Sesquiterpenoids from Atractylodes macrocephala act as farnesoid X receptor and progesterone receptor modulators

Two sesquiterpenoids, atractylenolide II and III, were isolated and identified from Atractylodes macrocephala (Asteraceae) to be subsequently evaluated for their activity against farnesoid X receptor (FXR) and progesterone receptor (PR) by transient transfection reporter assays. These sesquiterpenoids did not exert significant agonistic effect but antagonized the activity of chenodeoxycholic acid (CDCA), an endogenous FXR agonist, for FXR driven SHP promoter transactivation. Additionally, they transactivated CYP7A1 gene promoter activity by antagonizing FXR. Apart from acting as a FXR antagonist, atractylenolide III also showed agonistic activity against PR. All these results demonstrated that atractylenolide II and III are the active components of Atractylodes macrocephala to exert specific pharmacologic effects.     

Establishment of the model of white blood cell membrane chromatography and screening of antagonizing TLR_4 receptor component from Atractylodes macrocephala Koidz

Inflammation is a common and fundamental patho- physiological response. The inflammatory reaction is characterized by activation of white blood cell (WBC) with an accompanying vascular reaction. Recently, it has been found that the inflammatory reaction d…     

10种中草药提取物体外抗铜绿假单胞菌作用研究

通过对粗糠柴等10种中草药采用80%乙醇室温下浸渍制备的提取物进行体外抗铜绿假单胞菌及其耐药菌活性研究,并采取药敏纸片法测定临床分离菌株的耐药性。结果表明:这10种中草药80%乙醇提取物中,粗糠柴的乙酸乙酯层对铜绿假单胞菌标准菌及其耐药菌的抑菌效果最好,其抑菌圈直径范围在10~17 mm之间,MIC范围在0.125~0.5 mg·mL~(-1)之间,MBC范围在0.5~1 mg·mL~(-1)之间;正丁醇层、水层的抑菌活性较乙酸乙酯层弱,石油醚层对铜绿假单胞菌没有效果。而小叶藤黄、滇南红厚壳、续随子的乙酸乙酯层,巴豆、罗汉松、肉桂醇提物对铜绿假单胞菌及其耐药菌株有较弱抗菌活性;滇南红厚壳的正丁醇层、续随子乙酸乙酯层以及大八角和郁金的醇提物对铜绿假单胞菌及其耐药菌株均无活性。从这些数据中可以得出,粗糠柴的乙酸乙酯层、正丁醇层和水层对铜绿假单胞菌及其耐药菌有较好的抑菌活性,尤以乙酸乙酯层活性最好,而粗糠柴的石油醚层没有活性。     

18种中草药提取物对褐飞虱和甜菜夜蛾的杀虫活性分析

为了筛选对农产品和环境安全、对害虫高效的植物源杀虫剂,分别采用喷雾法和饲毒法,测定了18种中草药的3种溶剂（水、乙醇、石油醚）提取物对褐飞虱Nilaparvata lugens Stål的触杀活性和对甜菜夜蛾Spodoptera exigua Hübner的胃毒作用。结果表明,各种提取物（0.8 g/mL）对甜菜夜蛾的胃毒作用不明显,校正死亡率最高为33.33%;但对褐飞虱的杀虫活性较高,其中百部、黄柏、榧子、生山栀、鹤虱、木香的乙醇或石油醚提取物,对褐飞虱3龄若虫的24 h校正死亡率均在80%以上,其石油乙醚提取物的LC50值依次为：0.0826,0.0455,0.0145,0.0047,0.0038,0.0033 g/mL。采用系统溶剂法分析发现,木香和鹤虱的主要杀虫活性成分均在氯仿萃取物中,表明其杀虫成分易溶于较弱极性溶剂中。进一步通过活性追踪法,对鹤虱提取物的柱层析各流分的活性检测表明,其杀虫活性成分的Rf值为0.5556~0.5926。该研究为进一步纯化新型植物源杀虫物质并确定其分子结构,从而开发其应用前景及发现新的杀虫活性先导化合物奠定了基础。     

Quantitative determination of atractylenolide III in rat plasma by liquid chromatography electrospray ionization mass spectrometry

