莽吉柿提取物通过调控MAPK/ERK信号通路诱导宫颈癌细胞凋亡的作用研究

目的: 研究莽吉柿(Garcinia mangostanaSL.)提取物对宫颈癌Hela细胞凋亡的影响。方法:使用0μg/ml、0.75μg/ml、1.25μg/ml、2.5μg/ml、5μg/ml的莽吉柿提取物体外培养Hela细胞,CCK-8法检测其对宫颈癌细胞增殖的影响;使用不同浓度莽吉柿提取物体外培养Hela细胞,流式细胞术检测细胞凋亡和细胞活性氧(Cell reactive oxygen, ROS)表达水平;不同浓度莽吉柿提取物体体外培养Hela细胞,Western Blot检测凋亡相关蛋白BCL-2、BAX、p-ERK的表达。 结果: 莽吉柿提取物对宫颈癌细胞的增殖具有显著的抑制作用(P<0.05),IC50为1.63μg/ml。流式细胞术检测发现, 0、2.5μg/ml、5μg/ml的莽吉柿提取物处理后Hela细胞的凋亡率分别为(3.30 ± 0.10)%,(4.19 ± 0.24)%,(14.03±0.21)%,具有显著性差异(p＜0.05)。流式细胞术检测发现0、5μg/ml的莽吉柿提取物处理后,细胞活性氧(ROS)水平显著提高(P<0.05),mean值分别为(129796 ± 1336)和(481665 ± 9804)。荧光显微镜结果显示其ROS荧光水平显著提高。Western Blot检测发现宫颈癌Hela细胞中Bcl-2蛋白显著降低、BAX蛋白显著升高、p-ERK蛋白显著降低(P均<0.05)。结论: 莽吉柿提取物对宫颈癌细胞的影响可能是通过诱导细胞氧化损伤,调控肿瘤细胞MAPK/ERK信号通路,调控凋亡相关蛋白,进而诱导细胞发生凋亡,抑制肿瘤细胞的增殖。     

藤黄酸的抗肿瘤机制

目前发现藤黄酸可通过不同机制在多种肿瘤细胞中发挥抗肿瘤作用,包括诱导细胞凋亡,抑制端粒末端转移酶和拓扑异构酶活性,抑制热休克蛋白和通道蛋白表达,抑制肿瘤血管生成和转移,逆转肿瘤多药耐药,提示藤黄酸有望成为新型抗肿瘤药物,且仍需进一步探索其在抗肿瘤领域的价值.     

中国藤黄属植物中(口山)酮类化合物研究进展

酮类化合物是藤黄属植物中的主要特征成分,具有多样的生物活性,在中国藤黄属植物中广泛分布。由于氧化程度、取代基种类、数量和取代基位置的不同,(口山)酮类化合物具有多样的结构类型。文章综述了中国藤黄属植物中(口山)酮类化合物的研究概况,总结了该类化合物的分布、提取分离、结构分类、波谱学特征和生物合成途径。     

高速逆流色谱快速分离山竹子素的制备方法实验研究

目的：制备山竹子素（garcinol）化学对照品。方法：采用高速逆流色谱法,从多花山竹子、山木瓜、大叶藤黄三种藤黄属植物粗提物中快速分离化合物garcinol,溶剂系统为正己烷-乙酸乙酯-95%乙醇-水（8:8:12:4,体积比）,上相做固定相,下相做流动相,仪器转速850rpm,温度25℃,检测波长254nm,目标化合物馏分经Sephadex LH-20凝胶柱柱色谱纯化,所得样品由高效液相色谱法检测纯度。结果：可从104.765g多花山竹子枝、105.270g山木瓜枝、102.318g大叶藤黄果实中分离得到garcinol的量分别为45mg、281mg、4080mg,纯度分别为98.72%、98.36%、98.42%。结论：通过对比三种植物样品处理方法,结果以大叶藤黄果实作为原料时,正己烷-乙酸乙酯-95%乙醇-水（5:5:5:5,体积比）萃取的上相浸膏,经高速逆流色谱法结合凝胶柱柱色谱法,可快速高效、大量制备化合物garcinol。实验表明该方法效率高,可操作性强,制备量大。     

Effects of garcinia cambogia (Hydroxycitric Acid) on visceral fat accumulation: a double-blind, randomized, placebo-controlled trial

Background

(-)-Hydroxycitric acid (HCA) is an active ingredient extracted from the rind of the Indian fruit Garcinia cambogia. It inhibits adenosine triphosphate citrate lyase and has been used in the treatment of obesity.

