摘要
近年研究表明,炎症和癌症都与花生四烯酸的代谢产物环氧酶和5-脂氧酶密切相关。据此选择对环氧酶或5-脂氧酶具有抑制作用的苯丙烯酸类化合物作为抗炎、抗癌先导化合物,并对其酯类衍生物及其苯乙烯酮类类似物进行初步探讨。本文作者设计并合成上述类型化合物共十九个,其中十五个为未见文献报道的新化合物,并经红外光谱、~1H-核磁共振光谱及元素分析等证实其化学结构。对所合成的化合物进行了抗炎及抗癌药理活性初步筛选。体内抗炎实验表明,所合成的苯丙烯酸类化合物Ⅰ_A,Ⅰ_B,Ⅰ_C人及其酯类衍生物Ⅱ_(2A),Ⅱ_(2C),Ⅱ_(5C)和苯乙烯酮类似物Ⅲ_C对巴豆油诱发的小鼠耳廓肿胀均有不同程度和抑制作用。体外抗癌作用初步筛选结果表明,化合物Ⅰ_B,Ⅱ_(5A),Ⅱ_(5C),及Ⅲ_D对HL-60人癌细胞均有较好的抑制作用。值得注意的是,化合物Ⅰ_B和Ⅱ_(5C)不仅对体外HL-60人癌细胞具有明显的抑制作用,而且对巴豆油所致小鼠炎症亦有较强的活性。深入的药理实验还在进行中。
Cinnamic acids were selected as lead compounds of antiinflammatory
and anticancer agents through the investigation of their biological properties. Their esters
and related styryl ketones were also studied. A total of nineteen compounds, fifteen of them
not reported previously, were synthesized and found to be of considerable pharmacological
interest. In preliminary biological tests, compounds Ⅰ_A, Ⅰ_B, Ⅰ_c, Ⅱ_(2c) and II_(5c) showed signifi-
cant inhibiting effect on croton oil induced mouse ear edema, Ⅰ_B, Ⅱ_(sA), Ⅱ_(sc) and Ⅲ_D exhibited
good activity on HL--60 human cancer cells in vitro. It is well worth noticing that com-
pounds Ⅰ_B and Ⅱ_(5c) exhibited excellent antiinflammatory action as well as anticancer activity.
出处
《药学学报》
CAS
CSCD
北大核心
1992年第11期817-823,共7页
Acta Pharmaceutica Sinica
关键词
苯丙烯酸
苯乙烯酮
化合物
合成
Cinnamic acids
Styryl ketones
Antiinflammatory activity
Anticancer activity
