牛蒡的化学研究进展

按照化学结构类型对牛蒡中的多种化学成分分别以木脂素、有机酸、硫炔类、挥发油以及多炔类化合物的结构特点进行分类综述，为牛蒡的研究与开发提供参考。     

杜仲木脂素化合物降压药效学研究与机制初探

目的：研究杜仲中木脂素化合物（EUL）的降血压作用并初步探讨降压机制。方法：SHR大鼠实验组分为低、中、高3个剂量组给予EUL溶液，连续给药4周，每周定时测量血压、心率和体重。100例高血压受试者随机分为2组，实验组服用EUL胶囊，对照组服用安慰剂，连续给药4周，定期测量血压。去甲肾上腺素预收缩内皮完整的离体SD大鼠胸主动脉血管环，累积加入不同浓度EUL溶液，观察舒张变化。结果：EUL高剂量与模型组相比，能降低SHR大鼠血压（P〈0．05），对大鼠体重和心率均无影响。实验组高血压患者服用EUL胶囊后，收缩压、舒张压与服用前相比显著下降（P〈0．01），与对照组相比显著降低（P〈0．01）。NE预收缩离体血管环，EUL累积浓度升高，舒张率增大。结论：EUL有一定的降压作用，作用是使血管扩张，为进一步阐明杜仲降血压机制提供参考。     

Furfuran lignans and a flavone from Artemisia gorgonum Webb and their in vitro activity against Plasmodium falciparum

The chemical composition of the aerial parts of the Cape Verdean endemic shrub Artemisia gorgonum Webb (Asteraceae) was careful investigated, which led to the isolation and identification of six known furfuran lignans: eudesmin (1), magnolin (2), epimagnolin A (3), aschantin (4), kobusin (5), sesamin (6) and a flavone: artemetin (7). Compounds 1-7 were evaluated in vitro for their cytotoxicity in a screening panel consisting of various mammalian tumor cell lines, for their antimalarial activity against chloroquine-resistant Plasmodium falciparum (FcB1 strain) and for their cytotoxicity against murine normal cells (CFU-GM). While no promising cytotoxicity against human tumor cells were noticed, marginal potency and selectivity was found for compounds 1-5 against murine colon 38. Besides, compounds 2-7 showed mild antiplasmodial activities, 6 and 7 being the most active compounds (IC(50) 3.37 and 3.50 μg/ml respectively) without noticeable toxicity on mammalian normal cells. This is the first report of antiplasmodial activity for furfuran lignans and the first isolation of 1-7 from Artemisia gorgonum.     

黄荆子乙酸乙酯提取物及木脂类化合物对人卵巢癌COC1细胞体外增殖及裸鼠皮下移植瘤的抑制作用

目的:研究黄荆子乙酸乙酯提取物EVn-50及从中分级分离获得的4种木脂类化合物(Comp 6、Comp 7、Comp 8、Comp 10)体内外对人卵巢癌COC1细胞的作用。方法:体外培养人卵巢癌COC1细胞,细胞计数法检测EVn-50、Comp 6、Comp 7、Comp 8、Comp 10对人卵巢癌COC1细胞生长的影响;采用人卵巢癌COC1细胞裸鼠移植瘤模型治疗实验评价EVn-50、Comp 6、Comp 7、Comp 8、Comp 10体内治疗卵巢癌的有效性。结果:EVn-50、Comp 6、Comp 7、Comp 8、Comp 10对人卵巢癌COC1细胞生长具有抑制作用,且呈浓度及时间依赖性,其中,以Comp 8效价最高,其IC50为1.40μg/ml;其次为EVn-50,其IC50为1.56μg/ml;体内实验显示,5mg/kg给药20天时,EVn-50、Comp 6对人卵巢癌COC1细胞裸鼠皮下移植瘤生长抑制率分别为57.1%、55.7%;瘤重抑制率分别是61.6%、53.1%,Comp 8无效。结论:黄荆子乙酸乙酯提取物EVn-50及黄荆子木脂类化合物体内外均能抑制人卵巢癌COC1细胞的生长和增殖。     

