芹菜甲素和乙素的抗惊厥作用

1-芹菜甲素(1-3-丁基苯酞)和1-芹菜乙素(1-3-丁基-4,5二氢苯酞)是从芹菜籽分离出的抗惊厥有效成分。在小于TD₅₀剂量下,对最大电休克(MES),最小电休克(MET),戊四唑(MST)和原发听源性惊厥(MAS)等四种动物模型有效,可认为有广泛的抗惊作用。其人工合成的dl-芹菜甲素(dl-3-丁基苯酞)更有抗惊作用强,毒性小和便于推广应用的优点。     

中药地锦草芹菜素糖苷类化合物

为了研究中药地锦草抗HBV的活性物质基础,采用大孔树脂、Sephadex LH-20、MCI GEL CHP 20P等色谱方法,从地锦草70%乙醇提取物中分离得到5个芹菜素苷类化合物,通过MS、NMR、2D-NMR等波谱分析手段鉴定了化合物的结构,分别为：芹菜素-7-O-(6"-O-没食子酰)-β-D-葡萄糖苷 (1),芹菜素-7-O-β-D-芹糖(1→2)-β-D-葡萄糖苷 (2),芹菜素-7-O-β-D-芦丁糖苷 (3),芹菜素-7-O-β-D-葡萄糖苷 (4),芹菜素 (5)。化合物1为新化合物,化合物2、3为首次从该植物中分得。
     

半制备高效液相色谱法同时分离制备肉桂中5种苯丙素类化合物及其免疫抑制活性考察

摘 要 目的：建立一种从肉桂中同时分离5种苯丙素类化合物的制备分析方法,并对化合物的免疫抑制活性进行了评价。方法: 肉桂经乙醇提取后,取乙酸乙酯部位经高效液相色谱仪分离制备化合物,制备色谱条件：采用Ultimate XB-C₁₈（250 mm×10 mm,5 μm）半制备柱,流动相为乙腈 水,进行梯度洗脱,检测波长为330 nm,柱温为30℃,流速为2.5 ml·min^-1,进样量为0.3 ml。采用MS及NMR对化合物进行结构鉴定。采用CCK-8法对分离出的化合物进行免疫抑制活性考察。结果: 同时分离得到5种苯丙素类化合物,分别为赤式 愈创木甘油、(7R,8S)-syringoylglycerol、(7S,8S) syringoylglycerol、3-甲氧基苯基 丙烯醛、邻甲氧基肉桂醛。CCK-8法证明化合物3在浓度800 μmol·L^-1时对T细胞及B细胞的抑制率均大于20%,有一定免疫抑制作用。结论:苯丙素分离方法简便,分离效果好,能同时制备肉桂中5种苯丙素类化合物,其中化合物3有一定的免疫抑制活性。     

HPLC同时测定小蓟配方颗粒中蒙花苷和芹菜素的含量

目的 建立HPLC同时测定小蓟配方颗粒中蒙花苷和芹菜素含量的方法。方法 采用Diamonsil-C₁₈（4.6 mm×250 mm,5 μm）色谱柱,以乙腈-1%冰醋酸水溶液为流动相进行梯度洗脱,流速：1.0 ml·min^-1,检测波长：335 nm,柱温：30℃。结果 蒙花苷和芹菜素进样量分别在0.3~1.5 μg（r=0.999 4）和0.075~0.375 μg（r=0.999 7）内与峰面积呈良好的线性关系;加样回收率分别为99.19%和99.12%,RSD分别为1.27%和1.26%。结论 该方法操作简便,重复性好,可用于小蓟配方颗粒中蒙花苷和芹菜素的含量测定。     

