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Orally active osteoanabolic agent 6-C-β-D-glucopyranosyl-(2S, 3S)-(+)- 5,7, 3',4'- tetrahydroxydihydroflavonol binds to adiponectin receptors, with a preference for AdipoR1, induces adiponectin-associated signaling and improves metabolic health in a roden

หน่วยงาน Central Drug Research Institute (CDRI), India

รายละเอียด

ชื่อเรื่อง : Orally active osteoanabolic agent 6-C-β-D-glucopyranosyl-(2S, 3S)-(+)- 5,7, 3',4'- tetrahydroxydihydroflavonol binds to adiponectin receptors, with a preference for AdipoR1, induces adiponectin-associated signaling and improves metabolic health in a rodent model of diabetes
นักวิจัย : Singh, A K , Joharapurkar, A A , Khan, M P , Mishra, J S , Singh, Nidhi , Yadav, Manisha , Hossain, Zakir , Khan, Kainat , Kumar, Sudhir , Dhanesha, N A , Mishra, D P , Maurya, Rakesh , Sharma, Sharad , Jain, M R , Trivedi, A K , Godbole, M M , Gayen, J R , Chattopadhyay, Naibedya , Sanyal, Sabyasachi
คำค้น : Osteoanabolic , Adiponectin
หน่วยงาน : Central Drug Research Institute (CDRI), India
ผู้ร่วมงาน : -
ปีพิมพ์ : 2557
อ้างอิง : Diabetes, 2014, 63(10),3530-44 , http://hdl.handle.net/123456789/1428
ที่มา : -
ความเชี่ยวชาญ : -
ความสัมพันธ์ : CSIR-CDRI Communication No. 8700
ขอบเขตของเนื้อหา : -
บทคัดย่อ/คำอธิบาย :

Adiponectin is an adipocytokine that signals through plasma membrane-bound adiponectin receptors (AdipoR) -1 and -2. Plasma adiponectin depletion is associated with type 2 diabetes, obesity and cardiovascular diseases. Adiponectin therapy however, is yet unavailable owing to its large size, complex multimerization and functional differences of the multimers. We report discovery and characterization of 6-C-β-D-glucopyranosyl-(2S, 3S)-(+)- 5,7, 3',4'- tetrahydroxydihydroflavonol (GTDF) as an orally active adiponectin mimetic. GTDF interacted with both AdipoRs, with a preference for AdipoR1. It induced adiponectin-associated signaling and enhanced glucose uptake and fatty acid oxidation in vitro, which were augmented or abolished by AdipoR1 overexpression or silencing respectively. GTDF improved metabolic health, characterized by elevated glucose-clearance, β-cell-survival, reduced steatohepatitis, browning of white adipose tissue and improved lipid profile in an AdipoR1-expressing but not an AdipoR1-depleted strain of diabetic mice. The discovery of GTDF as an adiponectin mimetic provides a promising therapeutic tool for the treatment of metabolic diseases.

บรรณานุกรม :
Singh, A K , Joharapurkar, A A , Khan, M P , Mishra, J S , Singh, Nidhi , Yadav, Manisha , Hossain, Zakir , Khan, Kainat , Kumar, Sudhir , Dhanesha, N A , Mishra, D P , Maurya, Rakesh , Sharma, Sharad , Jain, M R , Trivedi, A K , Godbole, M M , Gayen, J R , Chattopadhyay, Naibedya , Sanyal, Sabyasachi . (2557). Orally active osteoanabolic agent 6-C-β-D-glucopyranosyl-(2S, 3S)-(+)- 5,7, 3',4'- tetrahydroxydihydroflavonol binds to adiponectin receptors, with a preference for AdipoR1, induces adiponectin-associated signaling and improves metabolic health in a roden.
    : Central Drug Research Institute (CDRI), India.
Singh, A K , Joharapurkar, A A , Khan, M P , Mishra, J S , Singh, Nidhi , Yadav, Manisha , Hossain, Zakir , Khan, Kainat , Kumar, Sudhir , Dhanesha, N A , Mishra, D P , Maurya, Rakesh , Sharma, Sharad , Jain, M R , Trivedi, A K , Godbole, M M , Gayen, J R , Chattopadhyay, Naibedya , Sanyal, Sabyasachi . 2557. "Orally active osteoanabolic agent 6-C-β-D-glucopyranosyl-(2S, 3S)-(+)- 5,7, 3',4'- tetrahydroxydihydroflavonol binds to adiponectin receptors, with a preference for AdipoR1, induces adiponectin-associated signaling and improves metabolic health in a roden".
    : Central Drug Research Institute (CDRI), India.
Singh, A K , Joharapurkar, A A , Khan, M P , Mishra, J S , Singh, Nidhi , Yadav, Manisha , Hossain, Zakir , Khan, Kainat , Kumar, Sudhir , Dhanesha, N A , Mishra, D P , Maurya, Rakesh , Sharma, Sharad , Jain, M R , Trivedi, A K , Godbole, M M , Gayen, J R , Chattopadhyay, Naibedya , Sanyal, Sabyasachi . "Orally active osteoanabolic agent 6-C-β-D-glucopyranosyl-(2S, 3S)-(+)- 5,7, 3',4'- tetrahydroxydihydroflavonol binds to adiponectin receptors, with a preference for AdipoR1, induces adiponectin-associated signaling and improves metabolic health in a roden."
    : Central Drug Research Institute (CDRI), India, 2557. Print.
Singh, A K , Joharapurkar, A A , Khan, M P , Mishra, J S , Singh, Nidhi , Yadav, Manisha , Hossain, Zakir , Khan, Kainat , Kumar, Sudhir , Dhanesha, N A , Mishra, D P , Maurya, Rakesh , Sharma, Sharad , Jain, M R , Trivedi, A K , Godbole, M M , Gayen, J R , Chattopadhyay, Naibedya , Sanyal, Sabyasachi . Orally active osteoanabolic agent 6-C-β-D-glucopyranosyl-(2S, 3S)-(+)- 5,7, 3',4'- tetrahydroxydihydroflavonol binds to adiponectin receptors, with a preference for AdipoR1, induces adiponectin-associated signaling and improves metabolic health in a roden. : Central Drug Research Institute (CDRI), India; 2557.