Dammarane-type saponins from steamed leaves of Panax notoginseng

Four new dammarane-type triterpenoid saponins,namely notoginsenosides SFt1-SFt4(1-4)were isolated from the steamed leaves of Panax notoginseng(Burk.)F.H.Chen(Araliaceae),together with 17 known saponins.Their structures were established on the basis of detailed spectroscopic analyses and acidic hydrolysis.The known ginsenosides Rk2 and Rh3 were obtained from P.notoginseng for the first time.All of these new saponins showed no in vitro cytotoxicity against five human cancer cell lines(HL-60,SMMC-7712,A-549,MCF-7,and SW480).

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.

STUDY ON DAMMARANE-TYPE SAPONINS OF GINSENG FRUIT——ISOLATION AND IDENTIFICATION OF TWO CONFIGURATIONAL ISOMERS

Ginseng fruit is the fully grown berries of the famous medicinal plant Panax ginseng C. A. Meyer. In recent years, it has been found that all the saponins the ginseng fruit contains are effective in resisting fatigue, reducing symptoms of oxygen deficit and preventing arteriosclerosis caused by excessive amount of cholesterol in the blood. So the dammarane-type saponins of the ginseng fruit have been studied. Eight such monomer

Antioxidant,antimicrobial,and α-glucosidase inhibitory activities of saponin extracts from walnut(Juglans regia L.) leaves

Objective:To investigate the relationship between triterpenoid saponin content and antioxidant,antimicrobial,and α-glucosidase inhibitory activities of 70%ethanolic,butanolic,aqueous,supernate and precipitate extracts of Juglans regia leaves.Methods:Triterpenoid saponins of different Juglans regia leaf extracts were measured by the vanillin method.Antioxidant activity was evaluated against DPPH and ABTS free radicals.We also assessed α-glucosidase inhibitory and antimicrobial activities of the leaf extracts.Pearson’s correlation coefficient was evaluated to determine the correlation between the saponin content and biological activities.Results:The butanolic extract was most effective against DPPH with an IC50of 6.63μg/mL,while the aqueous extract showed the highest scavenging activity against ABTS free radical with an IC50of 42.27μg/mL.Pearson’s correlation analysis indicated a strong negative correlation (r=-0.956) between DPPH radical scavenging activity (IC50) and the saponin content in the samples examined.In addition,the aqueous extract showed the best α-glucosidase inhibitory activity compared with other extracts.All the extracts had fair antibacterial activity against Bacillus subtilis,Escherichia coli,and Klebsiella pneumoniae except for the aqueous extract.Conclusions:Juglans regia extracts show potent antioxidant,antimicrobial,and α-glucosidase inhibitory activities.There is a correlation between saponin levels in Juglans regia leaf extracts and the studied activities.However,additional research is required to establish these relationships by identifying the specific saponin molecules responsible for these activities and elucidating their mechanisms of action.

PnMYB4 negatively modulates saponin biosynthesis in Panax notoginseng through interplay with PnMYB1

Saponins are the main triterpenoid ingredients from Panax notoginseng,a well-known Chinese medicine,and are important sources for producing drugs to prevent and treat cerebrovascular and cardiovascular diseases.However,the transcriptional regulatory network of saponin biosynthesis in P.notoginseng is largely unknown.In the present study we demonstrated that one R2R3-MYB transcription factor,designated PnMYB4,acts as a repressor of saponin accumulation.Suppression of PnMYB4 in P.notoginseng calli significantly increased the saponin content and the expression level of saponin biosynthetic genes.PnMYB4 directly bound to the promoters of key saponin biosynthetic genes,including PnSS,PnSE,and PnDS,to repress saponin accumulation.PnMYB4 and the activator PnMYB1 could inter-acted with PnbHLH,which is a positive regulator of saponin biosynthesis,to modulate the biosynthesis of saponin.PnMYB4 competed with PnMYB1 for binding to PnbHLH,repressing activation of the promoters of saponin structural genes induced by the PnMYB1-PnbHLH complex.Our study reveals that a complex regulatory module of saponin biosynthesis is associated with positive and negative MYB transcriptional regulators and provides a theoretical basis for improving the content of saponins and efficacy of P.notoginseng.

