title: Glucal-conjugated sterols as novel vascular leakage blocker: structure-activity relationship focusing on the C17-side chain.
abstract: A series of glucal-conjugated sterols as novel vascular leakage blocker were identified through design, synthesis and biologically evaluation. In addition, the structure-activity relationship (SAR) of the glucal-conjugated sterols focusing on the C17-side chain was also established. The sterol analogs linked with the rigid C17-side chain side chains exhibited potent cell survival activities. In particular, analog 21l, which possesses a cyclopentyl oxime moiety, was shown to have excellent pharmacological effects on retinal vascular leakage in a diabetic mouse model.
authors: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors: Kyeojin
authors: K
authors: Kim
authors: Department of Biochemistry, College of Life Science and Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea.
authors: Sony
authors: S
authors: Maharjan
authors: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors: Changjin
authors: C
authors: Lim
authors: Department of Pharmacy, College of Pharmacy, Kyung Hee University, Seoul 130-701, Republic of Korea.
authors: Nam-Jung
authors: NJ
authors: Kim
authors: Department of Biochemistry, College of Life Science and Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea.
authors: Vijayendra
authors: V
authors: Agrawal
authors: College of Pharmacy, Woosuk University, Wanju 565-701, Republic of Korea.
authors: Young Taek
authors: YT
authors: Han
authors: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors: Sujin
authors: S
authors: Lee
authors: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors: Hongchan
authors: H
authors: An
authors: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors: Hwayoung
authors: H
authors: Yun
authors: Department of Biochemistry, College of Life Science and Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea.
authors: Hyun-Jung
authors: HJ
authors: Choi
authors: Department of Biochemistry, College of Life Science and Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea. Electronic address: ygkwon@yonsei.ac.kr.
authors: Young-Guen
authors: YG
authors: Kwon
authors: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea. Electronic address: ygsuh@snu.ac.kr.
authors: Young-Ger
authors: YG
authors: Suh
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D002125:Calcium Gluconate / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D003921:Diabetes Mellitus, Experimental / Q000150:complications; D003930:Diabetic Retinopathy / Q000188:drug therapy* / Q000473:pathology; D042783:Endothelial Cells / Q000187:drug effects* / Q000473:pathology; D061307:Human Umbilical Vein Endothelial Cells; D051379:Mice; D008810:Mice, Inbred C57BL; D010091:Oximes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010539:Permeability / Q000187:drug effects; D012160:Retina / Q000166:cytology / Q000187:drug effects / Q000473:pathology; D013261:Sterols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D010091:Oximes; D013261:Sterols; D002125:Calcium Gluconate
keywords: Anti-apoptotic agents; Diabetic retinopathy; Ginsenoside Rk1; Oxime; Pregnenolone; Tight junction