芫花主要黄酮成分对肝微粒体UGTs及UGT1A1活性的体外抑制作用

目的 考察芫花主要黄酮成分芫花素和芹菜素对尿苷二磷酸葡萄糖醛酸转移酶（UGTs）及UGT1A1活性的影响。方法 采用体外肝微粒体孵育模型,以4-硝基酚（4-nitrophenol,4-NP）为底物检测UGTs活性,胆红素为底物检测UGT1A1活性;利用UV及UPLC-MS/MS测定底物或代谢产物的含量。结果 对UGTs,在大鼠肝微粒体、小鼠肝微粒体以及人肝微粒体孵育体系中,芫花素和芹菜素均能不同程度地抑制UTGs活性;抑制强弱顺序：在大鼠肝微粒体温孵体系中,芫花素>芹菜素;在小鼠肝微粒体以及人肝微粒体温孵体系中,芹菜素>芫花素。对UGT1A1,在人肝微粒体孵育体系中,芫花素和芹菜素均表现为中等强度的竞争性抑制作用,抑制强弱顺序：芹菜素（IC₅₀=12.40 μmol·L^-1）>芫花素（IC₅₀=23.21 μmol·L^-1）。结论 芫花素和芹菜素对不同肝微粒体孵育体系中UGTs及UGT1A1均可产生显著抑制作用且存在种属差异。芫花素及芹菜素可能存在基于UGT酶的药物相互作用。     

HPLC同时测定不同产地密蒙花中4种化合物的含量

目的 采用HPLC同时测定密蒙花中4种化合物（毛蕊花糖苷、蒙花苷、芹菜素、木犀草素）的含量,并对不同产地的密蒙花进行比较。方法 采用Waters Sunfire^TM C₁₈色谱柱（4.6 mm×250 mm,5μm）,以乙腈-0.2%磷酸水溶液为流动相,梯度洗脱;流速1.0 mL·min^-1;柱温30℃;检测波长330 nm（毛蕊花糖苷、蒙花苷、芹菜素）和350 nm（木犀草素）。结果 4种化合物在各自的范围内呈现良好的线性关系（r>0.999 0）,平均回收率为97.75%~98.49%,RSD为0.7%~1.5%。测得不同产地毛蕊花糖苷、蒙花苷、芹菜素、木犀草素的含量分别为21.046 3~42.886 3,8.514 4~17.400 8,0.317 3~1.205 3,0.030 4~0.145 6 mg·g^-1。结论 该法稳定可靠,重复性好,可为密蒙花质量评价提供一定依据。     

铁箍散化学成分的研究

目的：研究土家族药用植物铁箍散Schisandra propinqua var. sinensis根茎的化学成分。方法：采用硅胶柱色谱、凝胶柱色谱、制备高效液相色谱等方法分离化合物,根据理化性质和波谱解析鉴定各化合物的结构。结果：从铁箍散中分离鉴定了2个倍半萜（化合物1、2）和4个木脂素（化合物3～6）,分别为泽泻醇（alismol,1）、匙叶桉油烯醇（ent-spathulenol,2）、五味子酯I（schisantherin I,3）、五味子酯F（schisantherin F,4）、propinquanin A（5）、propinquanin D（6）。结论：化合物1～4为首次从该植物中分离得到。     

半枝莲黄酮类化学成分分析

目的 分析半枝莲黄酮类化学成分。方法 采用硅胶、Sephadex LH-20等多种色谱方法,依据波谱数据对其结构进行分析和鉴定。结果 半枝莲中共分离了12个化合物,分别为圣草酚、野黄芩素、三裂鼠尾草素、黄芩苷、芹菜素、汉黄芩素、4''-羟基汉黄芩素、木犀草素、4'',5-二羟基-3'',5'',6,7-四甲氧基黄酮、柚皮素、7-羟基-5,8,2''-三甲氧基黄烷酮、大波斯菊苷。结论 分离得到的化合物类型均为黄酮苷元和苷类化合物,可为半枝莲的黄酮成分分析提供一定的科学依据。     