Atractylenolide III is a major active component in Atractylodes macrocephala. This paper describes a simple, rapid, specific and sensitive method for the quantification of atractylenolide III in rat plasma using a liquid-liquid extraction procedure followed by liquid chromatography mass spectrometric (LC-MS) analysis. A Kromasil 3.5 microm C(18) column (150 mm x 2.00 mm) was used as the analytical column. Linear detection responses were obtained for atractylenolide III concentration ranging from 5 to 500 ng L(-1). The precision and accuracy data, based on intra-day and inter-day variations over 5 days were within 10.29%. The lower limit of quantitation for atractylenolide III was 5 ng mL(-1), using 0.1 mL plasma for extraction and its recoveries were greater than 85% at the low, medium and high concentrations. The method has been successfully applied to a pharmacokinetic study in rats after an oral administration of atractylenolide III with a dose of 20.0 mg kg(-1). With the lower limits of quantification at 5 ng mL(-1) for atractylenolide III, this method was proved to be sensitive enough for the pharmacokinetics study of atractylenolide III.     

七星瓢虫成虫石油醚提取物的化学成分及抑菌活性

【目的】确定七星瓢虫Coccinella septempunctata成虫石油醚提取物的化学成分及其抑菌活性。【方法】用甲醇室温提取, 石油醚、 乙酸乙酯和正丁醇梯度萃取, 利用气相色谱-质谱连用仪（Gas Chromatograph-Mass Spectrometer, GC-MS）对七星瓢虫成虫石油醚提取物成分进行分析, 通过硅胶、 凝胶Sephadex LH-20、 ODS-C₁₈柱层析法对正丁醇提取部分的成分进行分离, 采用质谱和核磁共振等手段鉴定结构。采用纸片扩散法对七星瓢虫成虫石油醚提取物的抑菌活性进行测试。【结果】经GC-MS联用技术从石油醚相中鉴定出14个化合物, 从正丁醇相中分离鉴定了7个化合物。石油醚提取物对肠道沙门氏菌Salmonella enterica有抑制作用, 在浓度为100和50 mg/mL时, 抑菌率分别为52.78%和27.05%, 在该浓度下对绿脓杆菌Pseudomonas aeruginosa、 玉米大斑病菌Exserohilum turcicum和水稻纹枯病菌Rhizoctonia solani没有表现出明显的抑制作用。【结论】七星瓢虫C. septempunctata成虫石油醚提取物对肠道沙门氏菌具有抑制作用。     

Anxiolytic effects of Equisetum arvense Linn. extracts in mice

The petroleum ether (PE), chloroform (CH), ethanol (ETH) and water extracts of E. arvense stems were evaluated for anti-anxiety activity in mice using elevated plus maze model. Ketamine induced hypnosis and actophotometer was used to evaluate sedative effect with various extracts in mice. The results were compared with standard drug diazepam. The ethanolic extract of E. arvense (50 and 100 mg/kg) significantly increased the time-spent and the percentage of the open arm entries in the elevated plus-maze model which was comparable to diazepam. Ethanolic extract (100 mg/kg) prolonged the ketamine-induced total sleeping time and decreased the locomotor activity in mice. The results suggest that the ethanolic extract of E. arvense seems to possess anxiolytic effect with lower sedative activity than that of diazepam. The results could be attributed to the flavonoid content of the ethanolic extract.     

苦槛蓝提取物对小菜蛾的生物活性

以干扰作用控制指数(IIPC)为评价指标,小菜蛾为试虫,分别对苦槛蓝茎叶的不同溶剂提取物进行了生物活性测定,结果表明,石油醚和氯仿萃取部分具有较强的生物活性,而乙酸乙酯和乙醇萃取部分活性较低．在0．01gDW·ml^-1时,用石油醚和氯仿萃取物对小菜蛾处理1d后的产卵忌避率(ODR)分别为84．69％、79．90％,3d后为76．47％、45．70％,IIPC为0．1565和0．2055．在0．05gDW·ml^-1·L^-1时,1d后为88．52％和72．25％,3d后为87．33％和58．37％,IIPC为0．1125和0．2620．进而对氯仿部分进行了柱层析分离,并鉴定了3种黄酮类化合物,它们分别是5,7-二羟基黄烷酮(Ⅰ)、5,7-二羟基黄酮醇(Ⅱ)、3,4′-二甲氧基-5,7-二羟基黄酮醇(Ⅲ),其中Ⅱ在生测中表现出较好的活性。     

Acaricidal activity of Juglans regia leaf extracts on Tetranychus viennensis and Tetranychus cinnabarinus (Acari: Tetranychidae)

