PEG modification of Amorfrutin B from Amorpha fructicosa increases gastric absorption, circulation half-life and glucose uptake by T3T-L1 adipocytes - 14/11/17
, Md Nazmul Hasan a , Sudipta Banarjee a , Mizanur Rahman a , Sabbir Raihan a , Faika Laz Banti a , Sania Sarker Sayfe b , S.M. Nageeb Hasan a , Farjana Akhter a , Ashraf Ul Kabir a , J.M.A. Hannan a Bienvenue sur EM-consulte, la référence des professionnels de santé.
L’accès au texte intégral de cet article nécessite un abonnement.
| pages | 7 |
| Iconographies | 8 |
| Vidéos | 0 |
| Autres | 0 |
Abstract |
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.
Le texte complet de cet article est disponible en PDF.Keywords : Amorfrutin, Amorpha fructicosa, PEGylation, Pharmacokinetics
Plan
Vol 95
P. 513-519 - novembre 2017 Retour au numéro
Article précédent
- Effects of Ganoderma lucidum polysaccharides against doxorubicin-induced cardiotoxicity
- Fan Xu, Xiao Li, Xu Xiao, Lan-fang Liu, Li Zhang, Ping-ping Lin, Sheng-lin Zhang, Qing-shan Li
- Erhuang Formula ameliorates renal damage in adenine–induced chronic renal failure rats via inhibiting inflammatory and fibrotic responses
- Chun-yan Zhang, Jian-yong Zhu, Ying Ye, Miao Zhang, Li-jun Zhang, Su-juan Wang, Ya-nan Song, Hong Zhang
Bienvenue sur EM-consulte, la référence des professionnels de santé.
L’accès au texte intégral de cet article nécessite un abonnement.
Bienvenue sur EM-consulte, la référence des professionnels de santé.
L’achat d’article à l’unité est indisponible à l’heure actuelle.
Déjà abonné à cette revue ?