Rodrigues Emanuelle T, Peretti Paulo, Bezerra Roberto M, Biancardi Manoel F, Sousa Francisco F O, Mendes Elizabeth P, Dutra João B R, Silveira Carla C R, Castro Carlos H, Cruz Jorddy N, Santos Cleydson B R, Santos Fernanda C A, Pinheiro Mayara T
Laboratory of Biotechnology in Natural Products, Faculty of Pharmacy, Department of Biological and Health Sciences, Federal University of Amapá, Macapá, Amapá, Brazil.
Graduate Program in Health Sciences, Department of Biological and Health Sciences, Federal University of Amapá, Macapá, Amapá, Brazil.
Evid Based Complement Alternat Med. 2023 Apr 29;2023:1278720. doi: 10.1155/2023/1278720. eCollection 2023.
(L.) R. K. Jansen, popularly known as jambu in Northern Brazil, is widely used in folk medicine and local cuisine. Its consumption in different ways reinforces the need for safety assessments. In this study, the major compounds found in the hydroethanolic extract of flowers (EHFAO) were characterized by ultra-performance liquid mass spectrometry (UHPLC-ESI-QTOF-MS/MS). The effects of oral administration of 100/mg/kg of EHFAO extract over 60 days in male spontaneously hypertensive (SHR) and Wistar (WR) rats and the ADME/Tox predictions, lipophilicity, and water solubility were accomplished for the compounds identified. Spilanthol was detected as the foremost major compound at a concentration of 97.7%, followed by 1.53% scopoletin and 0.77% d-limonene. The treatment with EHFAO did not alter the animals´ weight over the studied period. Moderate alterations were observed solely in the hepatic enzymes AST (WR = 97 UI/L and SHR = 150 UI/L < 0.05) and ALT (WR = 55 UI/L and SHR = 95 UI/L < 0.05), while no relevant histopathological alterations were found. The study confirmed the findings, as the identified compounds were considered highly bioactive orally, due to their drug similarity profiles, adequate lipid solubility, bioavailability, and pharmacokinetics. Therefore, the chronic treatment with EHFAO was found safe at the concentration of 100/mg/kg, with no interference in the blood pressure levels neither appreciable toxic effects.
（L.）R.K.詹森，在巴西北部俗称“占布”，在民间医学和当地烹饪中广泛使用。其不同的食用方式凸显了进行安全性评估的必要性。在本研究中，通过超高效液相色谱 - 电喷雾 - 四极杆飞行时间串联质谱（UHPLC - ESI - QTOF - MS/MS）对花的水乙醇提取物（EHFAO）中的主要化合物进行了表征。对雄性自发性高血压（SHR）大鼠和Wistar（WR）大鼠口服100mg/kg的EHFAO提取物60天的效果以及对所鉴定化合物的ADME/Tox预测、亲脂性和水溶性进行了研究。检测到最高含量的主要化合物是毛叶冬珊瑚碱，浓度为97.7%，其次是1.53%的东莨菪素和0.77%的d - 柠檬烯。在研究期间，EHFAO处理并未改变动物的体重。仅观察到肝脏酶AST（WR = 97 UI/L，SHR = 150 UI/L，P < 0.05）和ALT（WR = 55 UI/L，SHR = 95 UI/L，P < 0.05）有中度变化，而未发现相关的组织病理学改变。该研究证实了这些发现，因为所鉴定的化合物因其药物相似性特征、适当的脂溶性、生物利用度和药代动力学，被认为口服具有高生物活性。因此，发现以100mg/kg的浓度长期使用EHFAO是安全的，对血压水平无干扰且无明显毒性作用。
