中国云实属果实与种子形态特征及其分类鉴定学意义

目的:建立中国云实属果实与种子形态特征分类方法。方法:将野外采集的成熟果实置室内阴干,观察形态并描述后剥取种子观察描述。结果:中国云实属果实与种子形态特征种间区别明显,性状稳定,列出了分种检索表。结论:可以作为种级水平分类依据。     

苏木化学成分的研究

从苏木Caesalpinia sappanL.树干的甲醇提取物中分得2个结晶。经物理常数和光谱分析,分别鉴定为四乙酰基巴西灵(tetraacetylbrazilin)和protosappaninA.     

苦石莲总黄酮超声波提取工艺及含量研究

目的:优化苦石莲总黄酮超声波-乙醇提取工艺,研究苦石莲及其种皮、子叶总黄酮含量。方法:通过单因素实验,分别考察乙醇浓度、提取温度、提取时间、料液比等单因素对苦石莲黄酮类化合物得率的影响。采用L9(34)正交实验表进行实验,通过极差和方差分析确定最佳提取工艺。结果:确定苦石莲及其种皮的最佳提取工艺为乙醇浓度50%,提取温度80℃,提取时间60min,料液比1∶15。子叶的最佳提取工艺为乙醇浓度70%,提取温度70℃,提取时间30min,料液比1∶15。在最佳工艺下连续提取3次,苦石莲、种皮、子叶总黄酮提取率分别为2.75%、8.09%、0.246%。结论:苦石莲黄酮类化合物主要存在于种皮中。超声波辅助提取法是一种安全简便、节能又高效的苦石莲总黄酮提取途径。     

Two new cassane-type diterpenes from the seeds of Caesalpinia crista

Two new cassane-type diterpenes, phangininoxys D and E (1 and 2), together with five known compounds were isolated from the seeds of Caesalpinia crista Linn. The structures of these compounds were elucidated by means of various spectroscopic analyses. All the isolated compounds were evaluated for cytotoxicity activities against HeLa, HT-29 and KB cell lines, and compound 7 showed moderate selective activities against KB cell line with an IC₅₀ value of 17.1 μM.     

用肉荚云实代替进口塔拉工业化生产没食子酸的研究

目的 首次用国产肉荚云实作为工业化生产没食子酸的原料.方法 用与进口塔拉生产没食子酸的相同生产工艺的单耗与得率进行比较.结果 肉荚云实作为原料工业化生产没食子酸的单耗相当于或低于塔拉,其单宁酸含量、纯度及水解没食子酸的产率均优于进口塔拉.结论 国产肉荚云实可以代替进口塔拉作为工业化生产没食子酸的原料.     

苏木抗癌活性成分的研究

 目的 从苏木提取物中寻找抗癌活性物质。方法 采用不同溶剂从苏木中提取粗提物,液相色谱法测定各提取物中几种主要成分的含量;以人类膀胱癌T24细胞为靶细胞,采用锥虫蓝拒染法测定各提取物作用20、40、60、80、100 min时对靶细胞的杀伤率;选择与杀伤率呈正相关性的主要组分,进行反复色谱层析,分离得到纯度达到98 %以上的单体,采用核磁共振、质谱、红外等波谱学方法对该单体进行结构测定;以T24、人类卵巢癌SKOV3、小鼠肉瘤S180、小鼠肝癌H22细胞为靶细胞,以丝裂霉素、羟喜树碱为阳性对照药物,测定其对靶细胞抑制活性。结果 粗提物中R12与细胞杀伤率呈正相关性（r100 min＝0.941,P＜0.001）;R12的主要成分是巴西木素,其在1.2 mg／ml浓度下对T24、SKOV3、H22、S180细胞作用40 min时的杀伤率分别达到90.89 %、98.65 %、99.82 %和100.00 %,杀伤作用明显优于阳性对照药物。结论 巴西木素是苏木中主要抗癌活性物质之一。     

小叶云实的化学成分及抗菌活性研究

目的:深入研究小叶云实的化学成分及其抗菌活性。方法:利用多种色谱方法对小叶云实根的化学成分进行研究,并对分得的单体化合物进行抗菌筛选。结果:鉴定了6个高异黄酮的化学结构,分别为eucomin(1),intricatinol(2),8-methoxybonducellin(3),bonducellin(4),8-methoxyisobonducellin(5),3-(4-methoxybenzyl)-5,7-dimethoxychroman-4-one(6),并对从小叶云实中获得的单体化合物进行抗菌活性筛选。结论:化合物1～6均为首次从该植物根中分离得到。化合物8-me-thoxyisobonducellin,intricatinol,岩白菜素,金丝桃苷和11-没食子酰岩白菜素对金黄色葡萄球菌、肺炎克雷伯氏菌、乙型链球菌和绿脓杆菌均有不同程度的抑制作用。     

Hypoglycaemic activity and molecular mechanisms of Caesalpinia ferrea Martius bark extract on streptozotocin-induced diabetes in Wistar rats

Ethnopharmacological relevance

The tea from the stem bark of Caesalpinia ferrea Martius (Leguminosae) has been popularly used in the treatment of diabetes in Brazil.

