苦瓜茎叶醋酸乙酯部位的化学成分研究

目的研究苦瓜茎叶醋酸乙酯部位的化学成分,为进一步开发利用苦瓜茎叶提供依据。方法采用反复硅胶柱色谱、反相ODS柱色谱、Sephadex LH-20等柱色谱进行分离纯化,并根据波谱数据鉴定化合物的结构。结果分离得到3种苦瓜三萜,分别鉴定为苦瓜素I(1)、kuguacin N(2)、3,7-二羟基-23(R)-乙氧基-19-醛基-5,24-二烯醇(3)。结论化合物3为新化合物,命名为23-乙基苦瓜素I。     

续断的化学成分研究

目的研究续断的化学成分。方法运用大孔树脂、反相硅胶及制备高效液相等色谱技术进行分离纯化,并根据理化性质和波谱数据鉴定化合物的结构。结果分离得到13个化合物,其中7个环烯醚萜苷和6个木脂素类化合物,分别鉴定为马钱苷(1)、獐牙菜苷(2)、6’-O-β-D-apiofuranosyl-sweroside(3)、续断苷H(4)、续断苷F(5)、续断苷E(6)、triplostoside A(7)、(7R,8S,7’R,8’S)-5-methoxyprinsepiol-4-O-β-D-glucopyranoside(8)、(7R,8S,7’R,8’S)-prinsepiol-4-O-β-D-glucopyranoside(9)、acanthoside D(10)、(7R,8S,7’R,8’S)-fraxiresinol-4’-O-β-D-glucopyranoside(11)、(7R,8S,7’R,8’S)-8-hydroxypinoresinol-4’-O-β-D-glucopyranoside(12)、(7R,8S,7’R,8’S)-8-hydroxypinoresinol-4-O-β-D-glucopyranoside(13)。结论其中化合物8、9、11、12、13为首次从川续断属植物中分离得到。     

中国红参化学成分的研究(Ⅱ)

从中国红参(Panax ginseng C.A.Meyer)中分离出十种单体(RG 1～10),用IR.MS(FD-MS.FAB-MS)、~(13)C-NMR以及化学方法等鉴定了化学结构,分别为20(R)-ginsenoside Rh,(RG-1),ginsenoside-Rg,(RG-2),20(R)-ginsenoside-Rg_2(RG-3),20(R)proto-panaxatriol(RG-4)以及人参皂甙Rg.(RG-5),—Re(RG-6)—Rd(RG-7),—RC(RG-8),—Rd_2(RG-9),—Rb,(RG-10);其中RG-1、RG-3、RG-4系首次从中国红参分离得到的人参皂甙成分。用薄层对照未炮制前的白参不含以上三种成分,这可能是红参与白参药理作用上差异的原因之一。     

山苦瓜中三萜及甾体成分的研究

从葫芦科植物山苦瓜(Momordica dioica)干燥块根中分离鉴定出5个三萜及甾体化合物:α-菠甾醇硬脂酸酯(I),α-菠甾醇 3-O-β-D-吡喃葡萄糖甙(II),3β-羟基-23-氧-齐墩果-12-烯-28-酸-3-O-β-D-吡喃葡萄糖醛酸甙(II),3β-羟基-23-氧-齐墩果-12-烯-28-酸-3-O-β-D-吡喃葡萄糖甙(IV)和3β,23-二羟基齐墩果-12-烯-28-酸-3-O-β-D-吡喃葡萄糖甙(V)。其中,成分II为一新化合物。     

人参花蕾化学成分研究

用溶剂提取、硅胶柱层析及反相Lobar柱层析等方法,从人参花蕾中分离得到十八种化学成分。根据理化性质、光谱分析并与标准品对照进行正、反相TLC,鉴定了其中十三种化合物,分别为β-谷甾醇(1),胡罗卜甙(2),20(R)-人参皂甙-Rh_1(3),20(S)-Rg_2(4),20(R)-Rg_2(5),-Rf(6),-Re(7),-Rg_3(8),-Rd(9),-Re(10),-Rb_2(11),棕榈酸(12)和反式对羟基肉桂酸(13)。其中化合物(1),(2),(3),(5),(8)和(13)为首次从人参花蕾中分离得到的已知成分。     