Leaf extracts of the walnut, Juglans regia L., were evaluated under laboratory conditions to determine their acaricidal activity on the mites Tetranychus cinnabarinus (Boisduval) and Tetranychus viennensis Zacher (Acari: Tetranychidae). Extracts had both contact and systemic toxicity to these mites. The four solvents tested for preparing crude extracts were petroleum ether, chloroform, ethyl acetate, and methanol. Methanol was the most efficient solvent, with an extraction rate from 17.06 + 0.80 to 20.27 +/- 0.28%. Petroleum ether was the least effective solvent, with extraction rates from 2.30 +/- 0.13 to 2.71 +/- 0.13%. However, the crude extracts with petroleum ether resulted in the highest mite mortality (79.04 +/- 0.52%) in a slide dip bioassay. Mites mortalities from the concentrated extracts prepared by chloroform, ethyl acetate, methanol, or distilled water were significantly lower than petroleum ether. The mean lethal concentrations (LC50) of the extracts from petroleum ether, chloroform, ethyl acetate, methanol, and distilled water to the two mite species were 0.73 +/- 0.04, 1.66 +/- 0.28, 4.96 +/- 0.35, 7.45 +/- 0.67, and 9.91 +/- 0.32 mg/ml, respectively. After liquid chromatography and thin-layer chromatography, the concentrated extracts of petroleum ether were separated into eight fractions and tested for acaricidal activity. Fraction 6 produced significantly higher mite mortality rates than the other groups, killing approximately 90% of both species.     

Macrocyclic diarylheptanoids from Garuga pinnata

Three macrocyclic diarylheptanoids, 6'-hydroxygaruganin V (1), 9'-desmethylgarugamblin I (2) and 1,9'-didesmethylgaruganin III (3) were isolated from the petroleum ether and dichloromethane extracts of the stem bark of Garuga pinnata. The structures of these compounds were established by extensive spectroscopic studies, including high field NMR and MS measurements.     

乳孔硫磺菌的化学成分和抗氧化活性

对乳孔硫磺菌子实体不同极性提取物进行了DPPH和ABTS自由基清除能力的测定,并对氯仿和乙酸乙酯提取物进行了分离纯化。结果表明,乳孔硫磺菌的石油醚、氯仿、乙酸乙酯和甲醇提取物均有一定的抗氧化活性,各提取物对两种自由基的清除能力均表现为甲醇提取物＞乙酸乙酯提取物＞氯仿提取物＞石油醚提取物,甲醇提取物对DPPH自由基的清除率最高可达到93.78%;对ABTS自由基的清除率最高可达到62.06%;从氯仿和乙酸乙酯提取物中分离得到10个化合物,分别是：(22E,24R)-5α,8α-过氧麦角甾-6,22-二烯-3β-醇（1）,阿里红酸 A（2）,麦角甾-7,22-二烯-3β-醇（3）,啤酒甾醇（4）,硫色多孔菌酸（5）,(4E,8E)-N-d-2′-hydroxypalmitoyl-1-O-β-d-glycopyranosyl- 9-methyl-4,8-sphingadienine（6）,麦角甾醇（7）,N-(2′-羟基二十四碳酰基)-1,3,4-三羟基-2-氨基-十八烷（8）,烟酸（9）和齿孔酸（10）。其中,化合物2、6、8和9为首次从硫磺菌属真菌中分离得到。     

土荆芥提取物对玉米象的触杀与熏蒸活性

测定了土荆芥(Chenopodium ambrosioidesL.)4种溶剂(100%乙醇、丙酮、乙酸乙酯和石油醚)提取物对玉米象Sitophilusz eamais Motschulsky的触杀和,蒸活性。4种溶剂提取物在6.494mg/cm2浓度下对玉米象的触杀效果:48h后100%乙醇提取物和石油醚提取物的校正死亡率均达100%;丙酮提取物次之,为92.31%;乙酸乙酯提取物最低,为64.10%,但72h后达94.17%。4种溶剂提取物对玉米象的,蒸活性:72h后0.50mg/mL浓度处理下校正死亡率为98.73%～100%。     

Isolation and Identification of Atractylenolide lV from Atractylodes macrocephala Koidz.

Nine compounds have been isolated from the rhizomes of Atractylodes macrocephala Koidz. One of them is a new compound, named atractylenolide Ⅳ. Sitosterol and triterpenoid ester were also isolated firstly in this genus.     