芹菜素对百草枯致小鼠肺纤维化保护作用及机制研究

目的 研究芹菜素对百草枯致小鼠肺纤维化的保护作用及机制。方法 将小鼠随机分为对照组、模型组、地塞米松组（1 mg/kg）和芹菜素低、高剂量（10、20 mg/kg）组,除对照组外,其他各组ip百草枯（50 mg/kg）建立小鼠肺纤维化模型,第8天开始ig给药,连续给药21 d。观察小鼠体质量变化;测量小鼠肺系数;采用HE染色观察肺组织形态学变化;免疫组化法观察小鼠肺组织中Ⅰ、Ⅲ型胶原表达变化;ELISA法检测各组小鼠肺组织中Ⅰ、Ⅲ型胶原和炎症因子肿瘤坏死因子（TNF）-α、白细胞介素（IL）-6、IL-1β含量;Western blotting法测定肺组织Caveolin-1蛋白表达水平。结果 造模第28天时,与模型组比较,芹菜素低、高剂量组小鼠体质量显著增加（P<0.05）;地塞米松组和芹菜素低、高剂量组肺系数显著降低（P<0.05）;芹菜素低、高剂量组肺组织内炎性细胞浸润较少、肺泡壁断裂及肺泡腔融合较少,肺纤维化程度较轻;芹菜素低、高剂量组和地塞米松组小鼠的肺组织中Ⅰ、Ⅲ型胶原和IL-6、IL-1β、TNF-α含量显著下降（P<0.01）,Caveolin-1蛋白表达显著下降（P<0.01）。结论 芹菜素对百草枯诱导小鼠肺纤维化具有保护作用,其机制可能与Ⅰ、Ⅲ型胶原含量及炎症因子水平下调、Caveolin-1蛋白表达水平下调相关。     

短叶决明子的化学成分研究

摘 要 目的：研究豆科决明属植物短叶决明子的化学成分。 方法: 采用柱色谱、薄层色谱以及重结晶分离纯化短叶决明子的醇提物,并通过理化鉴别与波谱解析进行结构鉴定。 结果: 从短叶决明子分离得到7个化合物,经鉴定为1 去甲甲基钝叶决明素（Ⅰ）、橙钝叶决明素（Ⅱ）、芦荟大黄素（Ⅲ）、钝叶决明素（Ⅳ）、甲基钝叶决明素（Ⅴ）、美决明子素（Ⅵ）、橙黄决明素（Ⅶ）。 结论:所有化合物均为首次从短叶决明子中分离得到。     

药用植物芸香与对叶大戟比较鉴别研究

目的： 用传统的鉴别方法对芸香及其替代品对叶大戟进行比较分析,为芸香的初步鉴定提供参考依据。方法： 采用性状比较、显微观察和TLC等方法进行鉴定。TLC选用甲苯-乙酸乙酯-水（10：4：3）为展开剂,以5%氯化铝乙醇溶液为显色剂,置紫外光灯（365 nm）下检视。结果： 芸香与对叶大戟的外观性状在茎、叶、果等部位均有差异,显微特征明显,TLC色谱斑点清晰。结论： 本方法直观、简便,可为芸香药材的后续研究提供参考和支撑。     

Constituents from Apium graveolens and their anti-inflammatory effects

A phthalide glycoside, (3R, 4R)-4-O-β-D-glucopyranosyl-senkyunolide (1), and a megastigmane glycoside, (6S, 7R)-3-oxo-megastigma-4, 8-dien-7-O-β-D-glucoside (2), along with two known aglycones (3–4), were isolated from the 70% EtOH extract of fresh whole grass of Apium graveolens L. Their structures were elucidated by extensive spectroscopic analysis. All of these compounds were tested for their inhibitory effects on nitric oxide (NO) production in the RAW 264.7 macrophages. Among them, compounds 3 and 4 showed potent inhibitory activity against LPS-induced nitric oxide production in RAW 264.7 macrophages, with IC₅₀ values of 24.0 ± 2.1 μM and 28.6 ± 2.4 μM, respectively.     

Botanical origin of Indian celery seed (fruit)

In the course of our study on the traditional medicines and foodstuffs used in Pakistan, we investigated the origin of Indian celery by using the analysis of the internal transcribed spacer (ITS) sequence of nuclear rDNA and a phytochemical approach. We found that the source plant of the Indian celery containing coumarin derivatives such as seselin (1), bergapten (2) and isopimpinellin (3) was not common celery, Apium graveolens. Our results suggest the source plant is Seseli diffusum even though Indian workers reported that A. graveolens seeds contain the aforementioned compounds. In addition, a market survey of the Indian celery in Pakistan and related countries revealed that the Indian celery seeds in Pakistani markets are mainly composed of three species which have been confused in rural markets. Electronic supplementary material  The online version of this article (doi:) contains supplementary material, which is available to authorized users.