Rhizoma paridis saponins protected against liver injury in diethylnitrosamine-induced mice

Background:Diethylnitrosamine,one of food additives,possessed a strong carcinogenic effect in human.Rhizoma paridis saponins,as the main active components of Paris polyphylla,have a good anti-cancer effect in our previous research.To verify their inhibitory effect on diethylnitrosamine-induced liver cancer,we carried out this study.Methods:We established diethylnitrosamine-induced mouse hepatocarcinoma models to evaluate antitumor of Rhizoma paridis saponins.Subsequently,gas chromatography-mass spectrometry was applied to analyze the metabolites in the urine and serum samples.Results:Rhizoma paridis saponins alleviated diethylnitrosamine-induced hepatocarcinogenesis.On the one hand,Rhizoma paridis saponins down-regulated the levels of liver function markers,such as alanine aminotransferase,aspartate transaminase and alpha fetoprotein.On the other hand,Rhizoma paridis saponins reduced metabolic disorders by increasing fructose and mannose metabolism,and decreasing pentose and glucuronate interconversion,inositol phosphate metabolism,and the process of saturated fatty acids transforming to unsaturated fatty acids,which based on the regulating mRNA expression of glucose transporter type 4,lactate dehydrogenase A,fatty acid synthetas,acetyl-CoA carboxylase and apolipoprotein A-I.Conclusion:Rhizoma paridis saponins has the potential application to inhibit chemical-induced hepatocarcinogenesis in the future.

Effects of Tribulus terrestris saponins on proliferation and invasion of A549 cells

Objective:Tribulus terrestris saponin is a traditional Chinese medicine in China.This experiment was designed to investigate the effects of tribulus terrestris saponin on the proliferation and invasion ability of non-small cell lung cancer A549 cells.Methods:A549 cells were divided into normal control and experimental groups(Tribulus terrestris saponin 250μg/mL group,Tribulus terrestris saponin 200μg/mL group,Tribulus terrestris saponin 150μg/mL group,Tribulus terrestris saponin 100μg/mL group,Tribulus terrestris saponin 50μg/mL group).The proliferation viability of the cells in each group was detected by CCK8,the invasion of tumor cells was detected by Transwell model.The mRNA expression of MMP9 and caspase-3 in each group of cells was detected by RT-PCR.Immunofluorescence staining was used to observe the fluorescence intensity of caspase-3 in each group of cells.Results:Compared with the normal control group,tribulus terrestris saponin significantly inhibited the proliferation activity and invasion ability of A549 cells,which was statistically significant(P<0.01).In the invasion assay,compared with the control group,MMP9 expression was significantly reduced and caspase-3 expression was significantly increased in the tribulus terrestris saponin group,and both were concentration-dependent,with statistically significant differences(P<0.01).By cellular immunofluorescence staining experiments,it was found that the fluorescence expression of caspase-3 was enhanced in the experimental group compared with the normal control group,in which the high concentration saponin group was significantly higher than the low concentration group.Conclusion:Tribulus terrestris saponin can inhibit the invasive ability of A549 cells by down-regulating the expression of MMP9,and induce irreversible apoptosis by up-regulating the activation of caspase-3 expression to form caspase-3.