中国红参化学成分的研究(Ⅱ)

从中国红参(Panax ginseng C.A.Meyer)中分离出十种单体(RG 1～10),用IR.MS(FD-MS.FAB-MS)、¹³C-NMR以及化学方法等鉴定了化学结构,分别为20(R)-ginsenoside Rh,(RG-1),ginsenoside-Rg,(RG-2),20(R)-ginsenoside-Rg₂(RG-3),20(R)proto-panaxatriol(RG-4)以及人参皂甙Rg.(RG-5),—Re(RG-6)—Rd(RG-7),—RC(RG-8),—Rd₂(RG-9),—Rb,(RG-10);其中RG-1、RG-3、RG-4系首次从中国红参分离得到的人参皂甙成分。用薄层对照未炮制前的白参不含以上三种成分,这可能是红参与白参药理作用上差异的原因之一。     

人参茎叶中皂甙类化学成分的研究

从辽宁桓仁县产人参(Panax ginseng C.A.Meyer)茎叶中分离得到十一种人参皂甙单体(L_1—L_(11))。用化学方法,IR,FD—MS,~(13)C—NMR,HPLC 等方法鉴定了其中七种化学结构;分别为人参皂甙(ginsenosides —Rh_1,—Rg_3,—Rg_2,—Rg_1,—Re,—Rc,—Rb_2)。其中—Rh_1,—Rg_3两种,首次从人参茎叶中分离得到的已知皂甙类成分。未见报导.     

苦瓜中葫芦烷型三萜成分及其抗肝纤维化活性的研究

目的 研究苦瓜酸水解产物的化学成分及其抗肝纤维化活性。方法 用正、反相柱层析等色谱手段进行分离纯化,用波谱技术与文献数据对照鉴定其结构;并用四甲基偶氮唑盐(methylthiazolyl tetrazolium, MTT)法测定部分化合物体外对大鼠肝星状细胞(t-HSC/Cl-6)增殖的抑制作用。结果 共分离出10个葫芦烷型三萜类化合物,分别鉴定为:5β,19-epoxy-3β-hydroxy-19(R)-methoxy-27-norcucurbita-6,23(E)-dien-25-one(1);5β,19-epoxy-3β-hydroxy-19(S)-methoxy-27-norcucurbita-6, 23(E)-dien-25-one(2);5β,19-epoxy-25-methoxycucurbita-6,23(E)-dien-3β-ol(3);karavilagenin A(4);(23E)-5β,19-epoxycucurbita-6,23,25-triene-3β-ol(5);23E-5β,19-epoxy-cucurbita-6,23-dien-3β,25-diol(...     

仙鹤草根芽中化学成分的研究

从仙鹤草根芽的石油醚提取物中分得五个化合物。通过理化常数,光谱分析和化学合成将其中的一个新化合物确定为(R)-(-)-仙鹤草酚B(Ⅲ),其余四个已知化合物分别被鉴定为:鹤草酚(Ⅰ),正(?)九烷(Ⅱ),β-谷甾醇(Ⅳ)和伪绵马素(Ⅴ)。其中Ⅴ系首次从植物中得到。     

人参茎叶中微量三萜化合物的化学研究

近年报告从五加科人参属植物人参(Panax ginseng C.A.Meyer)的地上茎及叶中分得多种成分。日本学者从人参叶中分得人参皂甙-Rb_1,-Rb_2,-Rc,-Rd,-Re,-Rg_1,-F_1,-F_2,-F_3~((1,2))我国学者徐绥绪和王志学等人从人参茎叶(辽宁桓仁)中分得人参皂甙-Rb_1,-Rb_2,-Rc,     

