Sibiya Happiness P, Mabandla Musa V, Musabayane Cephas T
School of Laboratory Medicine and Medical Sciences, University of KwaZulu-Natal, Durban, South Africa.
PLoS One. 2016 Dec 1;11(12):e0167132. doi: 10.1371/journal.pone.0167132. eCollection 2016.
The present study investigated the effects of transdermally delivered oleanolic acid (OA) monotherapy and in combination with chloroquine (CHQ) on malaria parasites and glucose homeostasis of P. berghei-infected male Sprague-Dawley rats. Oral glucose test (OGT) responses to OA-pectin patch and CHQ-OA combination matrix patch were monitored in non-infected and infected rats. To evaluate the short-term effects of treatment, percentage parasitaemia, blood glucose, glycogen and plasma insulin were monitored in separate groups of animals treated with either OA-patch monotherapy or CHQ-OA combination pectin patch over a 21-days period. Animals treated with drug-free pectin and CHQ acted as untreated and treated positive controls, respectively. Infected control rats exhibited significantly increased parasitaemia which was accompanied by hypoglycaemia. Both OA monotherapy and CHQ-OA combination therapy reduced and cleared the malaria parasites within a period of 4 and 3 days, respectively. Compared to respective controls groups, OGT responses of animals treated with OA monotherapy or CHQ-OA combination therapy exhibited lower blood glucose levels at all time points. A once-off transdermal application of OA-patch or CHQ-OA combination patch significantly improved blood glucose concentrations inducing any changes in insulin concentration. Transdermal OA used as a monotherapy or in combination with CHQ is able to clear and reduce the malaria parasites within a shorter period of time without eliciting any adverse effects on glucose homeostasis of P. berghei-infected rats.
本研究调查了经皮递送齐墩果酸(OA)单药治疗以及与氯喹(CHQ)联合使用对感染伯氏疟原虫的雄性Sprague-Dawley大鼠体内疟原虫和葡萄糖稳态的影响。在未感染和感染的大鼠中监测了对OA-果胶贴剂和CHQ-OA联合基质贴剂的口服葡萄糖测试(OGT)反应。为了评估治疗的短期效果,在21天的时间内,对分别用OA贴剂单药治疗或CHQ-OA联合果胶贴剂治疗的不同组动物监测了疟原虫血症百分比、血糖、糖原和血浆胰岛素。用不含药物的果胶和CHQ治疗的动物分别作为未治疗和治疗的阳性对照。感染的对照大鼠疟原虫血症显著增加,并伴有低血糖。OA单药治疗和CHQ-OA联合治疗分别在4天和3天内减少并清除了疟原虫。与各自的对照组相比,接受OA单药治疗或CHQ-OA联合治疗的动物的OGT反应在所有时间点的血糖水平都较低。一次性经皮应用OA贴剂或CHQ-OA联合贴剂可显著改善血糖浓度,且不会引起胰岛素浓度的任何变化。经皮使用OA单药治疗或与CHQ联合使用能够在较短时间内清除和减少疟原虫,且不会对感染伯氏疟原虫的大鼠的葡萄糖稳态产生任何不利影响。