Ali Saqib, Alamzeb Muhammad, Igoli John, Clements Carol, Shah Syed Qaiser, Ferro Valerie A, Gray Alexander Irvine, Khan Muhammad Rafiullah
Phytopharmaceutical and Nutraceutical Research Laboratories (PNRL), Institute of Chemical Sciences, University of Peshawar , Peshawar , Pakistan .
Pharm Biol. 2014 Aug;52(8):983-7. doi: 10.3109/13880209.2013.874534. Epub 2014 Mar 6.
Trypanosoma brucei brucei (T.b. brucei) infection causes death in cattle, while the current treatments have serious toxicity problems. However, natural products can be used to overcome the problems associated with parasitic diseases including T.b. brucei.
Artemisia elegantissima Pamp (Asteraceae) was evaluated phytochemically for its constituents and antitrypanosomal potential against T.b. brucei for the first time. Scopoletin isolated from A. elegantissima has shown better potential then the standard drug suramin, used against T.b. brucei.
The ethanol extract of the aerial parts of A. elegantissima was fractionated by column and preparative thin-layer chromatography into six fractions (A-F) yielding 13 compounds, these were evaluated for their antitrypanosomal activity against T.b. brucei at different concentrations.
Thirteen compounds were isolated from A. elegantissima: (Z)-p-hydroxy cinnamic acid, stigmasterol, β-sitosterol, betulinic acid, bis-dracunculin, dracunculin, scopoletin, apigenin, dihydroluteolin, scoparol, nepetin, bonanzin, and 3',4'-dihydroxy bonanzin. The fractions D-F were found to be active at the concentration of 20 µg/ml and three compounds isolated from these fractions, scopoletin (MIC ≤0.19 µg/ml), 3',4'-dihydroxy bonanzin (MIC = 6.25 µg/ml) and bonanzin (MIC = 20 µg/ml), were found to be highly active.
Artemisia elegantissima was phytochemically and biologically explored for its antitrypanosomal potential against T.b. brucei. The number and orientation of phenolic hydroxyl groups play an important role in the antitrypanosomal potential of coumarins and flavonoids. The compounds 3',4'-dihydroxy bonanzin and scopoletin with low MIC values, hold potential for use as antitrypanosomal drug leads.
布氏布氏锥虫（T.b. brucei）感染会导致牛死亡，而目前的治疗方法存在严重的毒性问题。然而，天然产物可用于克服与包括布氏布氏锥虫在内的寄生虫病相关的问题。
首次对优雅蒿（菊科）进行植物化学评估，以确定其成分及对布氏布氏锥虫的抗锥虫潜力。从优雅蒿中分离出的东莨菪素已显示出比用于对抗布氏布氏锥虫的标准药物苏拉明更好的潜力。
将优雅蒿地上部分的乙醇提取物通过柱色谱和制备薄层色谱法分离成六个馏分（A - F），得到13种化合物，评估它们在不同浓度下对布氏布氏锥虫的抗锥虫活性。
从优雅蒿中分离出13种化合物：（Z）-对羟基肉桂酸、豆甾醇、β-谷甾醇、桦木酸、双蛇床素、蛇床素、东莨菪素、芹菜素、二氢木犀草素、滨蒿内酯、尼泊尔黄酮素、波南辛和3',4'-二羟基波南辛。发现馏分D - F在20μg/ml浓度下具有活性，从这些馏分中分离出的三种化合物，即东莨菪素（MIC≤0.19μg/ml）、3',4'-二羟基波南辛（MIC = 6.25μg/ml）和波南辛（MIC = 20μg/ml），被发现具有高活性。
对优雅蒿进行了植物化学和生物学研究，以确定其对布氏布氏锥虫的抗锥虫潜力。酚羟基的数量和取向在香豆素和黄酮类化合物的抗锥虫潜力中起重要作用。MIC值较低的化合物3',4'-二羟基波南辛和东莨菪素具有作为抗锥虫药物先导物的潜力。
