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Design and synthesis of lupeol analogues and their glucose uptake stimulatory effect in L6 skeletal muscle cells

หน่วยงาน Central Drug Research Institute (CDRI), India

รายละเอียด

ชื่อเรื่อง : Design and synthesis of lupeol analogues and their glucose uptake stimulatory effect in L6 skeletal muscle cells
นักวิจัย : Khan, M F , Maurya, C K , Dev, Kapil , Arha, Deepti , Rai, A K , Tamrakar, A K , Maurya, Rakesh
คำค้น : Type 2 Diabetes Mellitus , Lupeol , Isopropylene Moiety , Glucose Uptake , Stimulation
หน่วยงาน : Central Drug Research Institute (CDRI), India
ผู้ร่วมงาน : -
ปีพิมพ์ : 2557
อ้างอิง : Bioorganic & Medicinal Chemistry Letters, 2014, 24(12), 2674-9 , http://hdl.handle.net/123456789/1362
ที่มา : -
ความเชี่ยวชาญ : -
ความสัมพันธ์ : CSIR-CDRI Communication No. 8662
ขอบเขตของเนื้อหา : -
บทคัดย่อ/คำอธิบาย :

Structure modifications of lupeol at the isopropylene moiety have been described via allylic oxidation using selenium dioxide. The antidiabetic efficacy of lupeol analogues were evaluated in vitro as glucose uptake stimulatory effect in L6 skeletal muscle cells. From all tested compounds, 2, 3, 4b and 6b showed significant stimulation of glucose uptake with respective percent stimulation of 173.1 (p<0.001), 114.1 (p<0.001), 98.3 (p<0.001) and 107.3 (p<0.001) at 10 µM concentration. Stimulation of glucose uptake by these compounds is associated with enhanced translocation of glucose transporter 4 (GLUT4) and activation of IRS-1/PI3-K/AKT-dependent signaling pathway in L6 cells. Structure-activity relationship analysis of these analogues demonstrated that the integrity of α, β-unsaturated carbonyl and acetyl moieties were important in the retention of glucose uptake stimulatory effect. It is therefore proposed that naturally occurring lupeol and their analogues might reduce blood glucose, at least in part, through stimulating glucose utilization by skeletal muscles.

บรรณานุกรม :
Khan, M F , Maurya, C K , Dev, Kapil , Arha, Deepti , Rai, A K , Tamrakar, A K , Maurya, Rakesh . (2557). Design and synthesis of lupeol analogues and their glucose uptake stimulatory effect in L6 skeletal muscle cells.
    : Central Drug Research Institute (CDRI), India.
Khan, M F , Maurya, C K , Dev, Kapil , Arha, Deepti , Rai, A K , Tamrakar, A K , Maurya, Rakesh . 2557. "Design and synthesis of lupeol analogues and their glucose uptake stimulatory effect in L6 skeletal muscle cells".
    : Central Drug Research Institute (CDRI), India.
Khan, M F , Maurya, C K , Dev, Kapil , Arha, Deepti , Rai, A K , Tamrakar, A K , Maurya, Rakesh . "Design and synthesis of lupeol analogues and their glucose uptake stimulatory effect in L6 skeletal muscle cells."
    : Central Drug Research Institute (CDRI), India, 2557. Print.
Khan, M F , Maurya, C K , Dev, Kapil , Arha, Deepti , Rai, A K , Tamrakar, A K , Maurya, Rakesh . Design and synthesis of lupeol analogues and their glucose uptake stimulatory effect in L6 skeletal muscle cells. : Central Drug Research Institute (CDRI), India; 2557.