Combinatorial anti-<Emphasis Type="Italic">Trichophyton</Emphasis> effects of <Emphasis Type="Italic">Ligusticum chuanxiong</Emphasis> essential oil components with antibiotics

The antifungal activities of ligustilide and butylidene phthalide, which are major oil components comprising the essential oil of Ligusticum chuanxiong, in combination with antifungal drugs were evaluated. Checkerboard microtiter and microdilution tests were used to measure combined effects against Trichophyton species, T. erinacei, T. mentagrophytes, T. rubrum, T. schoenleinii, T. tonsurans and T. soudanense. Susceptibility of these Trichophyton species to L. chuanxiong essential oil differed distinctly. The fractional inhibitory concentrations (FICIs) against Trichophyton species ranged between 0.27 and 0.56 for ketoconazole combined with ligustilde or butylidene phthalide, indicating synergism or additive effects between the antibiotic and essential oil compounds. Testing by itraconazole instead of ketoconazole, similar combination effects were observed with FICIs from 0.31 to 0.63 against the tested strains of T. mentagrophytes, T. rubrum, T. schoenleinii, and T. soudanense. Thus, data reported here showed that Trichophyton susceptibility to ketoconazole and itraconazole could be notably improved by ligustilde and butylidene phthalide.     

One new ergostane-type steroid and three new phthalide derivatives from cultures of the basidiomycete Albatrellus confluens

One new ergostane-type steroid, (12β,15β,22R,23S,24S)-22,25-epoxy-12,15,23-trihydroxyergost-4,6,8(14)-trien-3-one (1), three new phthalide derivatives, 5-(2′,3′-epoxy-3′,3′-dimethylpropoxy)-7-methoxy-6-methylphthalide (2), (2′)-(Z)-5-(3′-hydroxymethyl-3′-methylallyloxy)-7-methoxy-6-methylphthalide (3), and 5-(3′,3′-dimethylallyloxy)-7-hydroxy-6-methylphthalide (4), along with one known phthalide derivative, 5-(3′,3′-dimethylallyloxy)-7-methoxy-6-methylphthalide (5), were isolated from cultures of the basidiomycete Albatrellus confluens. The structures of the new compounds were established on the basis of extensive spectroscopic data (IR, MS, 1D, and 2D NMR) analyses. All compounds were evaluated for their cytotoxic activities on five tumor cell lines.     

Pharmacological evaluation of the anxiolytic-like effects of Lippia graveolens and bioactive compounds

Context: Lippia species (Verbenaceae) are widely used in Latin America and Africa as folk medicine for their tranquilizing properties.

Objective: To evaluate the anxiolytic-like effects and safety of Lippia graveolens Kunth. by exploring its aqueous and organic leaf extracts and identifying the responsible chemical constituents.

Material and methods: Aqueous and organic extracts (hexane, ethyl acetate and methanol) were pharmacologically evaluated at several doses. Chemical constituents were identified using MS, NMR and GC-MS analysis. The isolated compounds (3?mg/kg, i.p.), extracts (1, 3, 10 and 30?mg/kg, i.p.), and the reference drug diazepam (0.1?mg/kg, i.p.) were assessed in CD-1 mice using experimental behavioural models: open-field, cylinder, hole-board, plus-maze and sodium pentobarbital-induced hypnosis, as well as their acute toxicity (LD₅₀).

Results: After administration of the extracts and bioactive compounds, a significant anxiolytic-like response from 1?mg/kg, i.p. was observed, resembling the effect of diazepam. Major presence of thymol (33.40%) was observed in the hexane extract; whereas for the first time in this species a p-cymene?+?thymol mixture (9.78%), naringenin (0.18%) and cirsimaritin (1.16%) were obtained as bioactive constituents of the ethyl acetate crude extract. Acute toxicity was calculated to be LD₅₀ =?1000?mg/kg for the crude hexane extract, lower in comparison to the other extracts analyzed (LD₅₀ >?2000?mg/kg).

