Research progress on chemical constituents and pharmacological effects of medicinal plant Gynostemma pentaphyllum

Gynostemma pentaphyllum(G.pentaphyllum)is a traditional medicinal plant with medicinal and economic value.With in-depth research on the chemical compositions and pharmacological effects,the applications of G.pentaphyllum have been expanded.G.pentaphyllum has the effects of clearing heat and detoxification,relieving cough and phlegm,nourishing heart,tranquilizing nerves,and can be used to treat gastroenteritis,tracheitis,pharyngitis,hyperlipidemia,and arteriosclerosis.It can also be used to alleviate symptoms such as migraines,insufficient sleep,and white hair.In recent years,G.pentaphyllum has also been used for clinical adjuvant treatment of various cancers.In this study,the chemical constituents and pharmacological effects on G.pentaphyllum in recent years were reviewed.This review could provide reference for further development and utilization of G.pentaphyllum.

葫芦科植物绞股蓝(Gynostemma pentaphyllum)灭螺初步研究

采用绞股蓝地上部分的水提液处理钉螺，并用清水作对照，结果表明绞股蓝对钉螺具有一定的毒杀作用，随浓度的增加，钉螺的死亡率呈上升趋势，250、500、1000mg／L的溶液具有40％～100％的灭杀效果．即使是125mg／L低浓度的绞股蓝的水提液，处理时间达到5d后，钉螺的死亡率也可以达到50％以上．

Stevenleaf from Gynostemma Pentaphyllum inhibits human hepatoma cell(HepG2)through cell cycle arrest and apoptotic induction

The anticancer activity of stevenleaf(SV)on the basis of cell viability,cell cycle,and apoptosis induction in HepG2 cancer cells were evaluated.SV controlled the growth of HepG2 cells with IC50 of 139.82μmol/L for 24 h,IC50 of 119.12μmol/L for 48 h and cell cycle arrested at G0/G1 phase,induced cell apoptosis and enhanced intracellular ROS generation.For cell cycle arrest,the mRNA expression levels of p21,p27 and p53 were up-regulated,while the expression levels of Cyclin A,Cyclin D1,Cyclin E and CDK1/2 were downregulated.SV efficiently up-regulated TNF R1,TRADD1 and FADD and down-regulated Caspase8 for cell death receptors;similarly,up-regulated Bax,Bak,Cytc,Apaf1,Caspase3 and Caspase9,and down-regulated Bcl2,Bcl xl and Bad for mitochondrial signal pathway.SV induced the mTOR-mediated cell apoptosis in HepG2 cells via activation of Akt and AMPK.The mechanistic explanation for the anticancer activity of SV as functional food can be derived from above results.

Two Ways to Induce Gynostemma pentaphyllum Plantlets from Tissue Culture

[Objectives]This study was conducted to investigate rapid propagation systems of Gynostemma pentaphyllum.[Methods]Ten different media were tested to select the optimal media for inducing callus proliferation,bud differentiation and rooting by using tissue culture technology,with G.pentaphyllum stem segments and leaves as explants.The stem segments of G.pentaphyllum were used as explants to directly induce rooting and germination,and appropriate media were selected.[Results]The optimum callus induction medium for G.pentaphyllum stem segments was MS+6-BA 1.0 mg/L+NAA 0.4 mg/L;the optimum rooting medium for stem callus was MS+NAA 0.2 mg/L;and the optimum germination medium for stem segments was MS+6-BA 1.0 mg/L.The optimum callus induction medium for G.pentaphyllum leaves was MS+6-BA 0.5 mg/L+NAA 0.2 mg/L;and the optimum rooting medium for leaves was MS+NAA 0.4 mg/L.The optimum rooting medium for G.pentaphyllum stem segments was MS+IAA 1.0 mg/L,with which the rooting rate was 100%,the average root length was about 3 cm,and the average number of sprouts per explant was 1.48,so it is the optimal condition.[Conclusions]This study provides a new method for in-vitro cultivation of G.pentaphyllum and has far-reaching significance for improving human health.

A new dammarane-type triterpene saponin from Gynostemma pentaphyllum

One new dammarane-type triterpene saponin, named (20S)-3β,20,21-trihydroxydammar-24-ene 3-O[α-L- rhamnopyranosyl-(1→2)][β-D-xylopyranosyl(l→3)]-β-D-glucopyranoside (1), was isolated from the aerial parts of Gynostemma pentaphyllum (Thunb.) Makino. Its structural elucidation was accomplished mainly on the basis of the interrelation of spectroscopic methods, such as IR, HR-TOF-MS, NMR.

