New triterpenoid sapoin from Ardisia gigantifolia Stapf.

One new triterpenoid sapoin with two known triterpenoid sapoins:3β-O-{α-L-rhamnopyranosyl-(1→3)-[β-D-xylopyranose-(1→2)]-β-D-glucopyranosyl-(1→4)-α-L-arabinopyranosyl}-3β-hydroxy-13β,28-epoxy-oleanan-16-oxo-30-al(1),3β-O-{α-L-rhamnopyranosyl-(1→3)-[(β-D-xylopyranosyl-(1→2)]-β-D-galactopyranosyl-(1→4)-[(β-D-glucopyranosyl-(1→2)]-α-L-ara-binopyranoside}-16α-hydroxy-13,28-epoxy-oleanane(2) and cyclamiretin A 3β-O-α-L-rhamnopyranosyl-(l→3)-[P-D-xylopyranosyl-(1→2)]-β-D-glucopyranosyl-(1→4)-[β-D-glucopyranosyl-(...

Screening of Anti-inflammatory and Analgesic Parts of Ardisia gigantifolia stapf.and Its Toxicological Safety Study

[Objectives] To screen out the anti-inflammatory and analgesic parts of Ardisia gigantifolia stapf.and to explore the toxicological safety of each part.[Methods]The carrageenan-induced toe swelling experiment of mice,acetic acid-induced peritoneal capillary permeability experiment,pain writhing test,and mouse maximum tolerated dose experiment were carried out.Taking mouse toe swelling,capillary permeability,pain writhing reaction times,and animal death number as indicators,anti-inflammatory and analgesic effects were screened and toxicological safety was evaluated for petroleum ether,ethyl acetate,n-butanol and water parts of A.gigantifolia.[Results] The petroleum ether part of A.gigantifolia can significantly reduce the degree of carrageenan-induced toe swelling of(P < 0.05),significantly inhibit the glacial acetic acid induced capillary permeability of mice(P < 0.05) and the times of pain writhing of mice(P < 0.01),no death was observed in each group after 150-fold of clinical equivalent dose administration,and no abnormality was observed in body weight and tissues of mice.[Conclusions]The petroleum ether part of A.gigantifolia is active part of anti-inflammatory and analgesic effect,and each part is low in toxicological safety.

Antioxidant and Hypoglycemic Ability of Ardisia gigantifolia Stapf Parts

[Objectives]To study the antioxidant and hypoglycemic effects of different parts of Ardisia gigantifolia Stapf.[Methods]The hydroxyl radical scavenging activity,DPPH radical scavenging activity and total antioxidant capacity of ABTS of 75%ethanol extract of A.gigantifolia Stapf and the petroleum ether,ethyl acetate,n-butanol,chloroform and aqueous extract were measured with Vc as positive control.At the same time,acarbose was used as reference substance to determine the inhibitory effect of each polar site onα-glucosidase.[Results]All parts of A.gigantifolia Stapf had antioxidant activity,among which ethyl acetate had the strongest antioxidant activity,and the scavenging rate of hydroxyl radical and DPPH radical was higher than that of positive control.The results showed that petroleum ether,ethyl acetate and chloroform had a good inhibitory effect onα-glucosidase(better than acarbose).[Conclusions]The ethyl acetate part of A.gigantifolia Stapf had the best antioxidant activity and inhibitory effect onα-glucosidase.It provides a basis for further research and development of A.gigantifolia Stapf.

Ardisia gigantifolia ethanolic extract inhibits cell proliferation and targets cancer stem cells in gastric cancer

Objective:To evaluate the effects of ethanol extract from Ardisia gigantifolia leaves on cell proliferation and cancer stem cell(CSC)number in gastric cancer.Methods:The inhibitory effect of Ardisia gigantifolia extract on the proliferation of MKN45 and MKN74 gastric cancer cells was assessed using 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide assay.Non-adherent culture(3D)model was used to evaluate the effect of the extract on tumorsphere size and number.Moreover,the expression of CD44,ALDH,and p21 was determined by immunofluorescence analysis.Flow cytometric analysis was performed to evaluate cell cycle arrest and the expression of gastric CSC markers CD44 and ALDH.Real-time PCR analysis was also carried out to assess the effect of the extract on the expression of cell cycle-regulated genes.Results:Ardisia gigantifolia extract effectively inhibited cell proliferation with an IC_(50)of 55.7μg/m L in MKN45 cells and 123.6μg/m L in MKN74 cells.The extract also arrested cell cycle in the G_(0)/G_(1)phase as well as significantly reduced the size and number of tumorspheres.The markedly increased expression of p21 was observed at both m RNA and protein levels in the extract-treated adherent cells and tumorspheres.In addition,Ardisia gigantifolia extract significantly reduced the number of CD44-and/or ALDH-expressing gastric CSC.Conclusions:The development of gastric CSC can be inhibited by the ethanol extract of Ardisia gigantifolia.