Objective

The primary end point of this study was the effects of 12 weeks of G cambogia extract administration on visceral fat accumulation. The secondary end points were body indices (including height, body weight, body mass index [BMI], waist and hip circumference, and waist-hip ratio) and laboratory values (including total cholesterol, triacylglycerol, and free fatty acid).

Methods

This study was performed according to a double-blind, randomized, placebo-controlled, parallel-group design. Subjects aged 20 to 65 years with a visceral fat area >90 cm² were enrolled. Subjects were randomly assigned to receive treatment for 12 weeks with G cambogia (containing 1000 mg of HCA per day) or placebo. At the end of the treatment period, both groups were administered placebo for 4 weeks to assess any rebound effect. Each subject underwent a computed tomography scan at the umbilical level at −2, 0, 12, and 16 weeks.

Results

Forty-four subjects were randomized at baseline, and 39 completed the study (G cambogia group, n = 18; placebo group, n = 21). At 16 weeks, the G cambogia group had significantly reduced visceral, subcutaneous, and total fat areas compared with the placebo group (all indices P<0.001). No severe adverse effect was observed at any time in the test period. There were no significant differences in BMI or body weight at week 12, but there were slight numeric decreases in body weight and BMI in men. There were no signs of a rebound effect from week 12 to week 16.

Conclusion

G cambogia reduced abdominal fat accumulation in subjects, regardless of sex, who had the visceral fat accumulation type of obesity. No rebound effect was observed. It is therefore expected that G cambogia may be useful for the prevention and reduction of accumulation of visceral fat.     

藤黄茎皮中莽吉柿素对人胃癌HGC-27细胞的作用研究

目的 探讨藤黄树茎皮中氧杂环酮类成分莽吉柿素对人胃癌HGC-27细胞的生长抑制作用及潜在的作用机制。方法 采用噻唑蓝（MTT）染色实验检测莽吉柿素对HGC-27细胞的抑制作用。采用克隆形成实验评估莽吉柿素对HGC-27细胞增殖的影响。采用Hoechst染色实验研究莽吉柿素对HGC-27细胞形态变化的影响。采用蛋白免疫印迹法（Western blot）检测莽吉柿素给药后与凋亡过程、Neddylation修饰途径及丝裂原活化蛋白激酶（MAPK）信号通路相关的蛋白表达水平变化。采用裸鼠移植瘤模型进行莽吉柿素裸鼠体内抗肿瘤药效研究。结果 莽吉柿素给药后能够抑制HGC-27细胞的增殖能力和细胞集落形成。与对照组比较,莽吉柿素显著上调HGC-27细胞多聚ADP核糖聚合酶1（PARP1）和Bax蛋白表达（P<0.001）,下调抗凋亡蛋白B细胞淋巴瘤-2（Bcl-2）的表达（P<0.001）,发挥促进胃癌细胞凋亡的作用。莽吉柿素给药后HGC-27细胞中β淀粉样蛋白前体蛋白结合蛋白1（APPBP1）、泛素样修饰激活酶3（UBA3）和泛素结合酶E2M（UBC12）蛋白及MAPK信号通路蛋白c-Jun、c-Jun氨基端激酶（JNK）和p38的磷酸化水平均显著下调（P<0.001）。进一步的体内移植瘤动物实验结果显示,莽吉柿素给药后裸鼠肿瘤体积缩小18.7%,差异具有统计学意义（P<0.05）。与对照组比较,莽吉柿素组裸鼠体内与肿瘤细胞增殖相关的标志蛋白Ki67阳性细胞数明显减少,肿瘤组织中棕色细胞数量明显增加。结论 藤黄树茎皮中氧杂环酮类化学成分莽吉柿素在HGC-27细胞和裸鼠上均显示良好的抗胃癌活性,其作用机制可能与抑制Neddylation修饰途径以及抑制MAPK信号通路相关。     

