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Biochemical and Molecular Actions of Nutrients

Salacia reticulata and Its Polyphenolic Constituents with Lipase Inhibitory and Lipolytic Activities Have Mild Antiobesity Effects in Rats

Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8412, Japan and ^* Research and Development Division, Morishita Jintan Company, Chuo-ku, Osaka 540-8566, Japan

¹To whom correspondence should be addressed. E-mail: shoyaku{at}mb.kyoto-phu.ac.jp.

Salacia (S.) reticulata, a Hippocrateaceae plant distributed in Sri Lankan and Indian forests, has been used as a supplementary food in Japan to prevent obesity and diabetes. We examined the antiobesity effects of the hot water–soluble extract (SRHW) from the roots of S. reticulata using obese rat models and an in vitro study. Body weight (P = 0.07) and periuterine fat storage (P = 0.10) in female Zucker fatty rats (8–9 wk old) tended to be suppressed by oral administration of SRHW (125 mg/kg) for 27 d. Male rats fed a high fat diet were not affected by SRHW. Furthermore, SRHW inhibited porcine pancreatic lipase (PL), rat adipose tissue–derived lipoprotein lipase (LPL) and glycerophosphate dehydrogenase (GPDH) activities with 50% inhibitory concentrations (IC₅₀) of 264 (95% confidence limits: 203–393) mg/L, 15 (12–18) mg/L and 54 (35–85) mg/L, respectively, but did not inhibit hormone-sensitive lipase activity in rat adipose tissue. Next, we examined the effects of polyphenols, di- and triterpenes and salacinol isolated from the roots of S. reticulata on lipid metabolizing enzymes and lipolysis. (-)-Epigallocatechin and (-)-epicatechin-(4ß8)-(-)-4'-O-methylepigallocatechin inhibited PL activity with IC₅₀ of 88 (not calculated) and 68 (26–122) mg/L, respectively. (-)-Epicatechin, 3ß, 22ß-dihydroxyolean-12-en-29-oic acid and the tannin fraction inhibited LPL activity with IC₅₀ of 81 (54–214), 89 (62–214) and 35 (24–62) mg/L. Only the tannin fraction inhibited GPDH activity with an IC₅₀ of 6.8 (3.4–10.9) mg/L. These constituents may be involved in the lipase and GPDH inhibitory activities of SRHW. On the other hand, SRHW at 100 mg/L tended to enhance lipolysis in rat adipocytes (P = 0.06). Significant lipolytic effects were exerted by mangiferin, (-)-4'-O-methylepigallocatechin and maytenfolic acid at 100 mg/L (P < 0.01). In conclusion, polyphenolic compounds may be involved in the antiobesity effects of SRHW in rats through inhibition of fat metabolizing enzymes (PL, LPL and GPDH) and enhanced lipolysis.

KEY WORDS: • Salacia reticulata • obesity • polyphenol • lipase • lipolysis • rats

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