Research Progress on Pharmacological Effects of Ardisia gigantifolia Stapf,a Traditional Chinese Medicine with Lingnan Characteristics

This paper comprehensively reviews the research progress on the pharmacological effects of Ardisia gigantifolia Stapf in recent years,and finds that Ardisia gigantifolia Stapf has good pharmacological effects in many aspects,including anti-inflammation,anti-oxidation,anti-thrombosis,anti-tumor and so on.In particular,more than ten saponins have been found to have good anti-tumor activity and have potential research value,which can provide reference for the full development and utilization of Ardisia gigantifolia Stapf resources.

A Pharmacognostical Study on Ardisia gigantifolia and Its Adulterants

[Objectives]The research aimed to study the characteristics of Ardisia gigantifolia and its adulterants Embelia scandens and Mappianthus iodoides for identification. [Methods] Through the trait identification method,powder microscopic identification method,TLC,inclusions detection and content determination,A. gigantifolia and its adulterants were contrasted. [Results]The morphological and histological characteristics of A. gigantifolia,E. scandens and M. iodoides were different from each other. Containing water,total ash,acid insoluble ash and other inclusions also had difference; the total triterpenoid saponins were respectively 122. 90 mg/g of A. gigantifolia,147. 052 mg/g of E. scandens,and 63. 06 mg/g of M. iodoides. [Conclusions] These methods are accurate and reliable,which could be used for the identification of A. gigantifolia and its adulterants.

Two new phenolic compounds from Ardisia gigantifolia

Two new compounds were isolated from the 60% ethanol extract of the dried rhizome of Ardisia gigantifolia Stapf. The structures were elucidated on the basis of spectroscopic methods as （＋）-5-（1,2-dihydroxypentyl）-benzene- 1,3-diol and （-）-5-（1,2- dihydroxypentyl）benzene- 1,3-diol.

走马胎种子萌发影响因素研究

为探究药用植物走马胎种子萌发的影响因素,探讨了不同浸种时间(0、1、2、3、4、5 d)、不同土壤含水量(70%、50%、30%)、不同播种深度(0、1、3、5 cm)、不同光照条件(全黑、自然光)、不同基质(沙土、肥土、黄土、山苍子壳、黄土∶肥土=1∶1、黄土∶山苍子壳=1∶1)、不同植物生长调节剂(赤霉素、6-BA、萘乙酸)对走马胎种子发芽的影响。结果表明,走马胎种子浸泡3 d时种子发芽率最高(64%);土壤含水量为50%时种子发芽率最高,为60%;播种深度为1 cm时种子发芽率显著高于其他播种深度;全黑条件下种子发芽率(58%)显著高于自然光(54%);6种基质中发芽率最高的是肥土;3种植物生长调节剂处理中走马胎种子发芽率较高的处理方式为50 mg/L赤霉素浸泡6 h、10 mg/L和100 mg/L 6-BA溶液浸泡6 h、400 mg/L萘乙酸浸泡12 h。综合考量,将浸泡3 d或用400 mg/L萘乙酸浸泡12 h的走马胎种子播于含水量为50%的肥土基质中1 cm深,保持黑暗条件,可有效提高走马胎种子发芽率。

走马胎提取物对胰腺癌的影响及作用机制

目的探究走马胎提取物对胰腺癌细胞PANC-1增殖、迁移、侵袭和凋亡的影响及作用机制。方法采用MTT法检测走马胎提取物对PANC-1细胞增殖的影响,观察其对PANC-1细胞形态的影响;设计划痕及Transwell迁移/侵袭实验检测其对PANC-1细胞迁移和侵袭能力的影响;采用Western blot法检测其对癌细胞中相关蛋白p65、P-p65、Caspase-3、Caspase-9、Cleaved-Caspase-3、Cleaved-Caspase-9、Bcl-2及Bax表达水平的影响。结果走马胎提取物对PANC-1细胞的增殖、迁移和侵袭具有抑制作用,能下调P-p65、Caspase-3、Caspase-9及Bcl-2的蛋白表达水平,上调Cleaved-Caspase-3、Cleaved-Caspase-9、Bax的蛋白表达水平。结论走马胎提取物能抑制PANC-1细胞活性,其机制是通过抑制PANC-1细胞的增殖、迁移与侵袭,上调Bax,下调Bcl-2,抑制p65的磷酸化,促进Caspase-3、Caspase-9的激活以诱导PANC-1细胞凋亡,而发挥抗胰腺癌作用。

