Paris saponin Ⅶ,a direct activator of AMPK,induces autophagy and exhibits therapeutic potential in non-small-cell lung cancer

Paris saponinⅦ(PSⅦ),a bioactive constituent extracted from Trillium tschonoskii Maxim.,is cytotoxic to several cancer types.This study was designed to explore whether PSⅦprevents non-small-cell lung cancer(NSCLC)proliferation and to investigate its molecular target.AMP-activated protein kinase(AMPK)has been implicated in the activation of autophagy in distinct tissues.In cultured human NSCLC cell lines,PSⅦinduces autophagy by activating AMPK and inhibiting m TOR signaling.Furthermore,PSⅦ-induced autophagy activation was reversed by the AMPK inhibitor compound C.Computational docking analysis showed that PSⅦdirectly interacted with the allosteric drug and metabolite site of AMPK to stabilize its activation.Microscale thermophoresis assay and drug affinity responsive target stability assay further confirmed the high affinity between PSⅦand AMPK.In summary,PSⅦacts as a direct AMPK activator to induce cell autophagy,which inhibits the growth of NSCLC cells.In the future,PSⅦtherapy should be applied to treat patients with NSCLC.

Biopharmaceutics classification evaluation for paris saponin Ⅶ

To study the biopharmaceutics characteristics of paris saponin Ⅶ(PSⅦ). The solubility of PSⅦ was evaluated by measurement of the equilibrium solubility in different solvents and media. The permeability of PSⅦ was evaluated by measuring the oil/water partition coefficient(lgP_(app)) and determining the apparent permeability coefficient(PC_(app)) on a mono-layer Caco-2 cell model. The effects of p-glycoprotein and multidrug resistance related protein 2 on PSⅦ transport in mono-layer Caco-2 cell model were further investigated. Finally, the small intestinal absorption of PSⅦ was investigated in rat. In solvents of different pH, the equilibrium solubility of PSⅦ was quite low, and the dose number of PSⅦ was larger than 1. The lgP_(app) of PSⅦ was less than 0. The apparent permeability coefficient [PC_(app)(AP-BL)] of PSⅦ in mono-layer Caco-2 cell model was less than 14.96 × 10^(-6) cm·s^(-1), and the efflux ratio of PSⅦ in mono-layer Caco-2 cell model was less than 1. The transport rate of PSⅦ in mono-layer Caco-2 cell model was not affected by the inhibitors of p-glycoprotein and multidrug resistance related protein 2. After oral administration, PSⅦ could be detected in rat intestinal contents, but could not be detected in the small intestinal mucosa. PSⅦ showed low solubility and permeability,which would result in low oral bioavailability in clinic. PSⅦ belonged to Class IV compound in biopharmaceutics classification system.

Primary Comments on Chemotaxonomy of Paris spp. Based on Saponins Analysis

Aim The several species of the genus Paris called ＂Chonglou＂ are famous traditional Chinese herbal medicines. We established the quantitative analysis method of the steroidal saponins in some species of the genus Paris and discussed their relations. Methods We detected the contents of 11 steroidal saponins in Paris samples with a Kromasel C18 （ 150 mm× 4.6 mm ID, 5μm） column which was subjected to gradient elution with acetonitrile-water （30：70- 60：40, V/V） at a flow rate of 1 mL· min^-1 by HPLC-ELSD and established chemical cluster tree using SPSS 11 software. Results All the samples could be separated and calibration curves of 11 saponins were prepared. We successfully detected the contents of 11 steroidal saponins in 14 Paris spp. in 30 min. The recovery for the assay of saponins was between 95 % and 97 %. The RSD of precision of 11 saponins and stability of samples were below 3 %. Chemical phylogenetic tree based on saponin contents indicated that 17 samples of Paris spp. clustered separately. Conclusion The established method is accurate and convenient, and suitable for the quantitative analysis of these 11 steroidal saponins in Paris spp.. The chemical phylogenetic tree is in accordance with Takhtajian classical taxonomy.