Ethanol extract from Gynostemma pentaphyllum ameliorates dopaminergic neuronal cell death in transgenic mice expressing mutant A53T human alpha-synuclein

Gynostemma(G.) pentaphyllum(Cucurbitaceae) contains various bioactive gypenosides. Ethanol extract from G. pentaphyllum(GP-EX) has been shown to have ameliorative effects on the death of dopaminergic neurons in animal models of Parkinson’s disease(PD) induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-and 6-hydroxydopamine. PD patients exhibit multiple symptoms, so PD-related research should combine neurotoxin models with genetic models. In the present study, we investigated the ameliorative effects of GP-EX, including gypenosides, on the cell death of dopaminergic neurons in the midbrain of A53 T α-synuclein transgenic mouse models of PD(A53 T). Both GP-EX and gypenosides at 50 mg/kg per day were orally administered to the A53 T mice for 20 weeks.α-Synuclein-immunopositive cells and α-synuclein phosphorylation were increased in the midbrain of A53 T mice, which was reduced following treatment with GP-EX. Treatment with GP-EX modulated the reduced phosphorylation of tyrosine hydroxylase, extracellular signal-regulated kinase(ERK1/2), Bcl-2-associated death promoter(Bad) at Ser112, and c-Jun N-terminal kinase(JNK1/2) due to α-synuclein overexpression. In the A53 T group, GP-EX treatment prolonged the latency of the step-through passive avoidance test and shortened the transfer latency of the elevated plus maze test. Gypenosides treatment exhibited the effects and efficacy similar to those of GP-EX. Taken together, GP-EX, including gypenosides, has ameliorative effects on dopaminergic neuronal cell death due to the overexpression of α-synuclein by modulating ERK1/2, Bad at Ser112, and JNK1/2 signaling in the midbrain of A53 T mouse model of PD. Further studies are needed to investigate GP-EX as a treatment for neurodegenerative synucleinopathies, including PD. This study was approved by the Animal Ethics Committee of Chungbuk National University(approval No. CBNUA-956-16-01) on September 21, 2016.

ANTAGONISM OF TOTAL FLAVONES OF GYNOSTEMMA PENTAPHYLLUM (THUNB) MAK TO ANIMAL EXPERIMENTAL ARRHYTHMIA

The action of total flavones of Gynostemma pentaphyllum (Thunb) Mak (TFG) 60 mg/kg i.v. could prevent arrhythmias induced by drugs and myocardial ischemia were investigated. In anesthetized rats and guinea pigs. The results showed that in TFG group the duration of ventricular tachycardia (VT) induced by aconitine in rats was shortened (P<0 01) and the incidence of ventricular fibrillation (VF) and the mortality were decreased (P<0 01) respectively. The arrhythmias induced by i.v. BaCl 2 4 mg/kg in rats were immediately recovered to a normal sinus rhythm and VT induced by i.v. CaCl 2 130 mg/kg in rats was decreased by TFG i.v. TFG i.v. elevated the doses of i.v. strophanthin G to induce ectopic beats (EB), VT, VF and cardiac arrest (CA) in guinea pigs by 89%, 58%, 27%, and 28% (P<0 01) respectively. The incidence of VF induced by coronary artery ligation in rats was decreased (P<0 01), duration of EB, duraton of VT and VF decreased to 45%, 42% and 0% of the NS group respectively. The results suggest that TFG in dosage of 60 mg/kg might be useful for the prevention of VT and VF.

Three New Dammarane Glycosides from Gynostemma pentaphyllum

Three new dammarane-type glycosides (1-3) had been isolated from the aerial part of Gynostemma pentaphyllum (Thunb) Makino. The structures of compounds 1-3 had been elucidated as 3b, 12b, 25-trihydroxy-20(S), 24(S)-epoxydammarane 3-O-b-D-glucopyranosyl (12)-b-D- xylo -pyranoside, 3b, 12b, 25-trihydroxy-20(S), 24(R)-epoxydammarane 3-O-b-D-glucopyranosyl (12) -b-D-xylopyranoside and 3b, 12b, 23b, 25-tetrahydroxy-20(S), 24(S)-epoxydammarane 3-O-b-D- glucopyranosyl (12)-b-D-xylopyranoside, respectively, on the basis of chemical and spectro -scopic methods.