药用植物走马胎的种苗繁殖及栽培技术研究进展

走马胎(Ardisia gigantifolia)为紫金牛科(Myrsinaceae)紫金牛属(Ardisia)常绿植物,是多种中成药和药酒的主要原料,具有非常高的经济价值。走马胎野生资源临近枯竭,已不能满足市场需求,因此人工栽培技术发展迅速,有关其研究也从化学成分、药理作用和资源调查领域延伸至繁殖和栽培领域。目前,针对走马胎的繁殖研究主要集中在组培苗上,对种子和扦插育苗的研究相对缺乏;而栽培研究则多集中于走马胎的生长环境、立地条件和水分管理等方面,对其采后加工和病虫管理的研究不足。本文对现有的走马胎种苗繁殖和栽培技术进行归纳总结,并结合笔者自身的经验对目前研究中存在的问题进行分析与讨论,同时进一步对走马胎药材未来的研究方向进行展望。

濒危植物粗茎紫金牛茎段愈伤组织再生体系的建立

粗茎紫金牛(Ardisia gigantifolia Stapf)原产于云南河口县,野生个体数量稀少,被列为极危物种,其叶、花、果均具较好的观赏性,具有重要的保护价值和较好的园林开发应用前景。本研究以粗茎紫金牛茎段为外植体建立其高效愈伤组织再生体系。结果表明:最佳愈伤组织诱导培养基为WPM+0.50 mg/L TDZ+0.10 mg/L NAA,诱导率为96.67%;愈伤组织在培养基WPM+0.50 mg/L TDZ中增殖系数达4.42,在培养基WPM+2.00 mg/L 6-BA+0.20 mg/L NAA中不定芽诱导率为100%;不定芽在培养基WPM+4.00 mg/L 6-BA中增殖系数达3.90,于培养基WPM+10%CW+0.20 mg/L NAA中生根率为100%,且不定根发达,植株生长健壮;组培苗移栽至珍珠岩∶泥炭土=1∶3的混合基质中,60 d后成活率达96.67%。该研究可为种苗的规模化生产提供技术支撑,也为该物种的保护、种苗繁育和分子生物学研究提供理论基础和技术支持。

瑶药血风黄酮超声辅助提取工艺优化及其抗氧化、抑菌活性的初步研究

试验旨在探究超声辅助提取瑶药血风黄酮的工艺条件及其抗氧化、抑菌活性。利用Box-Behnken响应面法设计四因素三水平的响应面试验。在单因素试验的基础上,以黄酮含量为响应值,并以乙醇体积分数、提取时间、液料比和超声功率作为影响因素,进行29组试验并进行验证性试验,初步分析血风黄酮的体外抗氧化、抑菌活性。结果表明,血风黄酮处理温度60℃的超声辅助提取优化工艺条件为乙醇体积分数56%、提取时间15min、液料比64 mL/g、超声功率200 W,在此工艺条件下,提取得到血风黄酮含量为(52.52±0.25)mg/g。血风黄酮具有一定的抗氧化能力,对大肠杆菌、金黄色葡萄球菌的最低抑菌浓度分别为1.25、2.50 g/L。研究表明,瑶药血风黄酮具有抗氧化和抗菌双重活性,具有成为饲料添加剂的开发潜力。