Effects of Arbuscular Mycorrhizal Fungi on the Physiology and Saponin Synthesis of Paris polyphylla var. yunnanensis at Different Nitrogen Levels

Arbuscular mycorrhizal fungi(AMF)are important members of the plant microbiome and affect the uptake and transfer of mineral elements by forming a symbiotic relationship with plant roots.Nitrogen(N),as an important min­eral element,can directly affect plant growth and development at different N levels.It has been confirmed that inoc­ulation with AMF can improve the efficiency of N utilization by plants.However,there are still fewer reports on the dynamic relationship between arbuscular mycorrhizal and plant secondary metabolites at different nitrogen levels.In this experiment,the physiological indexes and genes related to saponin synthesis were determined by applying differ­ent concentration gradients of nitrogen to the medicinal plant P.polyphylla var.yunnanensis infested by AMF as the test material.It was found that nitrogen addition increased the biomass,chlorophyll content,and nutrient content of above-and below-ground plant parts and increased the content of saponin content of P.polyphylla var.yunnanensis to some extent,but AMF inoculation increased the saponin content of P.polyphylla var.yunnanensis more significantly.AMF inoculation also promoted the expression of genes related to the saponin synthesis pathway,including 3-hy­droxy-3-methylglutaryl coenzyme A synthase(HMGS),squalene epoxidase 1(SE1),and cycloartenol synthase(CAS),which is in according with the accumulation of saponin in plants.It also may increase the saponin content of AMF plants by altering the expression of P450s and UGTs related to saponin synthesis.

无患子皂苷对自发性高血压大鼠血管内皮功能和NLRP3炎性小体的影响

目的探讨无患子皂苷对自发性高血压大鼠血管内皮功能和核苷酸结合寡聚化结构域样受体蛋白3(NLRP3)炎性小体的影响。方法将6只WKY大鼠设为对照组,18只自发性高血压大鼠(SHR)分为模型组、无患子皂苷组和替米沙坦组,每组6只。对照组和模型组大鼠灌胃生理盐水,无患子皂苷组和替米沙坦组分别灌胃无患子皂苷(162 mg/kg)和替米沙坦(10 mg/kg),连续灌胃35 d。给药结束后测量各组大鼠尾动脉收缩压(SBP)和舒张压(DBP),免疫组化法检测胸主动脉内膜中血管性假血友病因子(vWF)表达,HE染色观察大鼠胸主动脉组织病理变化,ELISA法检测血清中半胱天冬氨酸蛋白酶1(caspase-1)和白细胞介素1β(IL-1β)水平,RT-qPCR和Western blot法检测主动脉组织中p38、NLRP3、caspase-1 mRNA和蛋白表达。结果与对照组比较,模型组大鼠尾动脉SBP和DBP、血清中caspase-1和IL-1β水平、胸主动脉中p38、NLRP3、caspase-1 mRNA和蛋白表达均升高(P<0.01),胸主动脉内膜中vWF阳性表达增多(P<0.01),主动脉内膜和外膜脱落严重,中膜增厚;与模型组比较,无患子皂苷组和替米沙坦组大鼠尾动脉SBP和DBP、血清中caspase-1和IL-1β水平、胸主动脉中p38、NLRP3、caspase-1 mRNA和蛋白表达均降低(P<0.05),胸主动脉内膜中vWF阳性表达减少(P<0.05),主动脉内外膜损伤减轻,中膜厚度也有所降低。结论无患子皂苷能够有效降低自发性高血压大鼠的血压,改善血管内皮功能障碍,抑制炎症反应,其机制可能与抑制NLRP3炎症通路的激活有关。

玉竹的化学成分、药理作用及其食品开发研究进展

玉竹不仅富含糖、蛋白质、氨基酸、维生素和矿物质等营养成分,还含较高的多糖、甾体皂苷、黄酮等生物活性成分,具有抗氧化、调节糖脂代谢、增强免疫、抗肿瘤、抗微生物、抗疲劳、抗衰老、护肝、调节胃肠道菌群、减肥等药理作用,已广泛用于普通食品和健康食品的开发利用。本文对其营养功能成分、生物活性及其在食品加工领域中的应用进展进行系统总结,以为其深入开发提供参考和支持。