A New Triterpene Saponin from Gynostemma pentaphyllum

Objective To study the triterpene saponins from Gynostemma pentaphyllum with antitumor activities. Methods The 75% EtOH extract of G. pentaphyllum was used for isolation by silica gel column chromatography and preparative HPLC. The structures of pure compounds isolated were identified by the spectral analysis and chemical evidence. Results Two compounds were isolated and identified as 23(S)-3β,20ξ,21ξ-trihydroxy-19-oxo-21,23-epoxydammar-24-ene 3-O-α-L-rhamnopyranosyl (1→2)-[β-D-xylopyranosyl (1→3)]-β-D-arabinopyranoside (1) and 23(S)-21(R)-O-n-butyl-3β,20ξ-dihydroxy-21,23-epoxydammar-24-ene 3-O-α-L-rhamnopyranosyl (1→2)-[β-D-xylo- pyranosyl (1→3)]-β-D-arabinopyranoside (2). Conclusion Compound 2 is a new triterpene saponin with moderate antitumor activities against the HL-60, Colon205, and Du145 cell lines.

Effect of light quality on total gypenosides accumulation and related key enzyme gene expression in Gynostemma pentaphyllum

Objective: Light quality has effect on the accumulation of gypenosides in the medicinal plant Gynostemma pentaphyllum in the family Cucurbitaceae,while the squalene synthase(SS)and squalene epoxidase(SE)are the key enzymes for gypenoside biosynthesis.The objective of this study was to elucidate the relationship between light quality and biosynthesis key enzyme involving the regulation of gypenoside accumulation.Methods: The content of total gypenosides was measured by colorimetric method and the expression of SS and SE gene was determined by quantitative Real-time PCR in the seedlings of G.pentaphyllum which were grown with different light quality.Results: Light quality showed remarkable impacts on the accumulation of total gypenosides.The highest content of total gypenosides in the plant under red light condition was determined,followed by blue light and white light,while the lowest content was recorded under dark condition.q RT-PCR analysis proved that the expression levels of SS and SE genes were also affected by light quality.The high-level gene expressions of SS and SE were found in the plant under red light condition,followed by blue light,with the least content in darkness.The statistical analysis revealed that the total gypenosides were significantly different in different light treatment and the content of total gypenosides was positively related to the expression of SS and SE genes.Conclusions: Light quality regulates gypenoside accumulation via altering the expression of SS and SE in G.pentaphyllum.

Two new dammarane-type sapogenins from Gynostemma pentaphyllum

Two new sapogenins,named(20S,24R)-3β,20,21β,25-tetrahydroxy-21,24-cyclodammarane(1)and 3β-hydroxyetio-17β-dammaranic acid(2),were isolated from the alkaline hydrolysate of Gynostemma pentaphyllum saponins.Their structures were elucidated by spectroscopic methods.

玉米须绞股蓝复合提取总黄酮工艺及其降压片的制备

以玉米须(stigma maydis)、绞股蓝(Gynostemma pentaphyllum)(1∶1)为提取原料,总黄酮含量为考察指标,通过提取溶剂、乙醇体积分数、提取温度、提取时间、料液比和提取次数等单因素考察对复合总黄酮含量的影响,再通过正交试验优化总黄酮的提取工艺,最后将优化提取的总黄酮过D101大孔吸附树脂精制后制备成降压片。结果表明,复方总黄酮的最佳提取工艺为乙醇体积分数50%,料液比1∶10,50℃下提取3.5 h。制备的片剂质量(片重差异±5.1%,脆碎度0.83%,崩解时限2.41 min)符合《中华人民共和国药典》(2020版)片剂的有关规定,并且降压片能降低SHR大鼠血压。

SPE-HPLC-UV法测定绞股蓝提取物中皂苷的含量

本试验旨在建立固相萃取-高效液相色谱-紫外检测法(SPE-HPLC-UV)对绞股蓝提取物中绞股蓝皂苷XLIX和皂苷A进行定量分析。样品经甲醇提取,采用C_(18)固相萃取柱净化,使用Kinetex C_(18)色谱柱(150 mm×4.6 mm,2.6μm)分离,流动相乙腈/水,柱温40℃,检测波长203 nm。依照此法测定绞股蓝粗提物中三萜皂苷XLIX和皂苷A的含量。结果表明:2种绞股蓝皂苷在一定质量浓度范围内线性关系良好(r≥0.999),平均回收率为91.38%~98.4%,相对标准偏差为0.69%~2.48%。该方法的灵敏度、准确度和精密度均符合检测技术要求,且简便快速,适用于绞股蓝提取物中绞股蓝皂苷XLIX和皂苷A含量的准确测定。

