PMID- 35947833 OWN - NLM STAT- MEDLINE DCOM- 20220812 LR - 20220822 IS - 0794-859X (Print) IS - 0794-859X (Linking) VI - 37 IP - 1 DP - 2022 Jun 30 TI - A novel gedunin-2-hydroxypropyl-beta-cyclodextrin inclusion complex improves anti-nociceptive and anti-inflammatory activities of gedunin in rodents. PG - 9-19 LID - 10.54548/njps.v37i1.2 [doi] AB - Gedunin is a bioactive compound, obtained from Entandrophragma angolense (EA), which has limited therapeutic usefulness due to poor aqueous solubility and first-pass effects. Cyclodextrins are cyclic oligosaccharides that form complexes with poorly soluble compounds, thus enhancing their pharmacological activity. In this article, we evaluated the pharmacological activities of gedunin-2-hydroxypropyl-beta-cyclodextrin complex (GCD) in rodents. The antinociceptive activity of GCD (50, 100, 200 mg/kg) and Gedunin (50mg/kg) was tested in acetic acid-induced writhing and formalin-induced paw licking in mice. The anti-inflammatory activity was investigated in carrageenan-induced paw oedema and air pouch inflammation models in rats. Leucocytes counts, Tumour Necrosis Factor-alpha (TNF-alpha) level, nitric oxide, malondialdehyde, reduced glutathione, and myeloperoxidase enzyme activities were assessed in the air pouch exudate. The GCD (200mg/kg) significantly decreased writhing response, reduced licking duration and decreased oedema compared with gedunin and control. Exudate volume and leucocyte count were significantly reduced by GCD (200 mg/kg), it decreased myeloperoxidase activity and inhibited TNF-alpha release. The carrageenan-induced GSH depletion, increased malondialdehyde and nitrite levels were significantly reversed by GCD (200 mg/kg) relative to gedunin and control. The GCD complex demonstrated significant antinociceptive and anti-inflammatory activities relative to gedunin alone via mechanisms associated with inhibition of oxidative stress and inflammation in rodents. FAU - Ologe, Mary Olufunmilayo AU - Ologe MO AD - University of Ilorin, Ilorin. funmiologe@yahoo.com. LA - eng PT - Journal Article DEP - 20220630 PL - Nigeria TA - Niger J Physiol Sci JT - Nigerian journal of physiological sciences : official publication of the Physiological Society of Nigeria JID - 8811109 RN - 0 (Analgesics) RN - 0 (Anti-Inflammatory Agents) RN - 0 (Antioxidants) RN - 0 (Limonins) RN - 0 (Plant Extracts) RN - 0 (Tumor Necrosis Factor-alpha) RN - 1I96OHX6EK (2-Hydroxypropyl-beta-cyclodextrin) RN - 2753-30-2 (gedunin) RN - 4Y8F71G49Q (Malondialdehyde) RN - 9000-07-1 (Carrageenan) RN - EC 1.11.1.7 (Peroxidase) SB - IM MH - 2-Hydroxypropyl-beta-cyclodextrin MH - *Analgesics/pharmacology/therapeutic use MH - Animals MH - Anti-Inflammatory Agents/pharmacology/therapeutic use MH - Antioxidants/therapeutic use MH - Carrageenan MH - Edema/chemically induced/drug therapy MH - Inflammation/drug therapy MH - Limonins MH - Malondialdehyde MH - Mice MH - Pain/chemically induced/drug therapy MH - Peroxidase MH - Plant Extracts/pharmacology MH - Rats MH - Rodentia MH - *Tumor Necrosis Factor-alpha EDAT- 2022/08/11 06:00 MHDA- 2022/08/13 06:00 CRDT- 2022/08/10 16:42 PHST- 2022/05/27 00:00 [received] PHST- 2022/06/07 00:00 [accepted] PHST- 2022/08/10 16:42 [entrez] PHST- 2022/08/11 06:00 [pubmed] PHST- 2022/08/13 06:00 [medline] AID - 10.54548/njps.v37i1.2 [doi] PST - epublish SO - Niger J Physiol Sci. 2022 Jun 30;37(1):9-19. doi: 10.54548/njps.v37i1.2.