Aim of the study

To investigate the hypoglycaemic properties and to elucidate the mechanisms by which the aqueous extract of the stem bark of Caesalpinia ferrea reduces blood glucose levels in streptozotocin-induced diabetic rats via the enzymatic pathways of protein kinase B (PKB/Akt), AMP-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC).

Materials and methods

The aqueous extract of the stem bark of Caesalpinia ferrea (300 and 450 mg/kg/day), vehicle and metformin (500 mg/kg/day) were administered orally to STZ-diabetic rats (n = 7/group) for 4 weeks. Changes in body weight, food and water intake, fasting glucose levels and oral glucose tolerance were evaluated. Phosphorylation (P) and the expression of Akt, AMPK and ACC in the liver and skeletal muscle were determined using Western blot.

Results

The aqueous extract of the stem bark of Caesalpinia ferrea reduced blood glucose levels and improved the metabolic state of the animals. P-Akt was increased in the liver and skeletal muscle of the treated animals, P-AMPK was reduced only in the skeletal muscle of these animals and P-ACC was reduced in both when compared with untreated rats.

Conclusion

The results indicate that the aqueous extract of the stem bark of Caesalpinia ferrea has hypoglycaemic properties and possibly acts to regulate glucose uptake in liver and muscles by way of Akt activation, restoring the intracellular energy balance confirmed by inhibition of AMPK activation.     

Analgesic Activity of Caesalpinia bonducella Flower Extract

Caesalpinia bonducella Fleming (Leguminosae) flower extract (CBFE) was administered orally (30, 100, and 300 mg/kg) and tested for analgesic and antipyretic activities in adult mice and rats. Analgesic activity was investigated in capsaicin-induced pain, formalin-induced pain, acetic acid-induced writhing test, hot plate test, and tail flick test. Antipyretic activity was tested in Brewer's yeast-induced pyrexia in rats. The extract was found to have significant antinociceptive effect in inflammatory phase of formalin-induced pain and acetic acid-induced parietal pain.     

Floating-bioadhesive gastroretentive Caesalpinia pulcherrima-based beads of amoxicillin trihydrate for Helicobacter pylori eradication

Abstract

Context: An oral dosage form containing floating bioadhesive gastroretentive microspheres forms a stomach-specific drug delivery system for the treatment of Helicobacter pylori.

Objectives: To prepare and evaluate controlled release floating bioadhesive gastroretentive chitosan-coated amoxicillin trihydrate-loaded Caesalpinia pulcherrima galactomannan (CPG)-alginate beads (CCA-CPG-A), for H. pylori eradication.

Materials and methods: CCA-CPG-A beads were prepared by ionotropic gelation, using 2³ factorial design with quantity of drug, combination of CPG with sodium alginate and concentration of calcium chloride as variables. Beads facilitated mucoadhesion to gastric mucosa with floating nature caused by chitosan coating for wide distribution throughout GIT. Developed beads were evaluated for characteristics like beads size-morphology, entrapment efficiency, DSC, XRD, FTIR, swelling ratio, in vitro mucoadhesion, in vitro drug release, in vitro floating and in vitro H. pylori growth inhibition studies. CCA-CPG-A beads were studied in Wistar rats for in vivo gastric mucoadhesion, in vivo H. pylori growth inhibition studies using PCR amplification of isolated DNA, rapid urease test.

Result: Developed beads possess drug release of 79–92%, entrapment efficiency of 65–89%, mucoadhesion of 61–89%. In vivo mucoadhesion study showed more than 85% mucoadhesion of beads even after 7th hour. In vitro–in vivo growth inhibition study showed complete eradication of H. pylori.

Discussion: CPG-alginate and chitosan in beads interacts with gastric mucosubstrate surface for prolonged gastric residence with floating bioadhesion mechanism for H. pylori eradication in rats.

Conclusion: Floating bioadhesive CCA-CPG-A beads offer a promising drug delivery system for H. pylori eradication at lower dose, reduced adverse effect and enhance bioavailability.