Parisaponin Ⅰ和Parisvietnaside A的NMR数据分析

从滇重楼中分离得到2个甾体皂苷,利用1H NMR、13C NMR、1H-1H COSY、HSQC、HMBC、1D和2D TOCSY等多种核磁共振方法鉴定其结构分别为(25R)-26-O-β-D-吡喃葡萄糖基-3β,22α,26-三羟基-呋甾-5-烯-3-O-α-L-吡喃鼠李糖基-(1→2)-[α-L-呋喃阿拉伯糖基-(1→4)]-β-D-吡喃葡萄糖苷(1,Parisaponin I)和(25R)-3β,5α,6β-三羟基-△7-螺甾烯-3-O-β-D-吡喃葡萄糖基-(1→3)-[α-L-吡喃鼠李糖基-(1→2)]-β-D-吡喃葡萄糖苷(2,paris-vietnaside A).对化合物1和2的1H NMR和13C NMR信号分别进行了归属和详细分析,并纠正了文献中的核磁数据归属错误.化合物2为首次从滇重楼中分离得到.

Paris Saponin Ⅰ Induces G_2/M Cell Cycle Arrest and Apoptosis in Human Gastric Carcinoma SGC7901 Cells

The aim of this study was to investigate the effect of Paris saponin I （PSI ） on human gastric carcinoma cell growth and apoptosis and to explore the potential mechanisms. The proliferation of SGC7901 cells was monitored by the MTT cell viability assay, while the nuclear morphology of apoptotic cells was assessed by Hoechst 33258 staining. Flow cytometry was performed to analyze the cell cycle progression of propidium iodide （PI）-stained SGC7901 cells and the apoptotic rate of annexin V/PI-stained ceils. Western blotting was used to examine the expression of several cell cycle proteins, including cyclin 131 and Cdkl, and the apoptosis-regulated proteins Bcl-2, Bax, cytochrome c, procaspase-9, and procaspase-3. The MTT assay demonstrated that PSI could induce significant dose- and time-dependent inhibition of SGC7901 cell proliferation. Marked morphological changes, including condensation of chromatin, nuclear fragmentation and apoptotic bodies were clearly shown on Hoechst 33258 staining. PS I treatment also resulted in the disruption of the cell cycle at Gz/M and the induction of apoptosis. Following PSI treatment, the cell cycle-related proteins cyclin B 1 and Cdkl were down- regulated. Expression of the pro-apoptotic protein Bax was increased, while anti-apoptotic protein Bcl-2 decreased. PSI treatment resulted in elevated cytoplasmic cytochrome c and activation of the apoptotic proteases caspase-9 and caspase-3. These data indicate that PS I acts as an inhibitor of proliferation in SGC7901 cells by inducing cell cycle arrest and mitochondria-dependent apoptosis. PSI is a potential therapeutic agent against human gastric carcinoma.

A new spirostanol saponin from the rhizomes of Paris mairei

A new spirostanol steroidal saponin, named maireioside A （1）, together with three known steroidal saponins, hypoglaucin G （2）, parisaponin I （3）, and diosgenin-3-O-α-L-rhamnopyranosyl （1→4）-[α-L-rhamnopyranosyl （1→2）]-β-D-glucopyranoside （4）, were isolated from the rhizomes of Paris mairei. The structure elucidation was accomplished by 1D and 2D NMR methods, HR-ESI-MS, and hydrolysis. C 2009 Qiang Wang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

Two New Highly Oxygenated Spirostanol Saponins from Paris polyphylla var.stenophylla

Phytochemical investigation of the rhizomes of Paris polyphylla var.stenophylla led to the isolation of two new highly oxygenated spirostanol saponins,named paristenosides A(1)and B(2),together with seven known compounds.Their structures were established mainly on the base of NMR spectroscopic techniques and mass spectrometry,as well as chemical methods.In addition,the cytotoxicity of the two new saponins was tested.Graphical Abstract Two new highly oxygenated spirostanol saponins,paristenosides A(1)and B(2),were isolated from the rhizomes of Paris polyphylla var.stenophylla.Their structures were established mainly based on NMR spectroscopic techniques and mass spectrometry,as well as chemical methods.