茶皂素和博落回生物碱复配对4种病原菌的联合毒力

为了明确博落回生物碱与茶皂素混配对棉花立枯病菌、棉花枯萎病菌、苹果轮纹病菌和柑橘炭疽病菌的联合毒力,采用生长速率法测定了博落回生物碱、茶皂素及其不同配比混剂对4种病菌的毒力,通过交互测定法测定了茶皂素和博落回生物碱的毒性比例和增效系数。结果表明:博落回生物碱与茶皂素复配对棉花枯萎病的联合毒力主要为拮抗或相加作用,博落回生物碱与茶皂素复配对苹果轮纹病的联合毒力主要为相加作用,博落回生物碱与茶皂素质量比为1∶48.7的混剂对棉花立枯病表现为增效作用,增效系数为1.536;博落回生物碱与茶皂素质量比为1∶20.2的混剂对柑橘炭疽病菌表现出较好的增效作用,增效系数为1.537。

β-七叶皂苷通过抑制NF-κB、NLRP3信号通路改善大鼠创伤性脊髓损伤

目的研究β-七叶皂苷对大鼠创伤性脊髓损伤(tSCI)的作用及其机制。方法将72只SD大鼠随机均分为假手术组、tSCI组、低剂量皂苷组和高剂量皂苷组。BV-2小胶质细胞分为对照组、模型组、低、中、高浓度皂苷组。采用旷场实验评估各组大鼠运动功能;HE染色观察各组大鼠脊髓组织病理学变化;ELISA法检测脊髓组织及BV-2细胞中炎症因子白细胞介素(IL)-1β、IL-6、肿瘤坏死因子-α(TNF-α)表达。免疫荧光法检测BV-2细胞中核因子-κB(NF-κB)蛋白表达;Western blotting检测BV-2细胞中NOD样受体热蛋白结构域相关蛋白3(NLRP3)、凋亡相关斑点样蛋白(ASC)、IL-1β和Caspase-1蛋白表达。结果β-七叶皂苷能减轻tSCI大鼠脊髓组织病理损害程度,促进大鼠运动功能的恢复。与tSCI组或模型组比较,不同剂量或浓度皂苷组大鼠脊髓组织或BV-2细胞中IL-1β、IL-6和TNF-α表达水平均降低,且呈剂量或浓度依赖性降低(P<0.05)。与模型组比较,不同浓度皂苷组BV-2细胞中NF-κB、NLRP3、ASC、IL-1β和Caspase-1蛋白表达均降低,且呈浓度依赖性降低(P<0.05)。结论β-七叶皂苷对大鼠创伤性脊髓损伤具有一定的保护作用,该作用可能与抑制NF-κB/NLRP3信号通路有关。

氮磷钾配方施肥提高林下七叶一枝花产量和重楼皂苷含量

【目的】研究氮、磷、钾不同组合用量对林下栽培七叶一枝花产量及重楼皂苷含量的影响,为七叶一枝花人工栽培合理施肥提供参考。【方法】采用“3414”试验设计,利用福建南平杉竹混交林下4年生七叶一枝花(Paris polyphylla Smith var.chinensis (Franch.) Hara)进行田间试验,将氮、磷、钾肥当地适宜水平定为“2”,分别为N 270 kg/hm^(2)、P_(2)O_(5) 375 kg/hm^(2)、K_(2)O 300 kg/hm^(2),不足“1”和过量“3”水平分别为适宜水平的0.5、1.5倍。在七叶一枝花收获时期,测定其植株形态、根茎产量、4种重楼皂苷含量等指标,并计算生产效益。【结果】氮、磷、钾肥用量均显著影响七叶一枝花的植株形态、根茎产量和重楼皂苷含量,对七叶一枝花根茎产量的提升率分别为59.75%、27.54%、63.15%,以钾肥的贡献率最高,其次为氮肥,磷肥较低。N1水平下,增加磷、钾水平显著降低七叶一枝花的株高、茎粗和叶长,N3水平七叶一枝花的株高、叶长均达到最高,但茎粗低于N1和N2水平,表明适宜氮肥用量对七叶一枝花的生长至关重要。七叶一枝花的根茎产量和总重楼皂苷含量还受肥料交互效应的影响。当N、P_(2)O_(5)、K_(2)O用量分别为270、375、450 kg/hm^(2) (N_(2)P_(2)K_3)和270、375、300 kg/hm^(2)(N_(2)P_(2)K_(2))时,根茎产量达到最高,分别为2804、2648 kg/hm^(2)。N_(2)P_(2)K_3的总重楼皂苷含量也最大,达到1.62%,显著高于其他处理。施氮磷钾肥净增收效益在N_(2)P_(2)K_3处理下最高,N_(2)P_(2)K_(2)处理次之。【结论】适量的氮、磷肥配合较高的钾肥可显著提升七叶一枝花根茎产量和总重楼皂苷含量,提高七叶一枝花的经济效益。因此,在供试地区,推荐N、P_(2)O_(5)、K_(2)O用量分别为270、375、450 kg/hm^(2)。

