Institute of Health Sciences, University for International Integration of the Afro-Brazilian Lusophony, Acarape, 62.785-000, CE, Brazil.
Center for Research and Drug Development, Federal University of Ceará, Fortaleza, 60.430.275, CE, Brazil.
ChemMedChem. 2021 Jan 19;16(2):420-428. doi: 10.1002/cmdc.202000387. Epub 2020 Oct 23.
The tambjamines are a small group of bipyrrolic alkaloids that, collectively, display a significant range of biological activities including antitumor, antimicrobial and immunosuppressive properties. The key objective of the present study was to undertake preclinical assessments of tambjamine J (T-J) so as to determine its in vivo antitumor effects. To that end, sarcoma 180 cells were transplanted in mice and the impacts of the title compound then evaluated using a range of protocols including hematological, biochemical, histopathological, genotoxic and clastogenic assays. As a result it was established that this alkaloid has a significant therapeutic window and effectively reduces tumor growth (by 40 % and 79 % at doses of 10 and 20 mg/kg/day, respectively). In this regard it displays similar antitumor activity to the anticancer agent cyclophosphamide and alters animal weight in an analogous manner.
唐竹精胺是一类双吡咯生物碱，具有显著的生物活性，包括抗肿瘤、抗菌和免疫抑制特性。本研究的主要目的是对唐竹精胺 J（T-J）进行临床前评估，以确定其体内抗肿瘤作用。为此，将肉瘤 180 细胞移植到小鼠体内，并使用一系列方案评估标题化合物的影响，包括血液学、生化、组织病理学、遗传毒性和致裂原性测定。结果表明，该生物碱具有显著的治疗窗，能有效抑制肿瘤生长（10 和 20mg/kg/天剂量下分别减少 40%和 79%）。在这方面，它显示出与抗癌药物环磷酰胺相似的抗肿瘤活性，并以类似的方式改变动物体重。
