| Preliminary research showed that ethanol extracts from fruit shell of Camellia oleifera Abel. (COE) had the ability to anti-oxidate, inhibit tumor cell proliferation, inhibit S180 tumor growth, reduce lipids and lose weight. Small scale study found that COE could alleviate symptoms of prostatic hyperplasia. This article aims to detect the effects of COE on inhibiting 5 alpha-reductase (5AR) and preventing enzyme related diseases, including benign prostatic hyperplasia (BPH) and prostate cancer (PCa). The main results are as follows:(1) Vanillin-acetic acid-perchloric acid, Folin-Ciocalteau and ultraviolet method were used by comparing the recovery rate, precision and stability to determine total saponin, total polyphenol and total flavonoids, respectively. The contents of total saponin, total polyphenol and total flavonoids in crude extract were 27.35%,22.41%,2.81%, respectively. Maximum amount of saponin was found in butanol fraction,44.05%; ethyl acetate fraction had a highest content of polyphenol with a value of 35.34%. After ethanol gradient elution by D101 macroporous resin, polyphenol in butanol fraction mainly concentrated in 20AL and 40AL while saponin were distrbuted in each elution.(2) Spectrophotometric method were used to establish 5AR screening model in vitro: testosterone 20μM, NADPH 40μM, enzyme extract 216 ug, DTT 1 mM, pH 6.5 sodium phosphate buffer 40mM,37℃for 4 min. When the concentration of COE was 10μg/mL in the system, the remain activity (RA) of 5AR was 54.92%±9.31%. At the same concentration, however, the inhibitory effects of ethyl acetate and butanol fraction on 5AR enhanced with RA values 30.58%±0.65% and 20.71%±0.54%, respectively. The inhibitory effects of 40AL on 5AR was far more than butanol fraction and its RA was 3.18%±2.81%。(3) In BPH rats model induced by propionic acid testosterone, COE could reduce rat prostate heavy, prostate index, increase the 22nd days of urine flow (high dose group P<0.05), reduce the height of the prostate epithelial cells. In obese mice model, COE plunder dose group (P<0.05) and high dose group (P<0.01) were significantly reduce obese mice prostate index.(4) COE can inhibit the proliferation of PC-3, half inhibiting concentration (IC50) was 151.6μg/mL. The inhibitory activity of butanol fraction was increased with an IC50 value of 54.8μg/mL. Among the eluting fractions, the activity of 20AL and 40AL were weakened, while 60AL and 80AL were enhanced. The IC50 value of 60AL and 80AL was respectively 43.0μg/mL,28.1μg/mL in 48h. Through morphological observation and acridine orange staining,60AL and 80AL were shown to induce PC-3 apoptosis.In summary, COE can inhibit 5AR activity effectively, improve prostatic hyperplasia rats and mice symptoms, and inhibit PC-3 cell proliferation through inducing apoptosis. |