Fabian Ifeanyi Eze1, Xavier Siwe Noundou2, Patience O Osadebe3, Rui W M Krause2. 1. Department of Pharmaceutical and Medicinal Chemistry, University of Nigeria Nsukka, 410001, Nigeria; Medicinal Organic Chemistry Laboratory, Department of Chemistry, Rhodes University, Grahamstown, 6140, South Africa. Electronic address: fabian.eze@unn.edu.ng. 2. Medicinal Organic Chemistry Laboratory, Department of Chemistry, Rhodes University, Grahamstown, 6140, South Africa; Marine Natural Products Chemistry Laboratory, Department of Biochemistry and Microbiology, Rhodes University, Grahamstown, 6140, South Africa. 3. Department of Pharmaceutical and Medicinal Chemistry, University of Nigeria Nsukka, 410001, Nigeria. Electronic address: patience.osadebe@unn.edu.ng.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: Anthocleista vogelii Planch (Loganiaceae) is used in African Traditional Medicine for the treatment of pain and inflammatory disorders as well as sleeping sickness. AIM OF THE STUDY: To determine the in vivo anti-inflammatory and in vitro anti-trypanosomal activities of the extracts of A. vogelii stem bark and identify the phytochemical classes of the fractions responsible for the activities. MATERIALS AND METHODS: The in vivo anti-inflammatory activity of the extracts was evaluated using the egg albumin-induced rat paw oedema model while the in vitro anti-trypanosomal activity was assessed on Trypanosoma brucei brucei. The in vitro cytotoxicity was assessed on HeLa (human cervix adenocarcinoma) cell line. RESULTS: The methanolic extract of A. vogelii stem bark, with 11.2% yield, gave LD50 > 5000 mg/kg. The n-hexane fraction of the extract contains steroids, terpenes and fatty acids and yielded non-cytotoxic terpenoidal column fraction with anti-trypanosomal IC50 of 3.0 μg/mL. The ethylacetate fraction at 100 mg/kg dose significantly (p < 0.05) provoked 37.8, 62.5 and 69.7% inhibition of oedema induced by egg-albumin at the second, fourth and sixth hours respectively. CONCLUSION: The study demonstrated that the anti-inflammatory and anti-trypanosomal activities of A. vogelii are probably due to non-cytotoxic terpenoids and validated the traditional use of A. vogelii in the treatment of inflammation and sleeping sickness.
ETHNOPHARMACOLOGICAL RELEVANCE: Anthocleista vogelii Planch (Loganiaceae) is used in African Traditional Medicine for the treatment of pain and inflammatory disorders as well as sleeping sickness. AIM OF THE STUDY: To determine the in vivo anti-inflammatory and in vitro anti-trypanosomal activities of the extracts of A. vogelii stem bark and identify the phytochemical classes of the fractions responsible for the activities. MATERIALS AND METHODS: The in vivo anti-inflammatory activity of the extracts was evaluated using the egg albumin-induced ratpaw oedema model while the in vitro anti-trypanosomal activity was assessed on Trypanosoma brucei brucei. The in vitro cytotoxicity was assessed on HeLa (human cervix adenocarcinoma) cell line. RESULTS: The methanolic extract of A. vogelii stem bark, with 11.2% yield, gave LD50 > 5000 mg/kg. The n-hexane fraction of the extract contains steroids, terpenes and fatty acids and yielded non-cytotoxic terpenoidal column fraction with anti-trypanosomal IC50 of 3.0 μg/mL. The ethylacetate fraction at 100 mg/kg dose significantly (p < 0.05) provoked 37.8, 62.5 and 69.7% inhibition of oedema induced by egg-albumin at the second, fourth and sixth hours respectively. CONCLUSION: The study demonstrated that the anti-inflammatory and anti-trypanosomal activities of A. vogelii are probably due to non-cytotoxic terpenoids and validated the traditional use of A. vogelii in the treatment of inflammation and sleeping sickness.
Authors: Khaled AbouAitah; Imane M Higazy; Anna Swiderska-Sroda; Reda M Abdelhameed; Stanislaw Gierlotka; Tarik A Mohamed; Urszula Szałaj; Witold Lojkowski Journal: Drug Deliv Date: 2021-12 Impact factor: 6.819