藤没有明显的抗炎作用，其抗血小板聚集及止痛作用稍强于毛Ｊｕ。     

海风藤化学成分及神经保护活性研究

目的 对海风藤Piperis kadsurae藤茎的化学成分进行研究,并对分离的化合物进行初步的神经保护活性筛选。方法 运用硅胶、ODS、和Sephadex LH-20等柱色谱以及反相制备型HPLC等各种现代色谱分离技术进行系统的分离纯化,利用波谱学方法确定化合物结构。同时采用MTT和RTCA法,以白藜芦醇作为阳性对照,对化合物进行体外神经保护活性实验。结果 从海风藤藤茎的二氯甲烷和醋酸乙酯提取物中分离得到22个化合物,分别鉴定为puberulin(1)、(-)-acuminatin(2)、dihydrocarinatin(3)、海风藤酮（4）、山蒟素C(5)、3-羟基苯甲酸苄酯（6）、2-羟基苯甲酸苄酯（7）、cherrevenol D(8)、trans-2,3-diacetoxy-1-[(benzoy1oxy)methyl]-cyclohexa-4,6-diene (9)、(3R,4R)-4-O-acetyl-5-(benzoyloxymethyl)cyclohexa-1,5-diene-3,4-diol(10)、(-)-sootepoxidechlorohydrinA(11)、香...     

山蒟醇提取物的抗血小板聚集作用?

以山蒟醇提取物在兔的体内和体外-体内进行抗血小板聚集实验。结果表明山蒟醇提取物可抑制由血小板活化因子和花生四烯酸所致的血小板聚集,对2者所致的血小板聚集（体外试验）的IC_（50）。分别为40． 34、345． 46 mg／L。静脉注射山蒟醇提取物30 mg／kg,15 min后产生的抗血小板聚集作用最明显,其对血小板活化因子和花生四烯酸所致的血小板聚集（体内-体外试验）的抑制率分别为82．75％和33．34％;血小板聚集的持续时间分别为60、30 min。这表明山蒟醇提取物对血小板活化因子作用有一定的选择性。     

New optimized piperamide analogues with potent in vivo hypotensive properties

We describe herein the structural optimization of new piperamide analogues, designed from two natural prototypes, piperine 1 and piperdardine 2, obtained from Piper tuberculatum Jacq. (Piperaceae). Molecular modeling studies using semiempirical AM1 method were made in order to establish rational modifications to optimize them by molecular simplification. The targeted compounds (10) and (11) were respectively obtained using benzaldehyde (12) and para-anisaldehyde (13) as starting materials. ¹H NMR spectra showed that the target compounds were diastereoselectively obtained as the (E)-isomer, the same geometry of the natural prototypes. These new synthetic amides presented significant hypotensive effects in cardiovascular essays using in vivo methodologies. Compound 11 (N-[5-(4′-methoxyphenyl)-2(E)-pentenoyl]thiomorpholine) showed a potency 10,000 times greater than its prototype 5, evidencing an optimization of the molecular architecture for this class of hypotensive drug candidates.     

海南人咀嚼槟榔引起的口腔鳞状细胞癌ceRNA网络分析

目的:构建咀嚼槟榔引起的口腔鳞状细胞癌（OSCC）的ceRNA网络,探究其表达异常可能影响的调节通路改变。方法:对咀嚼槟榔的OSCC及癌旁组织进行miRNA测序和lncRNA微阵列分析,并建立了ceRNA网络。结果:lncRNA-miRNA-mRNA网络由308个lncRNA,41个miRNA和115个mRNA组成。结论:GO和KEGG分析表明,ceRNA网络参与了MAPK、凋亡、p53和PI3K/Akt等不同的信号通路。     

海风藤的原植物——腺鳞蒟与山药的比较研究

本文对模式产地的山药Piper haneei Maxim, var, hancei Maxim,和腺鳞蒟P. kancei Maxim var. squamiglanduferum Fan var. nov.进行了原植物形态特征和花序轴、花序梗、茎、叶的显微特征以及化学成分的TLC及UV比较。挥发油的GC—MS研究共鉴定出38个成分,其中28个是胡椒属植物中首次报道的成分。结果证明了在福建长期以来被认为是山药的腺鳞蒟与模式产地的山药有较大差别,尤其是腺鳞蒟叶上表面有腺鳞,是迄今为止第1个发现具有腺鳞的胡椒属植物。据此把腺鳞蒟作为新变种从山药中分出。腺鳞药是福建南部海风藤主要来源之一。     

Effect of Plant Extracts Formulated in Different Ointment Bases on MDR Strains

Extracts of Aloe vera whole plant, Eucalyptus globulus leaves, Ficus infectoria bark, Ficus religiosa bark and Piper betel leaves were studied for antibacterial activity on resistant and sensitive strains, isolated from skin and soft tissue infections. A combination of hot alcoholic extracts of Ficus infectoria, Ficus religiosa and Piper betel were found to be more effective against all the isolates. The combined extract was formulated in different ointment bases such as polyethylene glycol, gelatin, sodium alginate, carbopol, cream base and honey. These were then evaluated to find a suitable base for preparation of an ointment. In vitro study of the release of antimicrobials and kill-time studies of the herbal ointments was carried out against multi-drug resistant isolate of Pseudomonas. The ointment showed bactericidal activity within 2 h against the resistant strain of Pseudomonas spp.     

苎叶蒟中1个新的含氮木脂素

目的对苎叶蒟Piper boehmeriifolium的枝叶部位进行化学成分研究。方法采用硅胶、RP-C_(18)柱色谱、Sephadex LH-20凝胶柱色谱和半制备HPLC等方法进行分离和纯化,并综合运用IR、HR-ESI-MS、~1H-NMR、~(13)C-NMR、DEPT、HSQC、HMBC等方法鉴定化合物的结构。结果从苎叶蒟乙醇提取物中分离得到15个化合物,分别鉴定为3-(3,4-methylenedioxybenzyl)-4-(3,4-dimethoxybenzyl)-1H-pyrrole-2,5-dione(1)、2E,4E-decadienoylpiperidide(2)、2E-decenoylpiperidide(3)、墙草碱(4)、piperchabamide B(5)、假蒟亭碱(6)、piperdardine(7)、胡椒新碱(8)、胡椒碱(9)、二氢荜茇明宁碱(10)、chingchengenamide A(11)、假荜茇酰胺B(12)、guineensine(13)、荜茇宁(14)和kusunokinin(15)。结论化合物1为新化合物,命名为胡椒木脂酰亚胺,化合物2、3、7、8、10和15为首次从该植物中分离得到。     

十八症提取物的药理作用研究

目的 :研究十八症提取物的镇静、镇痛、抗抑郁及抗炎活性。方法 :以十八症的醋酸乙酯提取物和乙醇提取物按 50 ,100mg·kg^-1对小鼠分别灌胃给药 ,测定小鼠穿格行走数、扭体数、强迫游泳累计不动时间及耳廓肿胀率来考察十八症提取物的镇静、镇痛、抗抑郁、抗炎活性。结果 :醋酸乙酯提取物可使小鼠穿格行走数、扭体数、累计不动时间及耳廓肿胀率均明显减小 ,而乙醇提取物仅引起小鼠穿格行走数和累计不动时间显著减小。结论 :十八症的醋酸乙酯提取物有较显著的镇静、镇痛、抗抑郁及抗炎作用 ,而乙醇提取物仅在镇静、抗抑郁作用方面具一定活性。