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西奈毛蕊花(玄参科)对刚果锥虫分离株的抗锥虫活性。

Antitrypanosomal activity of Verbascum sinaiticum Benth. (Scrophulariaceae) against Trypanosoma congolense isolates.

作者信息

Mergia Ermias, Shibeshi Workineh, Terefe Getachew, Teklehaymanot Tilahun

机构信息

Department of Pharmacology and Clinical Pharmacy, Faculty of Health Sciences, Addis Ababa University, Addis Ababa, Ethiopia.

Department of Parasitology, Faculty of Veterinary Medicine, Addis Ababa University, Addis Ababa, Ethiopia.

出版信息

BMC Complement Altern Med. 2016 Sep 15;16:362. doi: 10.1186/s12906-016-1346-z.

Abstract

BACKGROUND

African Trypanosomiasis is a neglected tropical disease with a large impact on the livelihood of the rural poor in Sub-Saharan Africa. The available drugs for managing this disease are old, expensive and are facing the problem of drug resistance. Thus, the aim of this study was to evaluate in vivo antitrypanosomal efficacy of aqueous and absolute methanol leaf extracts of Verbascum sinaiticum Benth. against Trypanosoma congolense field isolate.

METHODS

Verbascum sinaiticum (Local name 'qetetina') is a biennial plant, and 60-150 cm tall. It is traditionally used to treat wound, stomachache, viral infection, cancer, sunstroke, fever, abdominal colic, diarrhea, hemorrhage, anthrax, and hepatitis. The efficacy of aqueous and absolute methanol leaf extracts of V. sinaiticum was evaluated in a randomized experiment with Swiss albino mice infected with T. congolense field isolate. The extracts were administered at doses of 100, 200 and 400 mg/kg by intraperitoneal injection for seven days at 12 Days Post-Infection (DPI) when the peak parasitaemia level was approximately 10(8) trypanosomes/ml. Parasitaemia, Packed Cell Volume (PCV), mean survival time and change in body weight were used as indices for monitoring the efficacy of the extracts. Diminazene (28 mg/kg) was used as a positive control while 2 % Tween was used as the negative control. Phytochemicals screening were conducted following standard methods.

RESULTS

The extracts showed no toxicity effect in Swiss albino mice and had LD50 above 2000 mg/kg. The phytochemicals screened in V. sinaiticum were alkaloids, flavonoids, glycoside, saponins, steroids, phenolic compounds, and tannins. The mice treated with absolute methanol leaf extract of V. sinaiticum at 400 mg/kg dose had significantly lower mean parasitaemia (7.20 ± 0.16) (p < 0.001) as compared to the negative control group (8.82 ± 0.12) on day 14 of treatment. Animals treated with the same dose had significant (p < 0.001) higher PCV value and body weight and as well as the highest mean survival time of 40.20 ± 0.31 days as compared to the negative control at the end of the observation period.

CONCLUSION

This study established that Verbascum sinaiticum had trypanocidal activity. The crude extracts have partially eliminated trypanosomes in a dose-dependent manner. The study can be a basis for future in-depth analysis of the biologically active chemicals.

摘要

背景

非洲锥虫病是一种被忽视的热带疾病,对撒哈拉以南非洲农村贫困人口的生计有重大影响。现有的治疗该疾病的药物陈旧、昂贵且面临耐药性问题。因此,本研究的目的是评估西奈毛蕊花(Verbascum sinaiticum Benth.)水提物和无水甲醇叶提取物对刚果锥虫野外分离株的体内抗锥虫效果。

方法

西奈毛蕊花(当地名称“qetetina”)是一种两年生植物,高60 - 150厘米。传统上用于治疗伤口、胃痛、病毒感染、癌症、中暑、发烧、腹部绞痛、腹泻、出血、炭疽和肝炎。在一项随机实验中,对感染刚果锥虫野外分离株的瑞士白化小鼠评估了西奈毛蕊花水提物和无水甲醇叶提取物的疗效。在感染后12天(dpi),当寄生虫血症峰值水平约为10⁸锥虫/毫升时,通过腹腔注射以100、200和400毫克/千克的剂量给药提取物,持续7天。寄生虫血症、红细胞压积(PCV)、平均存活时间和体重变化被用作监测提取物疗效的指标。二脒那秦(28毫克/千克)用作阳性对照,2%吐温用作阴性对照。按照标准方法进行植物化学物质筛选。

结果

提取物在瑞士白化小鼠中未显示毒性作用,半数致死量(LD50)高于2000毫克/千克。在西奈毛蕊花中筛选出的植物化学物质有生物碱、黄酮类、糖苷、皂苷、甾体、酚类化合物和单宁。在治疗第14天,与阴性对照组(8.82±0.12)相比,用400毫克/千克剂量的西奈毛蕊花无水甲醇叶提取物处理的小鼠平均寄生虫血症显著更低(7.20±0.16)(p < 0.001)。在观察期结束时,用相同剂量处理的动物红细胞压积值和体重显著更高(p < 0.001),并且平均存活时间最长,为40.20±0.31天。

结论

本研究证实西奈毛蕊花具有杀锥虫活性。粗提取物以剂量依赖的方式部分清除了锥虫。该研究可为未来对生物活性化学物质的深入分析奠定基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1571/5024474/bdc8d16ced2e/12906_2016_1346_Fig1_HTML.jpg

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