重楼皂苷Ⅶ通过p38丝裂原活化蛋白激酶信号通路对肝癌细胞恶性生物学行为的影响

目的 观察重楼皂苷Ⅶ对肝癌细胞恶性生物学行为的影响,并探讨相关机制。方法 于2021年6月至2022年6月,取对数期人肝癌HepG2细胞,分为对照组(常规培养)、重楼皂苷Ⅶ组(重楼皂苷Ⅶ0.8μmol/L)、SB203580[p38丝裂原活化蛋白激酶(p38 MAPK)信号通路抑制剂]组(SB203580 10μmol/L)、联合组(重楼皂苷Ⅶ0.8μmol/L、SB203580 10μmol/L)。噻唑蓝法检测细胞增殖能力;膜联蛋白Ⅴ(AnnexinⅤ)/碘化丙啶(PI)双染法检测细胞凋亡率;划痕实验检测细胞迁移能力;小室实验检测细胞侵袭能力;蛋白质印迹法检测细胞p38 MAPK、磷酸化p38丝裂原活化蛋白激酶(p-p38 MAPK)、细胞外信号调节激酶(ERK)1/2、磷酸化细胞外信号调节激酶(p-ERK1/2)蛋白表达。结果 与对照组24、48、72 h吸光度值,迁移率(74.33±9.37)%,凋亡率(3.25±0.78)%,p-p38 MAPK/p38 MAPK、p-ERK1/2/ERK1/2及侵袭细胞数(364.92±47.99)个比较,重楼皂苷Ⅶ组24、48、72 h吸光度值,迁移率(11.21±3.35)%降低,凋亡率(39.87±8.94)%,p-p38 MAPK/p38 MAPK、p-ERK1/2/ERK1/2升高,侵袭细胞数(54.84±7.41)个减少(P<0.05);SB203580组24、48、72 h吸光度值,迁移率(89.30±14.56)%升高,凋亡率(1.05±0.15)%,p-p38MAPK/p38 MAPK、p-ERK1/2/ERK1/2降低,侵袭细胞数(617.04±75.34)个增加(P<0.05)。与重楼皂苷Ⅶ组比较,联合组24、48、72 h吸光度值,迁移率(40.52±8.18)%升高,凋亡率(11.30±2.80)%,p-p38 MAPK/p38 MAPK、p-ERK1/2/ERK1/2降低,侵袭细胞数(141.36±16.75)个增加(P<0.05);与SB203580组比较,联合组24、48、72 h吸光度值、迁移率降低,凋亡率、p-p38 MAPK/p38MAPK、p-ERK1/2/ERK1/2升高,侵袭细胞数减少(P<0.05)。结论 重楼皂苷Ⅶ可抑制肝癌HepG2细胞增殖、迁移及侵袭等恶性生物学行为,并诱导其凋亡,作用机制可能与激活p38 MAPK信号通路相关。

Determination of the Content of Total Saponins in Paris daliensis H.Li et V. G. Soukoup and Paris dulongensis H. Li et S. kurita

[Objectives]To determine the content of total saponins in Paris daliensis H. Li et V. G. Soukoup and Paris dulongensis H. Li et S.kurita,fill the gap in the study of Paris daliensis H. Li et V. G. Soukoup and Paris dulongensis H. Li et S. kurita,and lay a foundation for searching new medicinal resources of Paris L. [Methods]The perchloric acid colorimetric method and UV spectrophotometer were used to determine the content of total saponins in Paris daliensis H. Li et V. G. Soukoup and Paris dulongensis H. Li et S. kurita at 406 nm. [Results]The lowest content of total saponins in Paris daliensis H. Li et V. G. Soukoup was 2. 637%,while the highest content reached 5. 474%; the lowest content of total saponins in Paris dulongensis was 1. 806%,while the highest content reached 3. 532%. Through the methodological examination,it was found that this method was stable and reliable. [Conclusions] The content of total saponins was high in Paris daliensis H.Li et V. G. Soukoup and Paris dulongensis H. Li et S. kurita,and it was suggested to further study and find the medicinal resources of Paris L.

Contrastive Study on Content and Anti-oxidation Activity of Total Saponins from Cultivated and Wild Paris Plants in Southwest China

[Objectives]To study content of total saponins from cultivated and wild Paris herbs in Southwest China,evaluate its in vitro antioxidation activity,and explore the correlation between quality of Paris herbs and production place,variety,cultivated and wild varieties.[Methods]Colorimetric method of perchloric acid reaction was used,and content of total saponins from Paris herbs was determined by ultraviolet spectrophotometer at 406 nm. [Results]The lowest content of total saponins from cultivated and wild Paris herbs in Southwest China was0. 55%,while the maximum was 12. 24%,with obvious difference. Total saponins from Paris herbs had stronger clearance ability on free radical DPPH and stronger reduction ability on Fe^(3+),and the results showed good dose-effect relationship with concentration. Among them,S6 had the highest clearance ability on DPPH,which reached 89. 66%. In the determination of reduction ability,the absorbance of S16 reached3. 643 and was the highest,with very good reducing property. Content and anti-oxidation capacity of total saponins from Paris herbs in Southwest China did not have obvious correlation with production place,altitude and cultivation but was related to variety. [Conclusions]The quality of Paris herbs in Southwest China was unstable,and their anti-oxidation abilities were also different,and cultivation could not guarantee high quality. It should normalize cultivation,and develop planting industry of Paris herbs,which could guarantee stable supply of Paris herbs and stability and controllability of quality.

