云实种子中1个新颖卡山烷二萜类化合物

目的研究云实Caesalpinia decapetala种子的化学成分。方法采用硅胶、Sephadex LH-20、ODS等柱色谱技术进行分离纯化,采用各种波谱技术进行结构鉴定。结果从云实种子95%甲醇提取物中分离得到了1个新卡山烷二萜类化合物,鉴定为1α,2α-diacetoxy-14β-carboxymethyl-7β-hydro xyl-vouacapen-5α-ol(1)。结论化合物1为新的卡山烷二萜类化合物,命名为云实子C。     

原苏木素A对胃癌SGC-7901细胞系放疗增敏作用的研究

目的 本研究将原苏木素A、苏木醇提物、顺铂分别与放疗联合作用于胃癌细胞SGC-7901细胞系,研究原苏木素A是否增加胃癌SGC-7901细胞系放射敏感性,为临床用药开创更新的领域。方法 体外培养人胃癌细胞SGC-7901细胞系,以苏木醇提物、顺铂为对照,MTT法检测原苏木素A对细胞增殖作用的影响,以及其与作用浓度和作用时间的关系;采用克隆形成实验,拟合细胞存活曲线,以单纯放疗组为对比,计算放射增比(SER),分析原苏木素A的增敏效果。结果 原苏木素A对人胃癌细胞SGC-7901有生长抑制作用,但抑制作用相对较弱,其细胞毒性有明显的时间和浓度依赖性。不同作用时间及作用浓度下的细胞形态发生明显的改变。克隆形成实验显示原苏木素A显著增加了SGC-7901细胞的放射敏感性,与单纯放射组对比,差异有统计学意义。结论 原苏木素A对胃癌SGC-7901细胞的抑制有浓度和时间的依赖性,联合放射治疗能够提高放射增敏作用,两者可能具有协同抗肿瘤作用。     

苏木乙醇提取物对坐骨神经损伤小鼠血清髓鞘碱性蛋白含量及神经功能的影响

目的研究苏木乙醇提取物(SME)对坐骨神经损伤小鼠神经再生的影响。方法选取成年雄性Balb/c小鼠84只,随机分为SME高中低剂量组和空白对照组,行右侧坐骨神经离断吻合术,分别于术后3、5天1、2、4、8、12周以ELISA法血清髓鞘碱性蛋白浓度,术后4、8、12周行神经电生理检测,将所得结果进行统计学分析。结果各时间点动物的血清髓鞘碱性蛋白浓度及电生理检测结果与SME剂量呈现明确的量效对应关系。结论SME可以通过抑制损伤后的免疫反应,降低神经损伤局部神经的破坏程度,从而加速神经再生。     

Cytotoxic Effects of Phytophenolics from Caesalpinia mimosoides Lamk on Cervical Carcinoma Cell Lines through an Apoptotic Pathway

Background: Extracts of Caesalpinia mimosoides Lamk has been reported to possess anticancer effects, butthe active ingredients and the anti-cancer mechanisms are still unknown. Materials and Methods: The effectsof a C mimosoides Lamk extract on cell proliferation and apoptosis induction in human cervical carcinoma celllines, namely HeLa, SiHa, and C33A, as well as in normal Vero cells, were investigated. Results: Treatment with5 active fractions (F17-F21) of C mimosoides Lamk methanol extracts inhibited cell viability in a dose- and timedependentmanner. Neutral red assays indicated that treatment with F21 significantly decreased the viability ofall cervical cancer cell lines compared to F21-treated normal cells. In addition, HPLC analysis revealed that F21contained multiple phenolic compounds, namely gallic acid, caffeine, vanillic acid, ferulic acid and resveratrol.F21 had the lowest IC50 and, therefore, a much higher cytotoxicity than F20, F17, F19, and F18 by 20-, 25-,46- and 47- fold, respectively. Analysis of activation of the apoptosis pathway using a caspase 3/7 activity assayrevealed that F21 treatment resulted in a considerable increase in caspase activation in all cancer cell lines tested.At the same concentration of F21, HeLa cells had the highest caspase activity (6.5-fold) compared to the control.Conclusion: C mimosoides Lamk may be of value as an alternative therapeutic agent, especially in combinationwith other compounds offering possible of synergy of action. Moreover, HPV- and non-HPV-related cervicalcancer cells may differ in their responses to treatment regimens.     

The Cytotoxic and Anti-Migratory Properties of Caesalpinia sappan and Ficus septica,in Combination with Doxorubicin on 4T1 TNBC Cells with Nephroprotective Potential

Objective: To evaluate the anti-cancer properties of Caesalpinia sappan and Ficus septica in combination with doxorubicin on 4T1 cells, confirm their nephroprotective activities, and predict the molecular targets of the underlying mechanisms. Methods: The cytotoxic activities of all extracts and doxorubicin were determined by MTT assay followed by cell cycle and apoptosis analysis using flow cytometry. Immunoblotting was used to determine the protein expressions. The proteins involved in the cell proliferation and migration were analyzed through bioinformatics approaches, whereas, the interaction between compounds and protein targets was observed through molecular docking. Furthermore, the effect of the extracts on cell migration was analyzed by scratch wound healing assay. The intracellular ROS after treatment with extracts was observed using DCFDA staining flow cytometry. Results: Both ECS and EFS performed cytotoxic properties and significantly enhanced doxorubicin’s cytotoxic effects against 4T1 cells. However, these cytotoxic activities did not correlate with the cell cycle progression. On the contrary, the combination treatment caused apoptosis that may correlate with the decreasing of IκBα phosphorylation, indicating that all agents targeted the inhibition of NF-κB activation. The combination treatments also inhibited cell migration and decreased MMP-9 expression. TNBC proliferation and metastasis needed at least 54 proteins to be activated, some of them are related to NF-κB activation. The inhibitory effect of ECS correlated with the interaction of brazilin and brazilein to IKK, a kinase protein that plays a role in IκBα phosphorylation. In addition, ECS and EFS reduced ROS expression in Vero cells caused by doxorubicin. Conclusion: In conclusion, ECS and EFS effectively enhanced the cytotoxic effect of doxorubicin and inhibit cell migration on 4T1 cells and these activities may correlate to the inhibitory effect of NF-κB activation. ECS and EFS also exhibit ROS suppressing effect on Vero cells that may be beneficent to reduce nephrotoxicity of chemotherapeutic treatment.     