苦瓜水提物对实验性糖尿病小鼠血糖、血脂的影响

目的：研究苦瓜水提物对实验性2型糖尿病模型小鼠体重和血清中血糖值（GLU）、总胆固醇（TC）、甘油三酯（TG）、超氧化物歧化酶（SOD）、丙二醛（MDA）和游离脂肪酸（NEFA）的影响。方法：雄性昆明小鼠喂以高脂饲料（10％蛋黄。10％猪油,1％胆固醇,0．2％胆盐,78．8％基料）1个月,诱发胰岛素抵抗,继以低剂量四氧嘧啶（90mg·kg～,腹腔注射）,使之产生高血糖症,建立2型糖尿病小鼠模型。以苦瓜水提取物10g·kg^-1（相当于生药材重量）的剂量通过灌胃给药,30d后测定小鼠空腹血糖、糖耐量、血液各项生化指标。结果：显著降低了2型糖尿病小鼠的GLU、NEFA、TC、TG和MDA值（P〈0．05）;显著升高了2型糖尿病小鼠SOD值（P〈0．05）。结论：苦瓜水提物能够显著降低2型糖尿病小鼠的血糖值,并可调节其血脂代谢。     

落花生茎叶醋酸乙酯部位化学成分研究

目的 研究落花生Arachis hypogaea茎叶的化学成分.方法 采用硅胶柱色谱、凝胶柱色谱和ODS柱色谱进行分离纯化,通过理化方法和波谱数据进行结构鉴定.结果 从落花生茎叶70％乙醇提取液的醋酸乙酯萃取部位分离得到8个化合物,经波谱分析鉴定其结构,分别为肉豆蔻酸(1)、十五碳酸(2)、汉黄芩素(3)、美迪紫檀素(4)、邻苯二甲酸二丁酯(5)、异香草酸(6)、芒柄花素(7)、β-谷甾醇(8).结论 化合物2、3、4、5、7为首次从该植物中分离得到.     

半红树植物阔苞菊茎叶的化学成分

目的为寻找半红树植物阔苞菊[Pluchea indica(L.)Less.]不同于陆生植物的次生代谢产物及民间治疗瘰疬(淋巴腺结核)的物质基础,对其进行化学成分的研究。方法采用硅胶、SephadexLH-20、HPLC等色谱方法进行分离纯化,通过理化性质、波谱方法以及结合文献对照鉴定结构。结果从阔苞菊体积分数为90%的乙醇提取物的乙酸乙酯部分分离并鉴定了3个噻吩类衍生物及3个倍半萜类化合物,分别为:2-(1,3-戊二炔)-5-(4-乙酰氧基-3-羟基-1-丁炔)-噻吩[2-(pant-1,3-diynyl)-5-(4-acetoxy-3-hydroxybuta-1-ynyl)-thiophene,1]、2-(1,3-戊二炔)-5-(4-乙酰氧基-3-氯-1-丁炔)-噻吩[2-(pant-1,3-diynyl)-5-(4-acetoxy-3-chlorobuta-1-ynyl)-thio-phene,2]、2-(1,3-戊二炔)-5-(3、4-二羟基-1-丁炔)-噻吩[2-(pant-1,3-diynyl)-5-(3,4-dihydroxybuta-1-ynyl)-thiophene,3]、8,11-二羟基-1(10)-瓦伦烯[valenc-1(10)-ene-8,11-diol,4]、2,8,11-三羟基-1(10)-瓦伦烯[valenc-1(10)-ene-2,8,11-triol,5]、5-氧代-5,6-氢-希菲比尔醇[5-oxo-5,6-H-silphiperfolen,6]。结论化合物2-6均为首次从该种植物中获得。     