辽东楤木叶总皂苷提取工艺研究

以总皂苷提取率、两种质量标志性皂苷成分的提取率为指标探索辽东楤木叶药材中皂苷的提取工艺。分别考察药材浸泡达饱和的时间、回流提取时乙醇溶液用量、提取时间、提取次数以及乙醇溶液浓度对辽东楤木叶皂苷提取率的影响,并采用正交实验法对辽东楤木叶总皂苷的提取工艺进行优化。结果表明,药材经乙醇水溶液浸泡3h以上达到吸收饱和;加8倍量的70%乙醇水溶液回流提取3次,每次2.5h,所得的辽东楤木叶总皂苷提取率及两种指标性皂苷提取率均较高。

油茶籽粕发酵菌株的筛选鉴定及发酵产物特性分析

油茶行业的迅速发展导致油茶籽粕废弃物的大量产生,其落后的处理方式造成了严重的资源浪费,制约了我国油茶行业的可持续发展。油茶籽粕中富含有机质,利用微生物发酵法降解其中的纤维素、木质素及茶皂素等生物大分子来制备有机肥是实现油茶籽粕合理资源化利用的有效途径。通过筛选获得3株针对油茶籽粕中纤维素和木质素的高效降解菌,包括1株真菌X1-1,属于Pleurostomarichardsiae,以及2株细菌M4-2和M5-2,分别为蒙氏假单胞菌(Pseudomonas monteilii)和类芽孢杆菌(Paenibacillus sp)属,可有效降低发酵产物中茶皂素的含量,实现油茶籽粕的无害化处理。实验结果显示,经菌株X1-1、M4-2和M5-2发酵处理28 d后,油茶籽粕中纤维素含量的降解率分别为29.74%、19.65%和13.19%,木质素含量的降解率分别为12.84%、17.85%和26.39%,茶皂素含量的降解率分别为34.06%、45.05%和46.15%;且发酵后的油茶籽粕腐熟度、有机质含量和养分含量等指标均符合有机肥标准。研究结果拓展了油茶籽粕的资源化利用途径,同时为木质素和纤维素的高效降解提供了良好的菌种资源。

商陆提取物药理作用研究进展

商陆是我国传统峻下逐水中药,收载于历版《中华人民共和国药典》,入药部位为根部,具有利尿泻下、抗炎、抗肿瘤、祛痰镇咳平喘等药理活性。临床多用于治疗肾炎、肝硬化腹水、乳腺增生、银屑病等疾病。通过对商陆提取物和化学成分药理作用进行总结,为今后商陆深入研究及合理开发利用提供支持和参考依据。

不同覆盖栽培方式对金铁锁生长习性及总皂苷含量的影响

本研究设置绿色无纺布覆盖(处理1)、白色农膜覆盖(处理2)、银黑双色农膜覆盖(处理3)和不覆盖任何农膜对照(CK)4种栽培方式,探明金铁锁覆盖栽培的效果。结果表明:采用不同栽培方式,金铁锁生长情况及总皂苷含量存在较大差异,以处理3表现最好,杂草和病虫害发生较轻,长势较好,总皂苷含量最高。