基于“肾主水”理论的七叶胆总苷治疗膀胱癌大鼠的作用研究

目的基于“肾主水”理论观察膀胱灌注七叶胆总苷治疗N-甲基-N-亚硝基脲(MNU)诱导的SD大鼠膀胱癌(BC)的作用。方法取106只SPF级SD大鼠,随机分为空白组、模型组、低剂量组、中剂量组、高剂量组及阳性对照组,模型组、低剂量组、中剂量组、高剂量组及阳性对照组通过膀胱灌注的方式给予MNU进行造模,空白组和模型组予生理盐水0.5 ml膀胱灌注;低剂量组(20 mg/kg)、中剂量组(40 mg/kg)、高剂量组(80 mg/kg)予七叶胆药粉灌注给药;阳性对照组予卡介苗冻干粉灌注给药。通过组织学病理切片观察膀胱内的形态、计算各组膀胱脏器指数及检测相关生理指标,评价膀胱灌注七叶胆对MNU诱导SD大鼠BC的作用效果。结果第16周,模型组大鼠膀胱的脏器指标高于空白组,差异有统计学意义(P<0.05)。低剂量组、中剂量组、高剂量组和阳性对照组的大鼠膀胱脏器指标低于模型组,差异有统计学意义(P<0.05)。结论七叶胆总苷具有一定的抗膀胱癌的药理活性,可为抗膀胱癌药物开发提供一定的参考。

富硒绞股蓝功能性茶冻的研制

绞股蓝是一种药食同源的草本植物,兼具较高的营养价值与药用价值。目前,绞股蓝相关产品以绞股蓝茶为主,存在味苦、浮沫多的弊端,制约了绞股蓝茶推广销售。本文以富硒超微绞股蓝茶粉为主要原料,以黄原胶、甜菊糖苷(甜味剂)、水等为辅料,以感官评分为主要指标,利用正交试验与Box-Behnken设计-响应面法筛选出最优的富硒绞股蓝功能性茶冻配方工艺,即富硒超微绞股蓝茶粉0.65 g、水1.00 L、甜菊糖苷0.10 g、黄原胶0.20 g,同时添加魔芋葡甘聚糖60 g。相较于传统绞股蓝茶,所得产品克服了绞股蓝茶味苦、浮沫多的弊端,丰富了绞股蓝茶产品形式;茶冻状态突破了传统茶冲泡形式下功能成分利用率低的限制,极大地提高了硒等功能活性物质的摄取率;以膳食纤维魔芋葡甘聚糖为成胶成分,既使产品具有细腻弹爽的口感、透明均匀的色泽,又赋予其调节肠道菌群、缓解便秘的功能特性,增强了产品的功能活性;以甜菊糖苷甜味剂代替传统茶冻中的蔗糖,更适宜控糖人群食用。该研究结果为绞股蓝基功能性产品的研制与推广提供了技术和理论借鉴。

绞股蓝中达玛烷型四环三萜皂苷元的波谱学特征

达玛烷型四环三萜皂苷类成分是绞股蓝中主要有效成分,该类化学成分在人参、三七、西洋参等其他药用植物中也有分布,因其具有抗肿瘤、降血脂血糖等广泛的药理活性,一直是中药领域的研究热点。由于达玛烷型四环三萜皂苷元部分在核磁共振波谱中存在大量的亚甲基、次甲基信号叠加,其化学结构鉴定难度较大。本文拟对已报道的绞股蓝中达玛烷型四环三萜皂苷类成分的波谱学数据进行归纳,总结出绞股蓝皂苷元的结构特点及其波谱学特征,为绞股蓝乃至其他药材中达玛烷型四环三萜皂苷类成分的结构解析提供科学依据。

