title: Optimization of pancreatic lipase inhibition by Cudrania tricuspidata fruits using response surface methodology.
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.
authors.affiliation: College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Republic of Korea.
authors.forename: Ji Yeon
authors.initials: JY
authors.lastname: Jeong
authors.affiliation: College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Republic of Korea.
authors.forename: Yang Hee
authors.initials: YH
authors.lastname: Jo
authors.affiliation: College of Pharmacy, Korea University, Sejong City 339-700, Republic of Korea.
authors.forename: Ki Yong
authors.initials: KY
authors.lastname: Lee
authors.affiliation: Wellness R&D Center, Univera, Inc., Seoul, Republic of Korea.
authors.forename: Seon-Gil
authors.initials: SG
authors.lastname: Do
authors.affiliation: College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Republic of Korea.
authors.forename: Bang Yeon
authors.initials: BY
authors.lastname: Hwang
authors.affiliation: College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Republic of Korea. Electronic address: mklee@chungbuk.ac.kr.
authors.forename: Mi Kyeong
authors.initials: MK
authors.lastname: Lee
mesh_terms: D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology; D005638:Fruit / Q000737:chemistry*; D008049:Lipase / Q000037:antagonists & inhibitors*; D029586:Moraceae / Q000737:chemistry*; D010179:Pancreas / Q000201:enzymology*; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D010936:Plant Extracts; D008049:Lipase
keywords: 5,7,4′-Trihydroxy-6,8-diprenylisoflavone; Box–Behnken design; Cudrania tricuspidata; Optimization; Pancreatic lipase; Response surface methodology