Discussion and conclusion: Our results suggest that L. graveolens exerts anxiolytic-like activity involving many kinds of constituents, mainly of the terpenoid and flavonoid nature. These results reinforce the potential use of this species in the therapy of anxiety.     

New dimeric phthalides from Ligusticum sinense Oliv cv. Chaxiong

A new dimeric phthalide, chaxiongnolide A (1), and a new natural product, chaxiongnolide B (2), together with a known compound Z-ligustilide (3), were isolated from the rhizome of Ligusticum sinense Oliv cv. Chaxiong. Their structures were elucidated by various spectroscopic methods and confirmed by X-ray crystallographic analysis.     

基于代谢组学和网络药理学分析福建金线莲叶和台湾银线兰叶治疗肝纤维化作用差异

目的 初步分析福建金线莲(Anoectochilus roxburghii)和台湾银线兰(Anoectochilus formosanus)的叶片在治疗肝纤维化疾病的作用机制差异，为分析两者的临床疗效差异及其资源的精准利用提供参考信息。方法 利用代谢组学技术分析福建金线莲叶(the leaves of A.roxburghii，Arl)和台湾银线兰叶(the leaves of A.formosanus，Afl)的差异代谢物；并结合网络药理学方法分析其差异代谢物治疗肝纤维化疾病的作用差异。结果 利用代谢组学的方法分析初步得到Arl和Afl的46个差异代谢物，主要为黄酮类、糖苷类和甘油磷脂类等，其中有23种差异化合物具有潜在药用活性。基于网络药理学的方法，预测了23种差异化合物的759个相关靶点，与肝纤维化疾病的相关靶点进行映射，得到交集靶点249个，其中AKT1、STAT3、VEGFA等48个关键靶点被预测为治疗肝纤维化的主要差异靶点；作用靶点较多的关键差异化合物为Arl相比Afl含量较高的化合物，预示Arl中富含更多可以用于治疗肝纤维化的有效化合物。GO富集功能和KEGG富集分析表明，福建金线莲与台湾银线兰的差异成分参与治疗肝纤维化疾病的信号通路有所不同，VEGF信号通路为Arl相比Afl含量较高的差异化合物的主要差异信号通路，磷脂酰肌酶3-激酶-蛋白激酶B(PI3K-Akt)信号通路为Arl相比Afl含量较低的差异化合物治疗肝纤维化疾病的主要差异信号通路。分子对接结果表明各差异成分与其对应的关键靶点均有较好的结合活性。结论 本研究表明福建金线莲与台湾银线兰叶片中存在一些差异代谢物，预测了其治疗肝纤维化疾病作用机制差异，并初步验证了其作用靶点，为金线莲资源的精准利用具有指导性意义。     

Prenylated xanthones from <Emphasis Type="Italic">Hypericum ascyron</Emphasis>

Three new prenylated xanthones, 1,3,5-trihydroxy-6,7-[2′-(1-methylethenyl)-dihydrofurano]-xanthone (1), 1,3,5-trihydroxy-6,7-[2′-(1-hydroxy-1-methylethyl)-dihydrofurano]-xanthone (2), and 1,3,5-trihydroxy-6-O-prenyl-xanthone (3), together with eight known compounds were isolated from the leaves of Hypericum ascyron. Compound 3 has an O-prenyl moiety, and therefore represents the first reported xanthone to have an O-prenyl moiety from genus Hypericum. The structures of the isolated compounds were established based on spectroscopic data and on a comparison with values for previously identified analogues.     

6-甲氧基正丁苯酞在大鼠肝微粒体中的代谢研究

报道了用GC/MS方法及衍生化技术研究6-甲氧基正丁苯酞(MBP)在大鼠肝微粒体中的代谢转化结果。6-甲氧基正丁苯酞在苯巴比妥(PB)诱导的大鼠肝微粒体中主要转化为3-羟基、γ-羟基取代物,6-羟基正丁苯酞与一个环氧化代谢产物。