Pharmacological characterization of the pseudopterosins:: Novel anti-inflammatory natural products isolated from the Caribbean soft coral, Pseudopterogorgia elisabethae
Pharmacological characterization of the pseudopterosins:: Novel anti-inflammatory natural products isolated from the Caribbean soft coral, Pseudopterogorgia elisabethae
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DOI：
10.1016/s0024-3205(98)00229-x
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发表时间：
1998-05-22
期刊：
影响因子：
6.1
通讯作者：
Glaser, KB
中科院分区：
文献类型：
--
作者：
Mayer, AMS;Jacobson, PB;Glaser, KB
当局部（ED 50（μ g/耳）PSE（38）、PSA（8））或全身（ED 50（mg/kg，i. p.）PSE（14）、PSA（32））。两种化合物在苯基-对-苯醌诱导的扭体中均表现出体内镇痛活性（ED 50（mg/kg，i. p.）PSE（14）、PSA（4）。PSE抑制酵母多糖诱导的扭体（ED 50 = 6 mg/kg，i. p.），伴随腹膜渗出液6-酮-前列腺素F-1 α（ED 50 = 24 mg/kg）和白三烯C-4（ED 50 = 24 mg/kg）的剂量依赖性抑制。在体外，伪蝶呤作为磷脂酶A（2）、环氧合酶、细胞因子释放的抑制剂或粘附分子表达的调节剂没有活性。PSA抑制前列腺素E-2和白三烯C-4的生产酵母多糖刺激小鼠腹腔巨噬细胞（IC 50 = 4 μ M和1 μ M，分别），然而，PSE是有效得多。这些数据表明，假蝶呤可能通过抑制类花生酸类化合物从炎症细胞中释放，以浓度和剂量依赖性的方式介导其抗炎作用。(C)1998年爱思唯尔科学公司
Pseudopterosin E (PSE), a C-10 linked fucose glycoside and pseudopterosin A (PSA), a C-9 xylose glycoside isolated from the marine gorgonian Pseudopterogorgia elisabethae were both effective in reducing PMA-induced mouse ear edema when administered topically (ED50 (mu g/ear) PSE(38), PSA(8)) or systemically (ED50 (mg/kg, i.p.) PSE (14), PSA (32)). Both compounds exhibited in vivo analgesic activity in phenyl-p-benzoquinone-induced writhing (ED50 (mg/kg, i.p.) PSE(14), PSA(4). PSE inhibited zymosan-induced writhing (ED50 = 6 mg/kg, i.p.), with a concomitant dose-dependent inhibition of peritoneal exudate 6-keto-prostaglandin F-1 alpha (ED50 = 24 mg/kg) and leukotriene C-4 (ED50 = 24 mg/kg). In vitro, the pseudopterosins were inactive as inhibitors of phospholipase A(2), cyclooxygenase, cytokine release, or as regulators of adhesion molecule expression. PSA inhibited prostaglandin E-2 and leukotriene C-4 production in zymosan-stimulated murine peritoneal macrophages (IC50 = 4 mu M and 1 mu M, respectively); however, PSE was much less effective. These data suggest that the pseudopterosins may mediate their antiinflammatory effects by inhibiting eicosanoid release from inflammatory cells in a concentration and dose-dependent manner. (C) 1998 Elsevier Science Inc.