Changes in (poly)phenols intake and metabolic syndrome risk over ten years from adolescence to adulthood

Background and aims(Poly)phenols might contribute to prevent cardiovascular disease, but limited prospective studies exist among adolescents. This study aimed to evaluate within-subject longitudinal changes in (poly)phenols intakes and food group contributors while also exploring the association with metabolic syndrome risk (MetS) during 10 years of follow up in European adolescents becoming young adults.Methods and resultsIn 164 participants (58% girls, 13-18 y at baseline) from Ghent, Zaragoza and Lille, longitudinal data (2006–2016) on (poly)phenol intake was retrieved via 2 or 3 24 h recalls. Linear and logistic longitudinal regression tested the association of (poly)phenols intake (total and classes) with Mets risk or its components (waist-height-ratio, HDL cholesterol, LDL cholesterol, triglycerides, blood pressure and insulin resistance index), adjusted for age, sex, country and other nutrient intakes. The total (poly)phenols intake was 421 ± 107 mg/day (192 mg/1000 kcal/day) at baseline, while 610 ± 101 mg/day (311 mg/1000 kcal/day) at follow-up. The three major food sources for (poly)phenols were ‘chocolate’, ‘fruit and vegetable juices’, ‘cakes and biscuits’ during adolescence and ‘coffee’, ‘tea’ and ‘chocolate’ during adulthood. Phenolic acid intake was associated with less LDL increase over time, while stilbene intake with a steeper increase in triglycerides over time.ConclusionsDifferences in major (poly)phenols contributors over time were partially explained by age-specific dietary changes like increased coffee and tea during adulthood. Some significant (poly)phenols-MetS associations might argue for nutrition-based disease prevention during adolescence, especially since adolescents had low (poly)phenols intake.     

Application of coulometric electrode array detection to the analysis of isoflavonoids and lignans

A comprehensive review of the available methods for the analysis of isoflavonoids and lignans in biological matrices based on coulometric electrode array detection (CEAD) is presented. Different aspects such as sample extraction and purification procedures as well as instrumental settings and method validation are discussed. Comparisons with other available protocols using different detection techniques such as mass spectrometry or immunoassay are also reported to underline the versatility and reliability of the detector. Practical notes and tips for scientists working with CEAD are also provided.     

赶黄草木脂素及黄酮类成分抑制肝癌细胞增殖的作用

目的:研究赶黄草中木脂素类及黄酮类成分体外抑制肝癌细胞增殖的作用。方法:采用MTT法评价赶黄草中8个木脂素(1~8)和5个黄酮(9~13)体外抗人肝癌细胞SMMC-7721和Hep G2增殖的活性以及对正常肝细胞LO_2活力的影响。运用Image-i T DEAD Green/Hoechst 33342荧光双染和高内涵成像分析化合物1对SMMC-7721细胞的影响。结果:化合物1、6、8~11可抑制SMMC-7721的增殖,6、9、11、13可抑制Hep G2的增殖。除化合物11以外,以上化合物对正常肝细胞LO_2均无明显细胞毒作用,且化合物3、4、5、13还可促进LO_2增殖。结论:赶黄草中部分木脂素及黄酮类成分不仅具有抑制肝癌细胞增殖的作用,而且对正常肝细胞无毒作用,甚至可保护正常肝细胞,表现出较好的选择性。     

Chemical constituents from Qianliang tea

Ten compounds were isolated from Qianliang tea, a kind of dark tea fully fermented from the leaves of Camellia sinensis (L.) O. Kuntze var. sinensis, and identified as N-(2-hydroxyphenyl)-2-pyrrolidinone (1), p-hydroxyacetophenone (2), salicifoliol (3), (-)-3-hydroxy-β-ionone (4), p-hydroxy ethyl cinnamate (5), ethyl 4-(sulfooxy)benzoate (6), (+)-matairesinol (7), (-)-pinoresinol (8), (+)-lirioresinol-A (9), and caffeine (10), among which compound 1 was isolated as a new natural product, and compound 6 was isolated from Theaceae family for the first time. Compounds 3, 4, 5, 7, 8, and 9 were isolated from this species for the first time.     