南重楼Paris vietnamensis活性物质的分离与鉴定

目的研究南重楼Paris vietnamensis （Takht．）中具有细胞毒活性的甾体皂苷类化学成分。方法采用柱色谱进行分离纯化，通过光谱分析和理化方法鉴定化合物结构，并进行体外细胞毒活性筛选。结果从南重楼中分离得到11个甾体皂苷类化合物，化合物1结构为：3β，5α，6α-三羟基-7（8）-烯-异螺甾烷醇-3-氧-β-D-葡吡喃糖基（1→3）[α-L-鼠李吡喃糖基（1→2）]-β-D-葡吡喃糖苷（1），命名为南重楼皂苷A。化合物2—11分别为：25（R）-薯蓣皂苷元-3-氧-α-L-阿拉伯呋喃糖基（1→4）]-β-D-葡吡喃糖苷（2）；25（R）薯蓣皂苷元-3-氧-α-L-鼠李糖吡喃基（1→2）-β-D-葡吡喃糖苷（3）；25（R）薯蓣皂苷元-3-氧-α-L-阿拉伯呋喃糖基（1→4）[α—L-鼠李吡喃糖基-（1→2）]-β-D-葡吡喃糖苷（4）；25（R）薯蓣皂苷元-3-氧-α-L-葡吡喃糖基（1→3）[α—L-鼠李吡喃糖基-（1→2）]-β-D-葡吡喃糖苷（5）；25（R）薯蓣皂苷元-3-氧-α-L-鼠李吡喃糖基（1→4）]-α-L-鼠李吡喃糖基（1→4）[-α-L-鼠李吡喃糖基（1→2）]-β-D-葡吡喃糖苷（6）；25（R）偏诺苷元-3-氧-α-L-阿拉伯呋喃糖基（1→4）]-β-D-葡吡喃糖苷（7）；25（R）偏诺苷元-3-氧-α-L-鼠李吡喃糖基（1→2）]-β-D-葡吡喃糖苷（8）；25（R）偏诺苷元-3-氧-α-L-阿拉伯呋喃糖基（1→4）]-α-L-鼠李吡喃糖基（1→2）]-β-D-葡吡喃糖苷（9）;25（R）偏诺皂苷元-3-氧-α-L-葡吡喃糖基（1→3）[α-L-鼠李吡喃糖基（1→2）]-β-D-葡吡喃糖苷（10）；25（R）偏诺苷元-3-氧-α-L-鼠李吡喃糖基（1→4）-α-L-鼠李吡喃糖基（1→4）-α-L-鼠李吡喃糖基（1→2）]-β-D-葡吡喃糖苷（11），体外筛选表明部分甾体皂苷类化合物具有细胞毒作用。结论化合物1为一新化合物，化合物2，3，6—11均为首次从南重楼中获得。化合物3，4，6，8具有对肝癌HepG2和胃癌SGC-7901的细胞毒活性。

Comprehensive Evaluation on Impacts of Diseases on Quality of Paris polyphylla var. chinensis Based on Ultraviolet and Infrared Spectra

[Objectives] The research aimed to evaluate impacts of diseases on quality of Paris polyphylla var. chinensis. [Methods]Ultraviolet spectrophotometry was used to determine and contrast content of total saponins in root,stem and leaf from healthy and diseased plants. Infrared characteristic absorption peaks of healthy and diseased plants were found by infrared fingerprint method for comparative analysis.[Results]Total saponins content in root sample J4 of healthy plant reached 4. 89% and was the highest,while it was 0. 13% in stem sample J11 of healthy plant and was the lowest. Total saponins content in root sample B1 of diseased plant was 1. 68% and was the highest,while it was 0. 1% in stem sample B7 of diseased plant and was the lowest. In healthy and diseased plants,total saponins content in root was significantly higher than that in stem and leaf. Content of total saponins in root from healthy plant was significantly higher than that from diseased plant,and there was little difference in stem and leaf of healthy and diseased plants. Root sample Jg of healthy plant had obvious C-O characteristic vibration of polysaccharides and glycosides and absorption peak of O-H bending vibration in steroidal saponin near 1 160. 02 cm-1,while diseased plant had no obvious absorption peak. Near 861. 97 and 768. 07 cm-1,root sample Jg of healthy plant had significant C-C stretching vibration in sugar ring and characteristic absorption peak of characteristic vibration of steroidal saponin,while root sample Bg of diseased plant had no obvious characteristic peak. [Conclusions] Diseases significantly affected composition and content of total saponins and steroidal saponins from P. polyphylla var. chinensis,further affecting quality of P. polyphylla var. chinensis.

