西地球花（唇形科）油及其主要成分小茴香酮的毒性和抗肿瘤潜力
Toxicity and antitumor potential of Mesosphaerum sidifolium (Lamiaceae) oil and fenchone, its major component.
作者信息
Rolim Thaísa Leite, Meireles Déborah Ribeiro Pessoa, Batista Tatianne Mota, de Sousa Tatyanna Kelvia Gomes, Mangueira Vivianne Mendes, de Abrantes Renata Albuquerque, Pita João Carlos Lima Rodrigues, Xavier Aline Lira, Costa Vicente Carlos Oliveira, Batista Leônia Maria, da Silva Marcelo Sobral, Sobral Marianna Vieira
机构信息
Programa de Pós-graduação em Produtos Naturais e Sintéticos Bioativos, Centro de Ciências da Saúde, Universidade Federal da Paraíba, João Pessoa, Paraíba, 58051-970, Brazil.
Departamento de Ciências Farmacêuticas, Universidade Federal da Paraíba, João Pessoa, Paraíba, 58051-970, Brazil.
出版信息
BMC Complement Altern Med. 2017 Jul 3;17(1):347. doi: 10.1186/s12906-017-1779-z.
BACKGROUND
The essential oil from Mesosphaerum sidifolium (L'Hérit.) Harley & J.F.B.Pastore (syn. Hyptis umbrosa), Lamiaceae (EOM), and its major component, have been tested for toxicity and antitumor activity.
METHODS
EOM was obtained from aerial parts of M. sidifolium subjected to hydro distillation, and gas chromatography-mass spectrometry was used to characterize the EOM chemical composition. The toxicity was evaluated using haemolysis assay, and acute toxicity and micronucleus tests. Ehrlich ascites carcinoma model was used to evaluate the in vivo antitumor activity and toxicity of EOM (50, 100 and 150 mg/kg), and fenchone (30 and 60 mg/kg) after 9 d of treatment.
RESULTS
The EOM major components were fenchone (24.8%), cubebol (6.9%), limonene (5.4%), spathulenol (4.5%), β-caryophyllene (4.6%) and α-cadinol (4.7%). The HC50 (concentration producing 50% haemolysis) was 494.9 μg/mL for EOM and higher than 3000 μg/mL for fenchone. The LD50 for EOM was approximately 500 mg/kg in mice. The essential oil induced increase of micronucleated erythrocytes only at 300 mg/kg, suggesting moderate genotoxicity. EOM (100 or 150 mg/kg) and fenchone (60 mg/kg) reduced all analyzed parameters (tumor volume and mass, and total viable cancer cells). Survival also increased for the treated animals with EOM and fenchone. For EOM 150 mg/kg and 5-FU treatment, most cells were arrested in the G0/G1 phase, whereas for fenchone, cells arrested in the S phase, which represents a blockage in cell cycle progression. Regarding the toxicological evaluation, EOM induced weight loss, but did not induce hematological, biochemical or histological (liver and kidneys) toxicity. Fenchone induced decrease of AST and ALT, suggesting liver damage.
CONCLUSIONS
The data showed EOM caused in vivo cell growth inhibition on Ehrlich ascites carcinoma model by inducing cell cycle arrest, without major changes in the toxicity parameters evaluated. In addition, this activity was associated with the presence of fenchone, its major component.
背景
唇形科植物偏叶中球藻（Mesosphaerum sidifolium (L'Hérit.) Harley & J.F.B.Pastore，异名：荫生香科科（Hyptis umbrosa））的精油（EOM）及其主要成分已进行了毒性和抗肿瘤活性测试。
方法
通过水蒸馏法从偏叶中球藻地上部分获得EOM，采用气相色谱 - 质谱联用技术对EOM的化学成分进行表征。使用溶血试验、急性毒性试验和微核试验评估其毒性。采用艾氏腹水癌模型评估EOM（50、100和150 mg/kg）以及小茴香酮（30和60 mg/kg）在治疗9天后的体内抗肿瘤活性和毒性。
结果
EOM的主要成分是小茴香酮（24.8%）、葎草烯（6.9%）、柠檬烯（5.4%）、匙叶桉油烯醇（4.5%）、β - 石竹烯（4.6%）和α - 杜松醇（4.7%）。EOM的HC50（引起50%溶血的浓度）为494.9 μg/mL，小茴香酮的HC50高于3000 μg/mL。EOM对小鼠的LD50约为500 mg/kg。该精油仅在300 mg/kg时诱导微核红细胞增加，表明具有中等遗传毒性。EOM（100或150 mg/kg）和小茴香酮（60 mg/kg）降低了所有分析参数（肿瘤体积、质量和总存活癌细胞）。接受EOM和小茴香酮治疗的动物存活率也有所提高。对于EOM 150 mg/kg和5 - 氟尿嘧啶治疗，大多数细胞停滞在G0/G1期，而对于小茴香酮，细胞停滞在S期，这代表细胞周期进程受阻。关于毒理学评估，EOM导致体重减轻，但未诱导血液学、生化或组织学（肝脏和肾脏）毒性。小茴香酮导致AST和ALT降低，表示肝脏损伤。
结论
数据表明，EOM通过诱导细胞周期停滞在艾氏腹水癌模型中引起体内细胞生长抑制，在所评估的毒性参数方面无重大变化。此外，这种活性与主要成分小茴香酮的存在有关。
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