Di Silverio F, Monti S, Sciarra A, Varasano P A, Martini C, Lanzara S, D'Eramo G, Di Nicola S, Toscano V
Department of Urology, University of Rome La Sapienza, Italy.
Prostate. 1998 Oct 1;37(2):77-83. doi: 10.1002/(sici)1097-0045(19981001)37:2<77::aid-pros3>3.0.co;2-i.
The n-hexane lipido-sterol extract of Serenoa repens (LSESr, Permixon, Pierre Fabre Medicament, Castres, France), a phytotherapeutic agent used in the treatment of benign prostatic hyperplasia (BPH), has a multisite mechanism of action including inhibition of types 1 and 2 5alpha-reductase and competitive binding to androgen receptors in prostatic cells. Here, the response of testosterone (T), dihydrotestosterone (DHT), and epidermal growth factor (EGF) in BPH tissue of patients treated with LSESr (320 mg/day for 3 months) is analyzed.
BPH samples were sectioned in periurethral, subcapsular, and intermediate regions: in each region T, DHT, and EGF were determined by radioimmunoassay after purification on celite columns or Sep-pak C18 cartridges.
In the untreated group, T, DHT, and EGF presented the highest concentrations in the periurethral region (615 +/- 62 (SE) pg/g tissue, 7,317 +/- 551 pg/g tissue, and 20.9 +/- 3.3 ng/g tissue, respectively) with respect to the peripheral subcapsular region (425 +/- 45 pg/g tissue, 4,215 +/- 561 pg/g tissue, and 10.8 +/- 1.4 ng/g tissue, respectively). In the LSESr-treated group, a statistically significant reduction was observed, mainly in the periurethral region of DHT (2,363 +/- 553 pg/g tissue, P < 0.001) and EGF (6.98 +/- 2.48 ng/g tissue, P < 0.01), with increased T values (1,023 +/- 101 pg/g tissue, P < 0.001).
The decrease of DHT and the rise of T in BPH tissue of patients treated with Permixon confirms the capacity of this drug to inhibit in vivo 5alpha-reductase in human pathological prostate. A marked decrease of EGF, associated with DHT reduction, was also observed. These biochemical effects, similar to those obtained with finasteride, are particularly evident in the periurethral region, whose enlargement is responsible for urinary obstruction, with respect to the subcapsular region. A possible speculation is that the preferential reduction of DHT and EGF content in the periurethral region is involved in the clinical improvement of the obstructive symptoms in BPH during LSESr therapy.
锯叶棕果实提取物软胶囊(LSESr,保列治,法国皮埃尔法布雷制药公司,卡斯特尔)是一种用于治疗良性前列腺增生(BPH)的植物治疗药物,具有多部位作用机制,包括抑制1型和2型5α-还原酶以及与前列腺细胞中的雄激素受体竞争性结合。在此,分析了接受LSESr治疗(320毫克/天,持续3个月)的患者BPH组织中睾酮(T)、双氢睾酮(DHT)和表皮生长因子(EGF)的反应。
将BPH样本在尿道周围、包膜下和中间区域进行切片:在每个区域,通过在硅藻土柱或Sep-pak C18柱上纯化后用放射免疫分析法测定T、DHT和EGF。
在未治疗组中,尿道周围区域的T(615±62(SE)皮克/克组织)、DHT(7317±551皮克/克组织)和EGF(20.9±3.3纳克/克组织)的浓度相对于外周包膜下区域(分别为425±45皮克/克组织、4215±561皮克/克组织和10.8±1.4纳克/克组织)最高。在LSESr治疗组中,观察到有统计学意义的降低,主要是尿道周围区域中DHT(2363±553皮克/克组织,P<0.001)和EGF(6.98±2.48纳克/克组织,P<0.01)的降低,同时T值升高(1023±101皮克/克组织,P<0.001)。
保列治治疗患者的BPH组织中DHT降低和T升高证实了该药物在体内抑制人病理性前列腺中5α-还原酶的能力。还观察到与DHT降低相关的EGF显著降低。这些生化效应与非那雄胺获得的效应相似,在尿道周围区域相对于包膜下区域尤为明显,尿道周围区域的增大是导致尿路梗阻的原因。一种可能的推测是,尿道周围区域中DHT和EGF含量的优先降低与LSESr治疗期间BPH梗阻症状的临床改善有关。