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Bioorg Med Chem Lett. 2014 May 15;24(10):2329-33. doi: 10.1016/j.bmcl.2014.03.067. Epub 2014 Apr 1.

Optimization of pancreatic lipase inhibition by Cudrania tricuspidata fruits using response surface methodology.

Author information

1
College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Republic of Korea.
2
College of Pharmacy, Korea University, Sejong City 339-700, Republic of Korea.
3
Wellness R&D Center, Univera, Inc., Seoul, Republic of Korea.
4
College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Republic of Korea. Electronic address: mklee@chungbuk.ac.kr.

Abstract

The fruits of Cudrania tricuspidata (Carr.) Bur. (Moraceae) significantly inhibited pancreatic lipase, which plays a key role in fat absorption. Optimization of extraction conditions with minimum pancreatic lipase activity and maximum yield was determined using response surface methodology with three-level-three-factor Box-Behnken design (BBD). Regression analysis showed a good fit of the experimental data and the optimal condition was obtained as ethanol concentration, 74.5%; temperature 61.9°C and extraction time, 13.5h. The pancreatic lipase activity and extraction yield under optimal conditions were found to be 65.5% and 54.0%, respectively, which were well matched with the predicted value of 65.8% and 47.1%. Further fractionation of C. tricuspidata extract resulted in the isolation of compound 1, which was identified as 5,7,4'-trihydroxy-6,8-diprenylisoflavone. It inhibited pancreatic lipase activity with IC50 value of 65.0μM. HPLC analysis suggested positive correlation between pancreatic lipase inhibition and 5,7,4'-trihydroxy-6,8-diprenylisoflavone of C. tricuspidata fruits.

KEYWORDS:

5,7,4′-Trihydroxy-6,8-diprenylisoflavone; Box–Behnken design; Cudrania tricuspidata; Optimization; Pancreatic lipase; Response surface methodology

PMID:
24751440
DOI:
10.1016/j.bmcl.2014.03.067
[Indexed for MEDLINE]

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