分析珍珠粉、茯苓、绞股蓝及其复合物改善小鼠睡眠作用的影响

目的:分析珍珠粉、茯苓、绞股蓝及其复合物改善小鼠睡眠作用的影响。方法:通过直接睡眠试验、延长戊巴比妥钠睡眠时间试验、戊巴比妥钠阈下剂量催眠试验、巴比妥钠睡眠潜伏期试验评价其对小鼠睡眠情况的影响,通过急性毒性试验评价珍珠粉茯苓绞股蓝复合物的安全性。结果:珍珠粉、茯苓、绞股蓝及其复合物各剂量组对正常小鼠均无直接睡眠作用,但是复合物各剂量组均可以延长戊巴比妥钠诱导的小鼠睡眠时间,有统计学意义(P<0.01或P<0.001),增加戊巴比妥钠阈下催眠剂量入睡小鼠只数(P<0.01),能够显著缩短小鼠的睡眠潜伏期,有统计学意义(P<0.001)。此外,复合物高剂量组小鼠下丘脑及血清中的5-羟色胺(5-HT)及γ-氨基丁酸(GABA)含量均显著高于对照组,差异有统计学意义(P<0.01或P<0.001)。与珍珠粉、茯苓、绞股蓝比较,复合物在延长戊巴比妥钠睡眠时间、增加小鼠戊巴比妥钠阈下剂量催眠只数、缩短巴比妥钠睡眠潜伏期方面效果显著优于各单药组;急性毒性试验表明珍珠粉茯苓绞股蓝复合物对受试小鼠未出现不良反应。结论:以上结果表明,珍珠粉、茯苓、绞股蓝及复合物均可在一定程度上改善小鼠的睡眠,并且珍珠粉、茯苓、绞股蓝组成的复合物具有协同增效的作用,安全性良好。

不同水培条件对绞股蓝生长及总皂苷含量的影响

绞股蓝是一种重要的药食同源植物,因含有人参皂苷类物质而享有“南方人参”的美誉。由于野生绞股蓝资源日益枯竭,人工引种栽培绞股蓝已成为必然趋势。然而,受土壤灌溉、施肥、农药使用等因素影响,绞股蓝药材品质不稳定、重金属含量超标等问题时有发生,严重影响其规范化种植和药材质量安全。水培生产具有周期短、产量高、无连作障碍、可有效避免重金属污染等优点,被广泛应用于多种中药材生产中。对绞股蓝幼苗进行不同营养液、不同温度、不同光照强度和光周期处理,研究各处理对绞股蓝生长和总皂苷积累的影响,以期得到适合绞股蓝生长和有效成分积累的最优水培条件,研究结果表明,pH为6.0的日本园试营养液是绞股蓝水培的最佳营养液。相关性分析结果显示,不同营养液条件下,绞股蓝单株总皂苷量与株高、叶长、叶宽、叶片数、单株鲜重及单株干重呈高度正相关,表明培育高生物量植株是提高绞股蓝药材质量的关键。在环境温度为20~30℃,光周期为每天光照10~14 h,光照强度为100μmol/(m^(2)·s)条件下,绞股蓝幼苗生长较好,且干样品总皂苷含量超过3%,高于现有标准。

绞股蓝的化学成分及其生物活性研究进展

绞股蓝是我国重要的可食用植物资源,为葫芦科绞股蓝属草质攀援植物,广泛分布于我国陕西南部和长江以南等地区。文章对2000—2022年国内外绞股蓝的研究文献进行可视化分析,发现绞股蓝及其皂苷成分是研究热点,对绞股蓝的研究集中在化学成分、功能活性和药理作用等方面,但目前缺乏对其化学组成和生物活性的系统综述。基于此,文章对绞股蓝中皂苷类、多糖类、黄酮类、氨基酸和微量元素等化学成分,以及其抗氧化、抗衰老、降血脂、降血糖、护肝、抗肿瘤、保护神经等生物活性的最新研究进行归纳总结,结果表明目前对绞股蓝产地之间的质量比较,及其主要药效成分的吸收代谢和作用机制研究仍较匮乏。提出今后可将绞股蓝黄酮类化合物作为研究目标,进一步明确黄酮的成分结构及药理活性作用机制;基于绞股蓝多成分、多药理活性的特点,利用分子生物学、代谢组学等技术手段探究绞股蓝活性成分的药效物质基础和作用机制,以及活性成分代谢产物及代谢途径;规范绞股蓝产地道地性和产品质量标准,以期为绞股蓝资源的进一步开发利用提供参考。

绞股蓝的活性成分及其在畜禽生产和疾病防治中的应用

绞股蓝为葫芦科绞股蓝属植物的干燥全草,是我国常见的传统中草药,富含黄酮类、糖类、皂苷等多种药理活性成分,具有抗炎、抗氧化、增强免疫力、维护肠道菌群健康和护肝等多种生物学功能。绞股蓝作为可饲用天然植物,可改善畜禽的生产性能,提高机体免疫力,保障机体健康。文章对近几年绞股蓝研究成果进行整理,就绞股蓝的活性成分及其在畜禽生产中的应用进行综述,为其在动物生产中的应用提供参考。