高效液相色谱法同时测定马蓝根、茎、叶中4种成分的含量及其3种不同干燥方法的评价

目的：建立高效液相色谱法测定马蓝根、茎、叶中靛蓝、靛玉红、色胺酮、异鼠李素4种成分的含量,并对其烘干、阴干、冻干3种不同干燥方法进行评价。方法：采用Agilent 1200高效液相色谱仪,色谱柱为迪马Diamonsil C₁₈柱,流动相为0.2%甲酸甲醇溶液-0.2%甲酸水溶液的梯度溶液,流速为1.0 mL·min^-1,检测波长为289 nm,柱温为25℃,进样量为10 μL。结果：测定了36份分别采用烘干、阴干、冻干进行干燥处理的4个批次的马蓝根茎叶样品。马蓝根中仅能够检测出色胺酮。马蓝茎中能够同时检测出靛蓝、靛玉红、色胺酮。马蓝叶中能够同时检测出靛蓝、靛玉红、色胺酮、异鼠李素。3种不同干燥方法中,冻干法分别处理的马蓝茎、叶中靛蓝含量相对最高。3种不同干燥方法分别处理的马蓝茎、叶中靛玉红含量基本一致。阴干法分别处理的马蓝根、茎、叶中色胺酮含量相对最高。烘干法、冻干法分别处理的马蓝叶中异鼠李素含量基本一致,但阴干法处理的未检测到异鼠李素。结论：本方法操作简便快捷、精密准确、灵敏度高,重现性好,适用于马蓝不同部位药材的质量控制。马蓝根、茎、叶的干燥方法应根据其药用部位以及活性成分进行适当选择。     

A new saponin from the leaves and stems of Panax quinquefolium L. collected in Canada

A new dammarane-type saponin named quinquenoside L3 (1) together with vina-ginsenoside R3 (2) were isolated from the leaves and stems of Panax quinquefolium L. collected in Canada. On the basis of physicochemical and spectral evidences, 1 was established as 3-O-β-D-glucopyranosyl-20-O-[β-D-xylopyranosyl-(1 → 6)-β-D-glucopyranosyl] 20(S)-dammar-23-ene-3β, 12β,20,25-tetryol.     

博落回叶与小果博落回叶中4种生物碱的含量比较

目的比较博落回叶与小果博落回叶中4种生物碱含量的差异。方法 采用反相高效液相色谱法对博落回叶与小果博落回叶中4种生物碱———原阿片碱、别隐品碱、血根碱、白屈菜红碱的含量进行比较研究。结果在博落回叶中原阿片碱、别隐品碱、血根碱、白屈菜红碱的含量分别为0.48%～2.00%、0.36%～1.72%、0.18%～0.81%、0.07%～0.33%,小果博落回叶中分别为0.01%～0.13%、0.07%～0.48%、0.24%～0.75%、0.35%～1.24%。结论博落回叶中原阿片碱与别隐品碱含量较高;小果博落回叶中血根碱与白屈菜红碱含量较高。     

Effects of bisphenol A-related diphenylalkanes on vitellogenin production in male carp (Cyprinus carpio) hepatocytes and aromatase (CYP19) activity in human H295R adrenocortical carcinoma cells

The present study investigated the effects of the known xenoestrogen bisphenol A (BPA) relative to eight BPA-related diphenylalkanes on estrogen receptor (ER)-mediated vitellogenin (vtg) production in hepatocytes from male carp (Cyprinus carpio), and on aromatase (CYP19) activity in the human adrenocortical H295R carcinoma cell line. Of the eight diphenylalkanes, only 4,4'-(hexafluoropropylidene)diphenol (BHF) and 2,2'-bis(4-hydroxy-3-methylphenyl)propane (BPRO) induced vtg, i.e., to a maximum of 3% to 4% (at 100 microM) compared with 8% for BPA relative to the maximum induction by 17beta-estradiol (E2, 1 microM). Bisphenol A diglycidyl ether (BADGE) was a potent antagonist of vtg production with an IC50 of 5.5 microM, virtually 100% inhibition of vtg at 20 microM, and an inhibitive (IC50) potency about one-tenth that of the known ER antagonist tamoxifen (IC50, 0.6 microM). 2,2'-Diallyl bisphenol A, 4,4'-(1,4-phenylene-diisopropylidene)bisphenol, BPRO, and BHF were much less inhibitory with IC50 concentrations of 20-70 microM, and relative potencies of 0.03 and 0.009 with tamoxifen. Bisphenol ethoxylate showed no anti-estrogenicity (up to 100 microM), and 4,4'-isopropylidene-diphenol diacetate was only antagonistic at 100 microM. When comparing the (anti)estrogenic potencies of these bisphenol A analogues/diphenylalkanes, anti-estrogenicity occurred at lower concentrations than estrogenicity. 4,4'-Isopropylidenebis(2,6-dimethylphenol) (IC50, 2.0 microM) reduced E2-induced (EC50, 100 nM) vtg production due to concentration-dependent cytotoxicity as indicated by a parallel decrease in MTT activity and vtg, whereas the remaining diphenylalkanes did not cause any cytotoxicity relative to controls. None of the diphenylalkanes (up to 100 microM) induced EROD activity indicating that concentration-dependent, CYP1A enzyme-mediated metabolism of E2, or any Ah-receptor-mediated interaction with the ER, was not a likely explanation for the observed anti-estrogenic effects. At concentrations as great as 100 microM, none of the diphenylalkanes directly inhibited aromatase (CYP19) activity in H295R cells. Environmental exposure of fish to BPA and related diphenylalkanes, depending on the structure, may pose anti-estrogenic, and to a lesser extent estrogenic, risks to development and reproduction.     

