Mathew Nisha, Misra-Bhattacharya Shailja, Perumal Vanamail, Muthuswamy Kalyanasundaram
Vector Control Research Centre (ICMR), Indira Nagar, Pondicherry-605006, India.
Molecules. 2008 Sep 11;13(9):2156-68. doi: 10.3390/molecules13092156.
Lymphatic filariasis is caused by infection with the parasitic filarial nematodes Wuchereria bancrofti, Brugia malayi and B. timori, transmitted by mosquitoes. The lack of an adulticidal drug poses a challenge to filariasis elimination, hence it is essential to develop an effective antifilarial drug which could either kill or permanently sterilize the adult worms. In the reported work the in vitro activity of a methanolic extract of fruits of Trachyspermum ammi (Apiaceae) against adult bovine filarial Setaria digitata worms has been investigated. A bioassay-guided fractionation was carried out by subjecting the crude extract to flash chromatography. HPLC analysis was done for the crude extract and active fraction. The crude extract and the active fraction showed significant activity against the adult S. digitata by both a worm motility and MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] reduction assays. The isolated active principle was chemically characterized by IR, (1)H-NMR and MS analysis and identified as a phenolic monoterpene. It was screened for in vivo antifilarial activity against the human filarial worm B. malayi in Mastomys coucha, showing macrofilaricidal activity and female worm sterility in vivo against B. malayi. The findings thus provide a new lead for development of a macrofilaricidal drug from natural products.
淋巴丝虫病由寄生性丝虫线虫班氏吴策线虫、马来布鲁线虫和帝汶布鲁线虫感染引起，通过蚊子传播。缺乏杀成虫药物对丝虫病消除构成挑战，因此开发一种能杀死或永久使成虫绝育的有效抗丝虫药物至关重要。在报道的这项研究中，已对阿魏（伞形科）果实的甲醇提取物针对成年牛丝状线虫指状腹腔丝虫的体外活性进行了研究。通过对粗提物进行快速柱色谱法进行生物测定指导的分级分离。对粗提物和活性级分进行了高效液相色谱分析。通过蠕虫运动性和MTT [3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐]还原试验，粗提物和活性级分对成年指状腹腔丝虫均显示出显著活性。通过红外光谱、(1)H-核磁共振和质谱分析对分离出的活性成分进行化学表征，并鉴定为一种酚类单萜。在多乳鼠中对其针对人类丝虫马来布鲁线虫的体内抗丝虫活性进行了筛选，结果显示其在体内对马来布鲁线虫具有杀成虫活性和使雌虫绝育的作用。因此，这些发现为从天然产物开发杀成虫药物提供了新的线索。
