Faculty of Health Sciences, Federal University of Grande Dourados, Dourados, MS, Brazil.
Department of Plant Biology, PPG BTPB, and PPG BCE, Institute of Biology, University of Campinas (UNICAMP), Campinas, São Paulo, Brazil.
Inflammopharmacology. 2021 Apr;29(2):439-450. doi: 10.1007/s10787-020-00752-0. Epub 2020 Sep 10.
Information on the health benefits of ethanolic extracts obtained from Blutaparon portulacoides stem (EEBP) hasn´t been consistently described in the literature until the present moment. This study investigated the antimycobacterial, anti-inflammatory and toxicological effects of EEBP in models of inflammation/infection, as well as its chemical composition. Chemical analysis of EEBP by electrospray ionization-mass spectrometry/HPLC-MS/MS identified 3,5,3'-Trihydroxy-4'-methoxy-6,7-methylenedioxy-flavone, gomphrenol, ferulic, vanillic, and caffeic acids. The minimum inhibitory concentration of EEBP and isoniazid in the presence of Mycobacterium tuberculosis was 123.4 and 0.030 µg/ml, respectively. EEBP oral administration (p.o.) (300-1000 mg/kg) or dexamethasone subcutaneous injection (s.c.) (1 mg/kg) significantly inhibited leukocytes and proteins resulting from carrageenan-induced pleurisy in Swiss mice. In the BCG-induced pleurisy model, the oral treatments performed once a day for 7 days, with EEBP (30 and 100 mg/kg) and isoniazid (25 mg/kg), inhibited the increase in plasmatic IL-1β levels and in pleural exudate from C57BL-6 mice, and reduced M. tuberculosis growth in organs (colony forming units assays). EEBP (30-300 mg/kg, p.o.) and dexamethasone (1 mg/s.c.) significantly prevented carrageenan-induced oedema and mechanical hyperalgesia in Swiss mice. The treatments (once a day for 22 days) with EEBP (30 mg/kg, p.o.) and dexamethasone (1 mg/s.c.) substantially inhibited oedema and mechanical- and cold-hyperalgesia at 11, 16 and 22 days after the administration of Freund's Complete Adjuvant in C57bL6 mice. No evidence of physio-pathologic was observed in Wistar rats acutely treated with EEBP (2000 mg/kg, p.o.). This study confirms the anti-inflammatory and antibiotic properties of EEBP, opening possibilities for the development of safe new drugs with dual anti-inflammatory/antimycobacterial activities which could be favorable from a pharmacoeconomic perspective.
目前为止,关于龙舌兰属植物茎乙醇提取物(EEBP)对健康的益处的信息在文献中并没有得到一致的描述。本研究调查了 EEBP 在炎症/感染模型中的抗分枝杆菌、抗炎和毒理学作用,以及其化学组成。通过电喷雾电离-质谱/高效液相色谱-质谱/质谱对 EEBP 的化学分析鉴定出 3,5,3'-三羟基-4'-甲氧基-6,7-亚甲二氧基黄酮、荭草苷、阿魏酸、香草酸和咖啡酸。EEBP 和异烟肼对结核分枝杆菌的最小抑菌浓度分别为 123.4 和 0.030 µg/ml。EEBP 口服(p.o.)(300-1000 mg/kg)或地塞米松皮下注射(s.c.)(1 mg/kg)显著抑制了白细胞和蛋白质的渗出,这是由卡拉胶诱导的瑞士小鼠胸膜炎引起的。在卡介苗诱导的胸膜炎模型中,每天口服治疗一次,连续 7 天,用 EEBP(30 和 100 mg/kg)和异烟肼(25 mg/kg),可抑制 C57BL-6 小鼠血浆 IL-1β 水平和胸膜渗出物的增加,并减少分枝杆菌在器官中的生长(集落形成单位测定)。EEBP(30-300 mg/kg,p.o.)和地塞米松(1 mg/s.c.)显著预防了卡拉胶诱导的瑞士小鼠水肿和机械性痛觉过敏。EEBP(30 mg/kg,p.o.)和地塞米松(1 mg/s.c.)的治疗(每天一次,共 22 天)在 C57BL6 小鼠给予弗氏完全佐剂后第 11、16 和 22 天,显著抑制了水肿和机械性及冷性痛觉过敏。在急性给予 EEBP(2000 mg/kg,p.o.)的 Wistar 大鼠中未观察到生理病理变化。本研究证实了 EEBP 的抗炎和抗生素特性,为开发具有双重抗炎/抗分枝杆菌活性的安全新药提供了可能,从药物经济学的角度来看,这可能是有利的。