云树果实醋酸乙酯提取物对H22荷瘤小鼠抑瘤作用及机制研究

目的 研究云树果实醋酸乙酯提取物（EGCF）对H22实体移植瘤的抑制活性及作用机制。方法 皮下接种H22瘤株建立小鼠H22实体移植瘤模型,随机分为模型组、环磷酰胺（20 mg/kg,阳性对照,ip给药）组和EGCF高、中、低剂量（400、200、100 mg/kg,ig给药）组,连续给药10 d,另设一对照组。检测小鼠体质量变化、抑瘤率及脾脏指数,ELISA法测定血清中白细胞介素-6（IL-6）、肿瘤坏死因子-α（TNF-α）、转化生长因子-β1（TGF-β1）的含量,HE染色法观察肿瘤组织病理学改变,免疫组化法检测肿瘤组织p-STAT3及血管内皮生长因子（VEGF）的表达。结果 与模型组比较,EGCF高、中、低剂量组小鼠的肿瘤质量均显著降低（P<0.01、0.001）,脾脏指数均无显著性差异;高、低剂量组小鼠血清中IL-6水平显著降低（P<0.05）,各剂量组TNF-α含量显著增加（P<0.05、0.01）;各剂量组瘤组织均出现较多红染、碎片状的干酪样坏死区域,且伴有大量空泡形成;各剂量组均显著减少肿瘤组织VEGF表达,高剂量组显著抑制STAT3磷酸化（P<0.05、0.01）。结论 EGCF能够抑制H22实体移植瘤生长,其机制可能与阻断STAT3相关信号通路有关。     

Hypolipemic Effect of Garcinia cambogia in Obese Women

Garcinia cambogia seems to promote weight reduction and improvement on lipid profile by its major compound, hydroxycitric acid (HCA), blocking ATP‐citratelyase, potentially inhibiting lipogenesis. Furthermore, it is suggested that its extract is able to change the adipokine levels. Thus, the aim of this study was to analyse the effect of G. cambogia on the lipid profile, endocrine, calorimetric and anthropometric parameters of obese women. The women (BMI > 25 kg/m²; age 25–60 years), divided in treated (n = 30) and control (n = 13) groups, received 2.4 g (800 mg 3×/day) of garcinia extract (50% of HCA) or placebo during 60 days, respectively, as well as dietary control. Weight, BMI, waist–hip ratio and percentage of fat mass, resting metabolic rate, respiratory coefficient, triglycerides (TG), total cholesterol, HDL and LDL, leptin and insulin serum levels were evaluated. TG was significantly reduced in the treated group (p = 0.0002) and the post‐treatment variation was different compared to the placebo group (p = 0.04). No significant response was observed on other variables of the lipid profile, or on the anthropometric and calorimetric parameters. Leptin and insulin levels did not change significantly after the treatment. The short‐term treatment with G. cambogia demonstrated a hypotriglyceridemic effect, which does not appear to be related to changes in leptinemia. Copyright © 2013 John Wiley & Sons, Ltd.     

山竹果壳中α-倒捻子素和水溶性多糖的含量测定

目的:测定山竹果壳中α-倒捻子素(α-mangostin)和水溶性多糖的含量。方法:采用闪式提取技术结合高效液相色谱法测定山竹果壳中α-倒捻子素的含量;蒽酮浓硫酸法测定水溶性多糖的含量,紫外吸收光度法测定水溶性多糖与纳米二氧化钛(TiO2)及芦丁的抗紫外线作用。结果:闪式提取技术最佳提取工艺条件下测得山竹果壳中α-倒捻子素的质量分数为6.72%;水溶性多糖的含量为6.19%。结论:闪式提取技术结合高效液相色谱法测定山竹果壳中α-倒捻子素方法简单、准确。水溶性多糖具有较好的抗紫外线辐射作用。     

A new furanoxanthone from Garcinia mangostana

Our phytochemical study on the stem bark of Garcinia mangostana has led to the discovery of a new furanoxanthone, mangaxanthone A (1), together with five known analogs. The five known analogs that were isolated are α-mangostin (2), β-mangostin (3), cowagarcinone B (4), and dulcisxanthone F (5). The structural elucidations of these compounds were carried out by interpreting their spectroscopic data, mainly 1D and 2D NMR spectra and MS.