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恩氏樟茎皮生物碱提取物及其配制软膏的体外和体内抗菌评价

In vitro and in vivo antimicrobial evaluation of alkaloidal extracts of Enantia chlorantha stem bark and their formulated ointments.

作者信息

Nyong Emmanuel E, Odeniyi Michael A, Moody Jones O

出版信息

Acta Pol Pharm. 2015 Jan-Feb;72(1):147-52.

PMID:25850210
Abstract

The in vitro and in vivo antimicrobial evaluation of the formulated ointment of alkaloidal extract of Enantia chlorantha Oliv. (Annonaceae) was the concern of this study. The alkaloidal fraction of the stem bark extract was formulated into simple ointment using British Pharmacopoeia formula for preparation of simple ointment. Agar diffusion and agar dilution methods were used for the in vitro antimicrobial studies. Ketoconazole 4000 μg/mL and tioconazole cream 1% were used as reference standards while normal saline was used as control. The fungicidal activity kinetics of the plant extract was carried out using selected concentrations of the plant extract against the most sensitive organism (Candida albicans). For the in vivo studies, 25 albino rats weighing between 180-200 g were divided into 5 groups, anesthesized (thiopental sodium 50 mg/kg), infected with overnight culture of Candida albicans and incubated at 37 degrees C for three days to allow for growth of the microorganisms. Each of the five groups was treated on the third day of incubation with different concentrations of the formulated simple ointment (200 mg/mL, 100 mg/kg, 50 mg/mL), tioconazole cream 1% (reference standard) and normal saline control, respectively. The alkaloidal extract exhibited greater zones of inhibition with Candida glabrata and Trichophyton tonsurans while Candida albicans and Trichophyton interdigitali also showed some sensitivity. There was no surviving organism at the end of 240 min at 100 mg/mL concentration with 10(-4) dilution factor. Treatment of the infected rats with the formulated simple ointments (200, 100 and 50 mg/mL) showed that 50 mg/mL ointment had a better percentage reduction in the fungal loads at the end of the experiment when compared with the 200 mg/mL simple ointment as well as the standard tioconazole 1% cream and normal saline treated rats, respectively. The alkaloidal fraction of Enantia chlorantha stem bark as well as the formulated ointment exhibited significant in vitro and in vivo antifungal activities against different species of Candida, dermatophytes and plant fungi.

摘要

本研究关注的是对Enantia chlorantha Oliv.(番荔枝科)生物碱提取物制成的软膏进行体外和体内抗菌评估。采用英国药典中制备简单软膏的配方,将茎皮提取物的生物碱部分制成简单软膏。体外抗菌研究采用琼脂扩散法和琼脂稀释法。酮康唑4000μg/mL和1%的噻康唑乳膏用作参考标准,生理盐水用作对照。使用选定浓度的植物提取物对最敏感的生物体(白色念珠菌)进行植物提取物的杀菌活性动力学研究。在体内研究中,将25只体重在180 - 200g之间的白化大鼠分为5组,麻醉(硫喷妥钠50mg/kg),接种白色念珠菌过夜培养物,并在37℃下孵育三天以促进微生物生长。在孵育的第三天,分别用不同浓度的制成的简单软膏(200mg/mL、100mg/kg、50mg/mL)、1%的噻康唑乳膏(参考标准)和生理盐水对照处理这五组大鼠。生物碱提取物对光滑念珠菌和断发癣菌表现出更大的抑菌圈,而白色念珠菌和指间毛癣菌也表现出一定的敏感性。在100mg/mL浓度、10(-4)稀释因子下,240分钟结束时没有存活的生物体。用制成的简单软膏(200、100和50mg/mL)处理感染的大鼠表明,与200mg/mL简单软膏以及标准的1%噻康唑乳膏和生理盐水处理的大鼠相比,50mg/mL软膏在实验结束时真菌载量的降低百分比更好。Enantia chlorantha茎皮的生物碱部分以及制成的软膏对不同种类的念珠菌、皮肤癣菌和植物真菌均表现出显著的体外和体内抗真菌活性。

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