构树叶中的细胞毒成分（英文）

目的：研究构树叶的化学成分。方法：采用D101型大孔吸附树脂、硅胶、ODS和半制备型高效液相色谱等分离方法对构树叶提取物分离纯化,通过1D,2DNMR技术确定其结构,并采用MTT法对分得化合物进行细胞毒活性测定,同时比色法和采用高效液相色谱法建立了对构树叶中总黄酮和cosmosiin的含量测定方法。结果：分离鉴定了6个化合物,它们的结构鉴定为：（＋）-pinoresinol-4′-O-β-D-glucopyransyl-4″-O-β-D-apiofuranoside（1）,cosmosiin（2）,luteolin-7-O-β-D-glucopyranoside（3）,liriodendrin（4）,3,5,4′-trihydroxy-bibenzyl-3-O-β-D-glucoside（5）,apigenin-6-C-β-D-glycopyranside（6）。结论：化合物1为一个新的木脂素,化合物5,6为首次从该属植物中分离,化合物1,4,6对HepG-2细胞株有不同程度的抑制活性,而化合物2,3,5对HepG-2细胞株没有活性;根据含量测定结果得知,确定构树叶的最佳采收时间为9月份。     

Lignoids in insects: chemical probes for the study of ecdysis, excretion and Trypanosoma cruzi-triatomine interactions.

The effects of phytochemicals (lignans and neolignans) are reviewed in a variety of insect species with special focus on the recent advances on feeding, excretion and Trypanosoma cruzi interactions with Rhodnius prolixus. Burchellin, podophyllotoxin, pinoresinol, sesamin, licarin A, and nordihydroguaiaretic acid (NDGA) added to the diet of Rhodnius prolixus larvae induce antifeedant effects only in doses up to 100 microg/ml of blood meal. Additionally, pinoresinol and NDGA significantly inhibit ecdysis (ED(50)<20 microg/ml). Simultaneous application of ecdysone (1 microg/ml) counteracts ecdysial stasis as induced by NDGA in 5th-instar larvae. Experiments in vivo demonstrate that burchellin and podophyllotoxin (100 microg/ml) diminish excretion post-feeding. Simultaneous treatment with 5-hydroxytryptamine (1 mM, 5-HT), a diuretic hormone, partially reverses this effect of burchellin. Experiments in vitro, using isolated Malpighian tubules of R. prolixus, indicate that burchellin (i) decreases diuretic hormone levels in the hemolymph but not the amount of diuretic hormone stored in the thoracic ganglionic masses (including axons); (ii) reduces the volume of urine secreted by isolated Malpighian tubules; and (iii) 5-HT therapy cannot overcome the effect of burchellin on the Malpighian tubules. In R. prolixus fed on blood containing T. cruzi epimastigotes, the number of parasites in the digestive tract decreases drastically in the presence of burchellin and NDGA (10 microg/ml). When these phytochemicals are applied 20 days after T. cruzi infection, burchellin significantly reduces the gut infection, whereas NDGA does not. However, if the insects are pretreated with both compounds 20 days before subsequent infection with epimastigotes, the parasite infection is almost completely abolished. The same holds true when 5th-instar of R. prolixus are inoculated with 0.5 microg/microl/larva of both neolignans 1 day before infection. Taken together, these findings not only provide a better understanding of the lignoid function in insects, but also offer novel insights into basic physiological processes, which make lignoids interesting candidates for new types of insecticides.