预知子中saponins P_K的HPLC分析

目的分析不同种与不同产地预知子中saponins PK的含量,为预知子质量标准建立提供进一步参考。方法采用高效液相色谱分析,Alltech C18色谱柱,乙腈-水(0.1%磷酸)(29.5∶70.5)为流动相,检测波长203 nm。结果saponins PK的保留时间为14 min,线性范围为0.091～0.455μg(r=0.999 9),加样回收率101.93%。所测样品中saponins PK的含量在0.04%～2.04%。结论该法快捷、简便、准确,可用于预知子的质量评价。

藜麦糠皮皂苷提取技术研究进展

藜麦皂苷属于齐墩果烷型五环三萜化合物,具有广泛的生理和药理活性,包括抗炎、抗菌、抗螺、抗氧化、免疫调节以及提高皮肤渗透性等功能,在食品、药品和化妆品等行业有着重要的商业用途。藜麦糠皮是藜麦加工的副产物,由于皂苷含量高而无法在食品领域得到合理利用。目前,尚缺乏高效脱除藜麦糠皮皂苷的技术手段,因此,研究藜麦糠皮皂苷的提取技术具有重要的应用价值。本文总结了超高压提取、超声波辅助提取、微波辅助提取、生物酶辅助提取、双水相提取、丙酮溶液提取、超临界CO_(2)提取、离子液体提取及低共熔溶剂提取藜麦皂苷的技术特点,并结合作者的实践经验对原料预处理以及如何选择溶剂、温度和料液比等工艺参数进行分析,为藜麦糠皮的高效综合利用和藜麦皂苷新产品的开发提供有益借鉴。

基于转录组测序的苦瓜皂苷合成相关基因的鉴定和分析

【目的】皂苷是苦瓜果实苦味的主要来源,具有降血糖、抗癌等多种药用价值。鉴定和挖掘参与调控苦瓜皂苷生物合成的代谢通路及基因,为进一步深入解析苦瓜皂苷形成的分子机制提供参考。【方法】以苦瓜高代自交系GK24为试验材料,分别在子房期(T1)、幼果期(T2)、商品果期(T3)和完全成熟期(T4)取果实组织,通过香草醛-冰醋酸法测定不同时期的苦瓜皂苷含量,利用转录组测序的方法鉴定差异表达基因。【结果】从T1到T4,苦瓜内源皂苷含量随着果实发育而呈现显著下降的趋势。转录组测序共鉴定到17 504个基因,在T1-vs-T2、T2-vs-T3和T3-vs-T4三组比较中,下调表达基因数量均高于上调表达基因数量。GO富集分析表明含磷复合物代谢过程、驱动蛋白复合体和2-琥珀酰-6-羟基-环己二烯-1-羧酸合成酶活性分别是生物过程、细胞组分及分子功能模块最显著富集的条目。KEGG分析显示全局与概述图谱、碳水化合物代谢和氨基酸代谢是3组比较中共同的最显著富集的代谢通路。根据表达模式可将基因划分为20个模块,其中profile 0中基因的表达量从T1到T4逐渐降低,与苦瓜果实发育过程中皂苷含量变化规律一致。从profile 0中鉴定出与苦瓜皂苷生物合成相关的基因14个,包括萜类骨架生物合成通路上的基因AAT1、HMG1、MVK、PMK、MVD2和FPS1,倍半萜与三萜生物合成途径中的基因SS12、SQE1和CPQ及后修饰酶基因CYP97A3、CYP71AN24、UGT94E5及UGT73C6。实时荧光定量PCR(qRT-PCR)结果与RNA-seq结果一致。【结论】苦瓜果实中皂苷含量随着果实不断成熟而逐渐降低。苦瓜皂苷生物合成首先通过上游的萜类骨架生物合成(ko00900)代谢途径完成萜类皂苷骨架的积累,随后通过倍半萜与三萜生物合成(ko00909)代谢途径以及下游的氧化还原酶、糖基转移酶的修饰最终生成皂苷,本研究通过转录组测序共鉴定到14个与苦瓜皂苷生物合成相关的基因。