六种藜科植物提取物对植物病原菌的抑制活性

研究了角果藜（ Ceratocarpus arenarius）、盐穗木（ Halostachys caspica）、里海盐爪爪（ Kalidium caspicum） 、叉毛蓬（ Petrosimonia sibirica ）、盐角草（ Salicornia europaea ）和小叶碱蓬 （ Suaeda microphylla ）等六种新疆藜科植物提取物及其不同极性萃取部分对根癌土壤杆菌（Agrobacterium tumefaciens ）、黄瓜角斑病菌（P Pseudomonas lachrymarts）、番茄疮痂病菌（ Xanthomonas vesicatoria ） 等植物病原细菌以及杨树溃疡病菌（ Botryosphaeria dothidea ）、棉花枯萎病菌（Fusarium oxysporum f. sp. vasinfectum ）、稻纹枯病菌（Rhizoctonia solani）等病原真菌的抑制活性。结果显示角果藜、叉毛蓬和盐角草乙醇粗提物表现出一定抗细菌活性,其中以叉毛蓬和盐角草提取物对黄瓜角斑病菌的抑制活性最强。多数植物提取物及其不同极性萃取部分对杨树溃疡病菌表现出强的抑制活性。抗真菌活性成分主要存在于供试植物的石油醚、氯仿和正丁醇萃取部分中,提示活性成分为极性中等的化合物。角果藜和盐角草乙醇粗提物及其不同极性萃取部分对供试真菌有较好的抑制活性。     

山野木层孔菌子实体中抑制H22荷瘤小鼠肿瘤的活性成分研究

采用梯度提取法对山野木层孔菌子实体进行提取,得到石油醚层、甲醇层及水层3 种提取物及石油醚层中获得化合物4,6,8(14),22(23)-四烯-3-酮-麦角甾烷,并采用H22 荷瘤小鼠进行体内抗肿瘤活性研究,以抑瘤率、免疫器官指数、免疫因子为指标检测抗肿瘤活性。结果表明,石油醚高剂量组（100mg/kg）、单体化合物中剂量组（7.5mg/kg）抑制率分别为62.21%、57.67%;脾指数、胸腺指数均高于对照组和环磷酰胺（CTX）组,白介素-2（IL-2）的含量明显高于对照组和环磷酰胺（CTX）组（P＜0.01）;肿瘤坏死因子-α（TNF-α）含量明显低于对照组（P＜0.01）。因此认为上述石油醚提取物和单体化合物对H22荷瘤小鼠肿瘤有抑制作用,并且均能改善小鼠的免疫功能。     

Immunostimulatory effect of Tinospora cordifolia Miers leaf extract in Oreochromis mossambicus

Immunostimulatory effect of leaf extract of T. cordifolia on (i) specific immunity (antibody response), (ii) non-specific immunity (neutrophil activity) and (iii) disease resistance against Aeromonas hydrophila was investigated in O. mossambicus. Ethanol and petroleum ether extracts of the leaves were used. Both ethanol and petroleum ether extracts administered at doses of 0.8, 8 or 80 mg/kg body weight, prolonged the peak primary antibody titres upto one to three weeks. Ethanol extract at the dose of 8 mg/kg and petroleum ether extract at the doses of 0.8 or 8 mg/kg enhanced the secondary antibody response. All the doses of ethanol extract significantly enhanced neutrophil activity. Fish injected with petroleum ether or ethanol extract at a dose of 8 mg/kg were protected against experimental infection with virulent A. hydrophila. The results indicates the potential of T. cordifolia leaf extracts for use as an immunoprophylactic to prevent diseases in finfish aquaculture.     

Identification, isolation and characterization of the antifeedant constituent of Clausena anisata against Helicoverpa armigera (Lepidoptera: Noctuidae)

Abstract  Hexane, petroleum ether, chloroform, ethyl acetate, methanol and water extracts of Clausena anisata [(Willd.) Hook F. Ex Benth] leaves and roots were evaluated against Helicoverpa armigera (Hübner) for antifeedant activities. Antifeedant activity was confirmed, and was found to be higher in root extracts than those of the leaf. Chloroform and petroleum ether extracts of the root showed strongest antifeedant activities (DC₅₀s [concentration (C) causing 50% deterrence compared with the control] 0.014% and 0.016% respectively), and root extracts were fractionated using silica gel column chromatography. One fraction of the chloroform and one of the petroleum ether root extracts was active; and on the basis of mass spectroscopy and ¹H and ¹³C nuclear magnetic resonance spectral data, the active compounds in the two fractions were confirmed to be identical, and identified as osthol [2H-1-Benzopyran-2-one, 7-methoxy-8-(3-methyl-2-butenyl)]. The highest concentration of osthol was found in the chloroform root extract. Antifeedant activities of the root extracts, as measured by DC₅₀ values, were highly correlated with their osthol contents. Approximately 99% of the variation in bioactivity of the root extracts could be accounted for by variation in osthol content; osthol therefore, appeared to be an antifeedant component of C . anisata to H. armigera . This may provide a new approach to managing this pest.     

