Ferreira Paulo Michel Pinheiro, Bezerra Daniel Pereira, Silva Jurandy do Nascimento, da Costa Marcília Pinheiro, Ferreira José Roberto de Oliveira, Alencar Nylane Maria Nunes, Figueiredo Ingrid Samantha Tavares de, Cavalheiro Alberto José, Machado Camila Maria Longo, Chammas Roger, Alves Ana Paula Negreiros Nunes, Moraes Manoel Odorico de, Pessoa Claudia
Laboratory in Experimental Cancerology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina, Brazil; Postgraduate Program in Pharmaceutical Sciences, Federal University of Piauí, Teresina, Brazil; Postgraduate Program in Biotechnology, Federal University of Piauí, Teresina, Brazil.
Oswaldo Cruz Foundation, Salvador, Brazil.
J Ethnopharmacol. 2016 Jun 20;186:270-279. doi: 10.1016/j.jep.2016.04.011. Epub 2016 Apr 8.
Casearia sylvestris (Salicaceae) is found in South America and presents antiulcerogenic, cytotoxic, antimicrobial, anti-inflammatory and antihypertensive activities.
To assess the in vivo and ex vivo antitumor action of a fraction with casearins (FC) and its main component - Casearin X-isolated from C. sylvestris leaves.
Firstly, Sarcoma 180 bearing Swiss mice were treated with FC and Cas X for 7 days. Secondly, BALB/c nude animals received hollow fibers with colon carcinoma (HCT-116) or glioblastoma (SF-295) cells and were treated with FC for 4 days. On 5th day, proliferation was determined by MTT assay.
FC 10 and 25mg/kg/day i.p. and 50mg/kg/day oral and Cas X 25mg/kg/day i.p. and 50mg/kg/day oral revealed tumor growth inhibition rates of 35.8, 86.2, 53.7, 90.0 and 65.5% and such tumors demonstrated rare mitoses and coagulation necrosis areas. Similarly, FC reduced multiplying of HCT-116 and SF-295 cells when evaluated by the Hollow Fiber Assay (2.5 and 5mg/kg/day i.p. and 25 and 50mg/kg/day oral), with cell growth inhibition rates ranging from 33.3 to 67.4% (p<0.05). Flow cytometry experiments revealed that FC reduced membrane integrity and induced DNA fragmentation and mitochondrial depolarization (p<0.05).
FC and Cas X were efficient antitumor substances against murine and human cancer cells and caused reversible morphological changes in liver, kidneys and spleens, emphasizing clerodane diterpenes as an emerging class of anticancer molecules.
南美鼠李（鼠李科）分布于南美洲，具有抗溃疡、细胞毒性、抗菌、抗炎和抗高血压活性。
评估从南美鼠李叶中分离得到的含酪蛋白的馏分（FC）及其主要成分——酪蛋白X的体内和体外抗肿瘤作用。
首先，用FC和酪蛋白X对荷肉瘤180的瑞士小鼠进行7天治疗。其次，BALB/c裸鼠接受植入结肠癌（HCT-116）或胶质母细胞瘤（SF-295）细胞的中空纤维，并接受FC治疗4天。在第5天，通过MTT法测定细胞增殖。
腹腔注射FC 10和25mg/kg/天以及口服50mg/kg/天，以及腹腔注射酪蛋白X 25mg/kg/天和口服50mg/kg/天，肿瘤生长抑制率分别为35.8%、86.2%、53.7%、90.0%和65.5%，这些肿瘤显示出罕见的有丝分裂和凝固性坏死区域。同样，通过中空纤维试验评估（腹腔注射2.5和5mg/kg/天以及口服25和50mg/kg/天），FC可减少HCT-116和SF-295细胞的增殖，细胞生长抑制率在33.3%至67.4%之间（p<0.05）。流式细胞术实验表明，FC降低了膜完整性，诱导了DNA片段化和线粒体去极化（p<0.05）。
FC和酪蛋白X是针对鼠类和人类癌细胞的有效抗肿瘤物质，并在肝脏、肾脏和脾脏中引起可逆的形态学变化，强调克罗烷二萜作为一类新兴的抗癌分子。