苦石莲的化学成分分离鉴定(Ⅱ)

目的:研究和分离鉴定苦石莲的化学成分。方法:以苦石莲对牙周炎的关键因子白细胞介素-6(IL-6)和白细胞介素8(IL-8)的调控作用为依据,采取回流提取法和梯度萃取法进行提取分离,用反复硅胶柱色谱、薄层色谱、重结晶等方法分离纯化苦石莲的化学成分,通过质谱、核磁共振及理化常数对照等方法对化合物的结构进行鉴定。结果:分离鉴定了8个化合物,分别为豆甾醇(stigmasterol,1),caesalmin C(2),bonducellpin F(3),β-谷甾醇(β-sitsterol,4),β-香树脂醇(β-amyrin,5),正二十六烷(n-hexacosane,6),正三十烷(n-triacontane,7),西米杜鹃醇(simiarenol,8)。结论:化合物3,6,7,8为首次从苦石莲中分离得到,其中bonducellpin F为一个新的卡山烷型呋喃二萜类化合物,n-hexacosane和n-triacontane为脂肪烷烃类化合物,西米杜鹃醇为三萜类化合物。     

Two new diterpenes from the seeds of Caesalpinia minax Hance

Molecules with diterpene skeletons often possess valuable medicinal properties. Two new diterpenes 1α,6α,7β-triacetoxy-5α-hydroxy-14β-ethyl-O-vouacapane (1) and 2α-acetoxy-14,15-cyclopimara-7β,16-diol (2) were isolated from the seeds of Caesalpinia minax Hance. Their structures were established on the basis of extensive spectroscopic analyses, including HR-ESI-MS, UV, IR, 1D, and 2D NMR (HSQC, HMBC, NOESY) methods. The stereochemical structure of 1 was confirmed via the circular dichroism spectrum and calculated ECD experiment. The inhibitory activity of nitric oxide production of RAW264.7 macrophages stimulated by lipopolysaccharide of compounds 1 and 2 was evaluated, and compound 1 was found to show significant inhibitory effect.     

Chemical constituents from the the twigs and leaves of Caesalpinia enneaphylla

Fifteen compounds were isolated from the twigs and leaves of Caesalpiniaenneaphylla. Their structures were identified to be: (E)-3-(4-hydroxybenzylidene)- 5,7-dihydroxychroman-4-one (1), 8-methoxybonducellin (2), (E)-3-(3,4- dihydroxybenzylidene)-5,7-hydroxychroman-4-one (3), 2′,4′-dihydroxychalcone (4), oxyfadichalcone B (5), 7-hydroxyflavonone (6), pinocembrin (7), kaempferol (8), quercitrin (9), kaempferol 3-O-α-L-rhamnopyranoside (10), quercetin 3-O-α-D-arabinoside (11), trans-2,3-diacetoxy-1-[(benzoyloxy)methyl]-cyclohexa-4,6-diene (12), 3-hydroxybenzyl benzoate (13), 2-acetoxybenzyl benzoate (14), and glutinol (15). All the compounds were isolated from C. enneaphylla for the first time.     

50种中药甲醇提取物对嗜水气单胞菌的体外抑菌及抗生物膜活性的评价

目的 评价50种中药甲醇提取物对嗜水气单胞菌的体外抑菌效果以及抗生物膜生成活性。方法 采取甲醇浸提的方法制备中药甲醇提取物,计算提取率;利用多功能酶标仪检测600nm处的吸光度（A₆₀₀）值测定各提取物（0.1、0.2、0.4、0.8、1.6、3.2mg·mL^-1）作用16h对嗜水气单胞菌的抑菌率;结晶紫染色法结合多功能酶标仪测定各提取物的抗生物膜活性。结果 苏木、白芍、侧柏叶等32种中药甲醇提取物对嗜水气单胞菌抑菌效果明显,其中苏木甲醇提取物的抑菌效果最显著,最大抑菌率达95.56%,起效质量浓度为0.1mg·mL^-1;石菖蒲、大青叶、广藿香等20种中药甲醇提取物明显抑制嗜水气单胞菌生物被膜的生成,其中白芍的最大抑制率达96.78%。结论 夏枯草、野菊花、大青叶、赤芍、石菖蒲、地肤子、连翘、苏木、肉桂、女贞子、白芍、甘草、肉豆蔻、鸡血藤、乌药、莪术、侧柏叶17种中药对嗜水气单胞菌同时具有抑菌和抑制生物膜生长活性。     

正交试验优选苦石莲胶囊乙醇提取工艺

目的：优选苦石莲胶囊提取工艺。方法采用L9(34)正交试验法,以化合物Neocaesalpin L提取率为指标,考察提取方法、乙醇体积分数、提取时间、提取次数、乙醇用量对Neocaesalpin L提取率的影响。结果最佳提取工艺为用25倍量的95%乙醇,提取2次,每次提取时间1.5 h。结论优选的工艺稳定,可为工业化生产提供依据。