التفاصيل البيبلوغرافية
| العنوان: |
PEG modification of Amorfrutin B from Amorpha fructicosa increases gastric absorption, circulation half-life and glucose uptake by T3T-L1 adipocytes. |
| المؤلفون: |
Samad, Mehdi Bin1 mehdi.samad@unmc.edu, Hasan, Md Nazmul1 ryan.nsu092@yahoo.com, Banarjee, Sudipta1 sudipta.banerjee@hotmail.com, Rahman, Mizanur1 mm.rahmanbd@yahoo.com, Raihan, Sabbir1 sabbirraihan137@gmail.com, Banti, Faika Laz1 faika00@yahoo.com, Sayfe, Sania Sarker2 saniassaify@gmail.com, Hasan, S.M. Nageeb1 smnageebhasan@yahoo.com, Akhter, Farjana1 farjanaafrin88@yahoo.com, Kabir, Ashraf Ul1 a.kabir@wustl.edu, Hannan, J.M.A.1 jmahannan@northsouth.edu |
| المصدر: |
Biomedicine & Pharmacotherapy. Nov2017, Vol. 95, p513-519. 7p. |
| مصطلحات موضوعية: |
*AMORPHA, *GASTROINTESTINAL agents, *PHARMACOKINETICS, *GLUCOSE tolerance tests, *KIDNEY function tests |
| مستخلص: |
Through a simple PEG-conjugation of the natural product Amorfrutin B, we enhanced its pharmacokinetic profile. The PEGylated molecule displayed significantly improved gastrointestinal absorption (p < 0.05) and had a longer systemic circulation life (p < 0.05). Oral glucose tolerance study showed PEGylated Amorfrutin B displayed longer protection against oral glucose load compared to Amorfrutin B (p < 0.05). It also showed significant improvement in glucose uptake in-vitro by T3T-L1 adipocytes (p < 0.05). The PEGylated molecule also showed reduced propensity of crossing the blood brain barrier and accumulating in the brain (p < 0.05). It also showed reduced accumulation in the adipose tissue. Preliminary liver and kidney toxicity screening showed no significant alteration in liver or kidney function of Amorfrutin B or its PEGylated form. In conclusion, PEG modification can be an attractive strategy to reduce lipophilicity and enhance pharmacokinetic properties of natural products, derived from traditional medicine. [ABSTRACT FROM AUTHOR] |
| قاعدة البيانات: |
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