走马胎中皂苷成分AG4对MCF-7肿瘤细胞增殖的影响及机制研究

目的研究走马胎皂苷成分AG4对不同肿瘤细胞株增殖的影响,检测其对MCF-7细胞凋亡、细胞周期、Caspase-3和Caspase-9的活性、以及SOD活性和GSH、MDA含量的影响。方法终浓度为0.51～8.13μmol.L-1的AG4作用于肿瘤细胞株24～72 h后,采用MTT比色法检测AG4对9种肿瘤细胞株增殖的影响;筛选出对AG4敏感的细胞株,Hoechst染色观察细胞形态学变化;采用流式细胞术检测细胞凋亡和周期变化;采用相应试剂盒分别进行SOD活性和GSH、MDA含量的测定;采用Caspase-3和Caspase-9活性检测试剂盒对Caspase-3和Caspase-9活性进行检测。结果AG4作用于A549、BeL-7402、BGC-823、C6、EJ、HeLa、HepG2、MCF-7、LS180细胞24 h、48 h和72 h的IC50为3.67～11.1μmol.L-1,其中MCF-7细胞株对AG4较为敏感,24 h、48 h和72 h的IC50值分别为(3.67±0.61)、(3.76±0.66)和(4.03±0.47)μmol.L-1。高、中两剂量的AG4作用MCF-7细胞24 h后,细胞凋亡形态明显,发生早期凋亡;细胞阻滞在S期;SOD活性和GSH含量降低,MDA含量明显升高;Caspase-3和Caspase-9的活性均明显高于正常对照组。结论AG4对MCF-7细胞的增殖抑制作用最为明显。AG4干预MCF-7细胞内的氧化还原系统、阻滞周期并通过激活线粒体凋亡信号转导通路来诱导细胞凋亡。

走马胎中的三萜皂苷类成分及其体外抗肿瘤活性研究

目的研究走马胎根茎的三萜皂苷类成分及其体外抗肿瘤活性。方法采用溶剂萃取和柱色谱方法分离纯化,根据理化性质和波谱学数据鉴定化合物结构。采用MTT法测试三萜皂苷化合物的抗肿瘤活性。结果分离得到了7个三萜皂苷类化合物,包括3β-O-{β-D-吡喃木糖基-(1→2)β--D吡-喃葡萄糖基-(1→4)α--L吡-喃阿拉伯糖基}西-克拉敏A(1);3β-O-{α-L吡-喃鼠李糖基-(1→3)-[β-D-吡喃木糖基-(1→2)]β--D吡-喃葡萄糖基-(1→4-[β-D吡-喃葡萄糖-(1→2)]α--L-吡喃阿拉伯糖基}-西克拉敏A(2);lysikoianoside(3);3β-O-β-L吡-喃鼠李糖基-(1→3)-[β-D-吡喃葡萄糖基-(1→3)-β-D-吡喃木糖基-(1→2)]β--D-吡喃葡萄糖基-(1→4)-[β-D-吡喃葡萄糖基-(1→2)]α--L吡-喃阿拉伯糖基-西克拉敏A(4),3β-O-{β-L吡-喃鼠李糖基-(1→3)-[β-D吡-喃木糖基-(1→2)]β--D吡-喃葡萄糖基-(1→4)-[β-D-6-O乙-酰氧基-吡喃葡萄糖基(1→2)]α--L-吡喃阿拉伯糖基}-西克拉敏A(5),Ard isiacrisp in A(6)和3β-o-{α-L-rhamnopyranosyl-(1→3)-[β-D-xylopyranose-(1→2)]β--D-glucopyranosyl-(1→4)α--L-arab inopyranosyl}-3β-hydroxy-13β,28-epoxy-oleanan-16-oxo-30-al(7)。结论化合物1和3为首次从该植物中分离得到,化合物7首次从该属植物中分离得到。其中化合物2对BCG-823,EJ和Hepg2细胞有较好的抑制活性(IC50分别为0.29,9.99和2.03μg/m l)。化合物3对EJ细胞有选择性抑制作用(IC50为7.20μg/m l),化合物7对Hepg2细胞有选择性抑制活性(IC50为8.53μg/m l)。

走马胎中化合物AG4对人鼻咽癌细胞裸鼠移植瘤的影响

目的:研究走马胎中化合物AG4对人鼻咽癌细胞裸鼠移植瘤生长的影响。方法:建立人鼻咽癌细胞裸鼠皮下移植瘤模型,以抑瘤率为指标研究化合物AG4的体内抑瘤作用及AG4干预对裸鼠的一般情况(体质量、活动、食欲等)的影响;同时采用实时荧光定量PCR法观察AG4对肿瘤内凋亡相关基因表达的影响。结果:阳性药顺铂组(2.00 mg·kg-1)对荷瘤裸鼠的抑瘤率为49.41%,3.02 mg·kg-1AG4组的抑瘤率为42.34%,AG4对裸鼠体质量及肝、脾、肾的脏器指数没有明显影响;AG4能明显升高Bax和Bad基因的相对表达量,降低Bcl-2基因的相对表达量。结论:AG4在裸鼠体内对人鼻咽癌细胞有较强的抑制作用,对裸鼠没有明显的毒副作用,其作用机制可能与激活线粒体途径诱导肿瘤细胞凋亡有关。