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)。

Unraveling the serial glycosylation in the biosynthesis of steroidal saponins in the medicinal plant Paris polyphylla and their antifungal action

Sugar-sugar glycosyltransferases play important roles in constructing complex and bioactive saponins.Here,we characterized a series of UDP-glycosyltransferases responsible for biosynthesizing the branched sugar chain of bioactive steroidal saponins from a widely known medicinal plant Paris polyphylla var.yunnanensis.Among them,a 2'-O-rhamnosyltransferase and three 6'-O-glucosyltrasferases catalyzed a cascade of glycosylation to produce steroidal diglycosides and triglycosides,respectively.These UDP-glycosyltransferases showed astonishing substrate promiscuity,resulting in the generation of a panel of 24 terpenoid glycosides including 15 previously undescribed compounds.A mutant library containing 44 variants was constructed based on the identification of critical residues by molecular docking simulations and protein model alignments,and a mutant UGT91AH1^(Y187A)with increased catalytic efficiency was obtained.The steroidal saponins exhibited remarkable antifungal activity against four widespread strains of human pathogenic fungi attributed to ergosterol-dependent damage of fungal cell membranes,and 2'-O-rhamnosylation appeared to correlate with strong antifungal effects.The findings elucidated the biosynthetic machinery for their production of steroidal saponins and revealed their potential as new antifungal agents.

云南重楼的皂苷类化学成分研究

目的 研究云南重楼根状茎中的皂苷类化学成分。方法 利用硅胶柱色谱、硅胶C-18柱色谱、Sephadex LH-20凝胶柱色谱以及半制备高效液相色谱等技术,从云南重楼根茎70%乙醇提取物的水饱和正丁醇萃取物中,纯化得到单体成分。通过NMR、MS等波谱分析和酸水解等化学方法对其进行结构鉴定。结果 共分离得到6个皂苷类化合物,分别鉴定为parisyunnanosideⅠ(1)、paristenoside B(2)、26-O-β-D-吡喃葡萄糖基-3β,16α,26-三羟基-(23R,25R)-16,23-环胆甾烷醇-5,17(20)-二烯-22-酮-3-O-α-L-呋喃阿拉伯糖基-(1→4)-[α-L-吡喃鼠李糖基-(1→2)]-β-D-吡喃葡萄糖苷(3)、26-O-β-D-吡喃葡萄糖基-17,22-二羟基-(25R)-呋甾-5-烯-3-O-α-L-吡喃鼠李糖基-(1→2)-β-D-吡喃葡萄糖苷(4)、parisyunnanoside A(5)和26-O-β-D-吡喃葡萄糖基-3β,26-二羟基-(25R)-胆甾-5,17(20)-二烯-16,22-二酮-3-O-α-L-吡喃鼠李糖基-(1→4)-[α-L-吡喃鼠李糖基-(1→2)]-β-D-吡喃葡萄糖苷(6)。结论 化合物3、4和6为首次从云南重楼中发现。

云南重楼果皮中1个新的C_(21)甾体皂苷

目的:研究云南重楼果皮中的甾体皂苷类成分。方法:采用HPD-100大孔吸附树脂柱、正相硅胶柱、ODS柱、Sephadex LH-20葡聚糖凝胶柱和半制备型高效液相色谱等方法对云南重楼果皮70%乙醇渗漉提取物中的甾体皂苷类成分进行系统研究,通过现代波谱学技术结合参考文献对化合物结构进行鉴定。结果:从云南重楼果皮中分离得到8个甾体皂苷类化合物,分别鉴定为:17α-hydroperoxide pregn-5-en-20-one-3-O-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→4)]-β-D-glucopyranoside(1)、重楼皂苷Ⅳ(2)、ypsilandroside L(3)、重楼皂苷Ⅲ(4)、pregna-5,16-dien-3β-ol-20-one-3β-O-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→4)]-β-D-glucopyranoside(5)、pregna-5,16-dien-3β-ol-20-one-3β-O-α-L-rhamnopyranosyl-(1→2)-[α-L-arabinopyranosyl-(1→4)]-β-D-glucopyranoside(6)、pregna-5,16-dien-3β-ol-20-one-3β-O-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→4)]-β-D-glucopyranoside(7)、aethioside A(8)。结论:其中,化合物1为一个新的C_(21)甾体皂苷类化合物,化合物3、5、6、8为首次从重楼属植物中分离得到。