Antifungal activity of crude extracts and fat-soluble constituents of Holotrichia diomphalia larvae

In this study, chemical compositions of fatty oils and bioactivity of crude extracts from Holotrichia diomphalia larvae as Chinese materia medica were investigated for the first time. The chemical compositions of the fatty oils were obtained by two different methods and determined by GC/MS. In total, the petroleum ether extract produced 21 compounds (96.3%) while the supercritical fluid extract produced six compounds (99.53%) for identification. The effect of petroleum ether and other crude extracts on Pyricularia oryzae was also examined. Results indicated that ethanol and petroleum ether extracts had excellent antifungal activities. These findings demonstrated that fatty oils from H. diomphalia larvae had great potential to be used as a source for natural health products.     

Bio-insecticidal activities of halophytic plant extracts against Tribolium confusum (Coleoptera, Tenebrionidae)

Salt marsh plants were tested for their insecticidal activities against larvae of the confused flour beetle Tribolium confusum (Tenebrionidae). 16 aerial part extracts were obtained using organic solvents of increasing polarity and tested for their anti-feedant and toxicity effects. Responses varied with plant material and extract type. Ethyl acetate extracts of F. laevis, S. echioides and. T. boveana and petroleum ether extract of F. laevis presented, anti-feedant property. However, S. fructicosa seemed to be attractive to the tested flour beetle. Mortalities of 97, 87, 97 and 80% were observed by using respectively ethyl acetate extracts of F. laevis, S. echioides and T. boveana and petroleum ether extract of F. laevis, when applied at a dose of 1%, mixed with the insect diet. This preliminary study showed that F. laevis, S. echioides and T. boveana presented potential bio-insecticidal activity with ethyl acetate extracts, similar result was found with petroleum ether extract of F. laevis. More complementary studies are needed for the use of these extracts to control T. confusum.     

Potential of natural phenolic antioxidant compounds from Bersama abyssinica (Meliathacea) for treatment of chronic diseases

Chronic diseases including cardiovascular, diabetes and cancer persist for a long time in the course of treatment affecting health and are currently the cause of many deaths. In most cases, the treatment of chronic infectious diseases especially Tuberculosis relies on conventional drugs which are currently becoming fruitless due to drug resistance and unpredicted complications in course of treatment. However, herbal medicines have for a long time been used in prevention and treatment of chronic diseases including asthma and heart diseases in Africa. In this study, we extracted metabolites and screened for active compounds with potential free radical scavenging and pharmacological activities from Bersama abyssinica, the plant commonly used in traditional medicine in Tanzania. B. abyssinica root, stembark and leaf were air dried, sequentially extracted in various solvents including petroleum ether, dichloromethane, ethylacetate and methanol to yield extracts and fractions. The extracts and fractions were tested for the presence of several metabolites and antioxidant activity. The analysis of chemical compounds from resultant extracts was done by GC–MS for non-polar factions and LC-MS/MC for moderate polar extracts.High amount of phenolic acid, flavonoids and tannin were identified in ethylacetate fraction compared to ethanol, dichloromethane and petroleum ether. The GC–MS analysis of petroleum ether extract of B. abyssinica stem back yielded twelve (12) compounds with varying composition. The most abundant compounds were 2-Butenoic acid, 3-methyl-, ethyl ester comprising 33.8%, n-Hexadecanoic acid comprising 16.7% and Ethanolpentamethyl- yielded in 16.7%.The LC-MS/MS analysis of Ethyl acetate fractions yielded 20 compounds including; Mangiferin and Isoquercitin were abundant in leaves, stembark and roots. Lastly, ethyl vanillate was identified in both roots and leaves whereas Quercitrin and 7,8-Dimethoxycoumarin were found in stembark and root.These findings indicated that B. abyssinica is rich in phenolic compounds ranging from phenolic acids, flavonoids and coumarin that possess high antioxidant and pharmacological properties potential for treatment of chronic diseases.