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目的 观察有机磷与拟除虫菊酯农药的拟雌激素活性。方法 选用 5种有机磷农药[辛硫磷 (Pho)、马拉硫磷 (Mal)、乐果 (Dim)、久效磷 (Mon)和水胺硫磷 (Opt) ]和 4种拟除虫菊酯农药[氰戊菊酯 (Fen)、溴氰菊酯 (Del)、氯氰菊酯 (Cyp)和苄氯菊酯 (Per) ],进行大鼠子宫雌激素受体 (ER)竞争结合试验和人乳腺癌MCF 7细胞增殖试验。结果 5种有机磷农药在体外均不与大鼠子宫ER结合 ,不能诱导MCF 7细胞增殖 ;4种拟除虫菊酯农药在体外能与 2 ,4 ,6,7 3H雌二醇 ( 3H E2 )竞争ER ,其结合能力Fen >Cyp >Per>Del,Fen与Cyp抑制3H E2 与ER结合的IC50 分别为 0 .4 79、0 .5 62mmol/L ;拟除虫菊酯能引起MCF 7细胞不同程度的增殖 ,刺激增殖能力Per>Fen >Del>Cyp ,其中Cyp、Del和Per所引起的增殖效应能被雌激素拮抗剂ICI 178.82 0完全阻断 ,而Fen所引起的细胞增殖不能被完全阻断。结论 观察的 5种有机磷农药不具有拟雌激素活性 ;4种拟除虫菊酯农药通过激活ER显示其拟雌激素活性。Fen诱导的MCF 7细胞增殖不完全是由ER激活所引起。
Objective To observe the estrogenic activity of organophosphorus and pyrethroid pesticides. Methods Five organophosphorus pesticides (Pho, Mal, Dim, Mon and Opt) and four pyrethroids Pesticides [fen, Del, cypermethrin and Permethoxazole] were used to perform rat estrogen receptor (ER) competitive binding assay and human breast cancer MCF 7 Cell Proliferation Assay. Results All five kinds of organophosphorus pesticides did not bind with the ER of rat uterus in vitro and could not induce the proliferation of MCF 7 cells. Four kinds of pyrethroid pesticides could compete with 2,4,6,7H estradiol (3H E2) in vitro ER, the binding capacity of Fen> Cyp> Per> Del, Fen and Cyp inhibit the 3H E2 and ER binding of IC50 were 0.797.55 62mmol / L; pyrethroid can cause different degrees of proliferation of MCF 7 cells , And the proliferative ability Per> Fen> Del> Cyp. The proliferative effects induced by Cyp, Del and Per were completely blocked by the estrogen antagonist ICI 178.82 0, whereas the proliferation induced by Fen was not completely blocked. CONCLUSION: The five organophosphorus pesticides observed did not possess pseudo-estrogenic activity. Four pyrethroid-based pesticides displayed their pseudo-estrogenic activity by activating ER. Fen-induced MCF7 cell proliferation is not entirely caused by ER activation.