七叶一枝花抗癌临床应用及作用机制研究进展

七叶一枝花作为我国的传统中药,具有抗炎、抑菌、抗癌等多重药理活性,临床可广泛应用于辅助治疗胃癌、肝癌、肺癌、乳腺癌等恶性肿瘤疾病。研究表明甾体皂苷类成分是七叶一枝花抗癌作用的主要有效成分,其可通过抑制癌细胞增殖、诱导癌细胞凋亡、调控上皮间质转化过程、抗癌细胞血管生成以及诱导癌细胞的自噬等多方面发挥良好的抗癌作用。文章通过对七叶一枝花抗癌临床应用及作用机制的研究进展进行综述,为未来七叶一枝花及其有效成分进一步开发应用于抗癌临床治疗提供参考依据。

基于UPLC-MS对七叶一枝花不同部位化学成分的比较分析

目的:比较分析重楼属植物七叶一枝花的不同组织部位(叶片、茎秆、根茎、根)中化学成分的差异,科学合理开发药用资源。方法:采用超高效液相和质谱联用技术,结合代谢组学的方法,鉴定不同组织部位化学成分,检测相对含量的大小,探讨各类有机化合物的组成比例和分布规律。结果:七叶一枝花不同组织部位中共检测出63种化合物,含9中甾体皂苷类,其余为萜类化合物和萜类,化合物成分在叶片、茎秆、根茎中的的相对含量和分布规律存明显差异,采用主成分分析,能对不同组织器官进行直观的鉴定区分。结论:液质联用技术在中药的质量分析和品质控制上具有较好的指导意义,结合代谢组学的分析方法,在样品的分类鉴定上优势明显,数据结果也表明七叶一枝花在药用资源的开发利用上具有较好的前景。

不同病害对滇重楼甾体皂苷积累的影响

为研究根腐病、茎腐病、叶斑病对滇重楼根茎中甾体皂苷类活性成分积累的影响,采用高效液相色谱法(HPLC)对3种患病(根腐病、茎腐病、叶斑病)及健康滇重楼根茎中7种活性成分(重楼皂苷Ⅰ、重楼皂苷Ⅱ、重楼皂苷Ⅶ、重楼皂苷Ⅲ、重楼皂苷Ⅴ、重楼皂苷Ⅵ、重楼皂苷H)的含量进行测定;采用超高效液相色谱-电喷雾-四极杆飞行时间高分辨质谱联用(UPLC-ESI-Q-TOF-MS)技术对患病及健康滇重楼根茎中甾体皂苷类成分进行鉴定,并对质荷比m/z 50~2000的主成分进行分析。结果表明,在HPLC条件下,健康及患病滇重楼中均未检测到重楼皂苷Ⅴ;重楼皂苷H仅在茎腐病滇重楼根茎中检测到,且重楼皂苷H含量较高;重楼皂苷Ⅰ、Ⅱ、Ⅶ总含量表现为叶斑病>根腐病>茎腐病>健康滇重楼。通过UPLC-ESI-Q-TOF-MS从患病及健康滇重楼根茎中共鉴定出18个甾体皂苷成分;根腐病、茎腐病和叶斑病中甾体皂苷的化学成分均少于健康滇重楼。

Steroid and triterpenoid saponins from the rhizomes of Paris polyphylla var.stenophylla

Five new saponins,including three steroid saponins,paristenoids A-C(1-3),and two triterpenoid saponins,paristenoids D-E(4-5),along with four known ones(6-9)were isolated from the rhizomes of Paris polyphylla var.stenophylla.The structures of the isolated compounds were identified nainly by detailed spectroscopic analysis,including extensive 1D and 2D NMR,MS,as well as chemical methods.Compound 3 is a new cyclocholestanol-type steroidal saponin with a rare 6/6/6/5/5 fused-rings cholestanol skeleton,and this skeleton has been first found from the genus Paris.The cytotoxicities of the isolated compounds against three human three glioma cell lines(U87MG,U251MG and SHG44)were evaluated,and compound 7 displayed certain inhibitory effect with ICso values of 15.22±1.73,18.87±1.81 and 17.64±1.69μmol^(-1),respectively.