走马胎提取液体内抗血栓作用研究

目的观察走马胎提取液对血栓病理模型SD大鼠体内凝血系统和血液流变学的影响,以初探其抗血栓的作用机制。方法利用0.01%AD复制血栓模型,测定SD大鼠的PT,TT,APTT,RT,Fg,全血黏度和血液生理指标。结果与正常组相比较,病理模型组SD大鼠体内PT,APTT显著缩短(P<0.05),血浆Fg含量明显升高(P<0.05),全血低切率(6 r/min和12 r/min)黏度显著上升(P<0.01或P<0.05);与病理模型组相比较,高剂量组SD大鼠体内PT,TT和APTT显著延长(P<0.05),血浆Fg含量极显著降低(P<0.01),高、中、低剂量组全血低中切率(6,12 r/min和30 r/min)黏度显著下降(P<0.01,P<0.05)。结论走马胎提取液能有效地延长血栓模型大鼠体内PT,TT和APTT以及降低全血黏度及血浆Fg含量,影响机体内、外源性凝血系统从而发挥其抗凝血作用。

走马胎离体培养及植株再生

以走马胎幼嫩叶片为外植体,研究不同培养基对走马胎叶片愈伤组织诱导、不定芽分化、增殖及生根培养的影响。结果表明:叶片在MS+6-BA 1.0mg·L^(-1)+NAA 1.0mg·L^(-1)培养基上诱导产生的愈伤组织最适合用于进行分化和增殖;愈伤组织分化不定芽的最适培养基为MS+6-BA 2.0mg·L^(-1)+NAA 0.1mg·L^(-1),分化率高达88.9%;壮苗培养基为MS+6-BA0.5mg·L^(-1)+NAA 0.1mg·L^(-1)+10%椰子水(CW);最适的生根培养基为MS+NAA0.1mg·L^(-1)+IBA 1.0mg·L^(-1),生根率达100%,根系发达,植株生长健壮。经生根培养及练苗,走马胎的假植成活率达85%。

栽培年限对走马胎生长及有效成分含量的影响

本文研究不同栽培年限对走马胎(Ardisia gigantifolia Stapf.)生长、生物量及有效成分含量的影响,拟为走马胎药材应用和采收提供科学依据。以1-5年生走马胎植株为试验材料,用全株挖掘的方法测算其生物量,用紫外分光光度计检测其有效成分。结果表明:走马胎株高、基茎及各器官的生物量随栽培年限延长呈显著(P<0.05)增加趋势,生物量增量由大到小依次为根、茎、叶;根、茎生物量增速最快出现在第4年,最慢在第5年。栽培年限可显著影响走马胎各器官的生物量分配比(P<0.05),其中根比重为0.30-0.51,普遍高于茎、叶,且最大值出现在第4年。走马胎有效成分含量总体呈现根>叶>茎的趋势;3年生植株各器官的总皂苷含量最高,1年生茎、叶的总酚、总黄酮含量最高,2年和4年生根的总酚、总黄酮含量最高。综上,走马胎最佳药用部分为根系,栽培3-4年采收比较合适。

林下不同光照条件对走马胎苗木生长及光合特性的影响

探讨走马胎(Ardisia gigantifolia)苗木在林下不同光照条件下的生长及光合特性,来寻找适合其生长的最佳环境。试验分3个处理:L1透光度20.2%,L2透光度为7.6%,L3透光度为4.0%,3个不同林下环境,每个处理3个重复。结果表明:苗高、地径,茎、叶和总干重,总叶面积,净光合速率、光饱和点、光补偿点及光下呼吸速率随着透光度递减而递减,其中,苗高之间没有显著性差异,其他指标各处理间均有极显著或显著性差异;根干重、根冠比、最大净光合速率大小为L1>L3>L2,处理间有极显著差异或显著性差异;表观光量子速率大小为L3>L1>L2,处理间有显著性差异。通过本试验结果分析,认为透光度为20.2%的林下环境最适合走马胎苗木的生长。

大叶紫金牛化学成分的研究

从大叶紫金牛(Ardisis gigantifolia Stapf)的根茎分离得到三个结晶,鉴定为:正二十九烷,α-菠甾醇和新化合物大叶紫金牛酚。