Physicochemical,Pharmacokinetic and Cytotoxicity of the Compounds Isolated from an Endophyte Fusarium oxysporum: In Vitro and In Silico Approaches

The present study was intended to characterize the secondary metabolites of the endophyte Fusarium oxysporum isolated from the plant Aglaonema hookerianum Schott. And to investigate the cytotoxic and other pharmacological properties of the isolated compounds as part of the drug discovery and development process. Different chromatographic techniques were adopted to isolate the bioactive compounds that were identified by spectroscopic techniques. The cytotoxic properties of the compounds were assessed in the Vero cell line via the trypan blue method. Moreover, physicochemical, pharmacokinetic, bioactivity and toxicity profiles of the compounds were also investigated through in silico approaches. After careful spectral analysis, the isolated compounds were identified as 3β,5α-dihydroxy-ergosta-7,22-dien-6-one (1), 3β,5α,9α-trihydroxy-ergosta-7,22-dien-6-one (2), p-hydroxybenzaldehyde (3), 3-(R)-7-butyl-6,8-dihydroxy-3-pent-11-enylisochroman-1-one (4) and beauvericin (5). An in vitro study in the Vero cell line revealed that the presence of the compounds reduced the number of cells, as well as the percentage of viable cells, in most cases. An in silico cytotoxic analysis revealed that compounds 1, 2 and 5 might be explored as cytotoxic agents. Moreover, compounds 3 and 4 were found to be highly mutagenic. The present study suggested that further thorough investigations are necessary to use these molecules as leads for the cytotoxic drug development process.     

Phytochemical constituents and anticancer activities of Tarchonanthus camphoratus essential oils grown in Saudi Arabia

Tarchonanthus Camphoratus L. is traditionally known for its various medicinal purposes. In this study, the T. camphoratus essential oil (TCEO) was isolated via steam distillation, and its chemical constituents were determined using GC–MS. The in vitro antiproliferative effects of TCEO on A549, HepG2, MCF-7 cancer cells, and HUVEC non-tumor cells was investigated using an MTT assay. Flow cytometry analysis was conducted to evaluate cell cycle distribution using propidium iodide staining, and cell death mode using Annexin V-FITC/PI assays. The expression of some apoptosis related genes was investigated using qRT-PCR. Major constituents of TCEO included fenchol, borneol, 3-cyclohexene-1-methanol and 3-ethyl-3-methyl. Cell viability test showed that TCEO is highly effective against MCF-7 cells with IC₅₀ 12.5 µg/mL. Cell cycle arrest at the G1/S phase, and apoptosis mediation were evident in the presence of TCEO. Gene expression analysis of several pro-apoptotic and anti-apoptotic genes revealed the initiation of apoptosis in TCEO-MCF-7 cells. In conclusion, our study confirms the antiproliferative activity of the T. camphoratus essential oil.