Zero Hunger (SDG 2), Good Health & Well-being (SDG 3)
SDG3: prediction of pharmacokinetics profile of new cytotoxicities compounds from trunk bark and root bark of Citrus x paradisi (Rutaceae) Fanny-Aimée Essombe Malolo 1* , Lidwine Ngah 1 , Julien Moïse NKO’O 3 , Jean Claude Ndom 4 , Emmanuel Mpondo Mpondo 5 , Jean Duplex Wansi 4* , and Bikele Mama 4* 1 Department of Pharmacy; Faculty of Medicine and Pharmaceutical Sciences of the University of Dschang, P.O BOX: 96 Dschang-Cameroon, Department of Pharmacy; 2 Faculty of Medicine and Pharmaceutical Sciences of the University of Douala, P.O BOX: 2701 Douala-Cameroon, Department of Pharmacy; 3 Faculty of Medicine and Pharmaceutical Sciences of the University of Ebolowa, P.O BOX: 118 Ebolowa-Cameroon, Department of Chemistry; 4 Faculty of Sciences of the University of Douala, P.O BOX: 24157 Douala-Cameroon, Department of Pharmacotoxicology and Pharmacokinetics; 5 Faculty of Medicine and Biomedical Sciences of Pharmacokinetic and toxicity profile of new compounds with cytotoxicities effects isolated from the hybrid species Citrus X Paradisi Macfad [1,2] have been performed to molecular modeling and best choice of galenic form. 24 parameters of each compounds have been estimated. According to the Lipinski rules, the 1-Formyl-5-Hydroxy-N-Methylindolin-1-ium is the best drug candidate for all pharmaceutical forms and a good lead compound. For oral form (Violation of five Rule: 2), the 23 (s) -isolimonexin and the decyloxycleomiscosin D are not good drugs candidates. However, due to their hydrophilic character, the IV formulations would be appropriate. The 23 (s) -isolimonexin is also a good leader (violation of 3 Rule: 3). All those molecules would be highly toxic with a low therapeutic index (LD50 Oral Range, IP and IV in Rats: 0.35 - 3.44) and eliminated from kidney as metabolites with a short half-life time (T1/2 <1h). Consequently, it would be recommended to use hydrophobic formulations or substitute less hydrophilic groups with more hydrophobic groups (for 23 (s) -isolimonexin and decyloxleomiscosin D) or coating formulations ( 23 (s) -isolimonexin); or favor prolonged release forms to limit the toxic risk which could be induced by several close administrations but and keep an effective concentration. Key words: Pharmacokinetic, cytotoxicities, compounds, Rutaceae References 1. [Essombe Malolo, F.-A.; Kouam, A.D.K.; Nyobe, J.C.N.; Ngah, L.; Frese, M.; Ndom, J.C.; Langat, M.K.; Lenta, B.N.; Mulholland, D.A.; Sewald, N.; et al. Coumarinolignoid and Indole Alkaloids from the Roots of the Hybrid Plant Citrus × paradisi Macfad (Rutaceae). Molecules 2023, 28, 1078. https://doi.org/10.3390/ molecules28031078] 2. [Fanny-Aimée Essombe Malolo, George Bellier Tabekoueng, Willifred Dogmo Tekapi Tsopgni, Valery Wilfried Nguemdjo Chimeze, Ariane Kenmogne Kouam, Eduard Mas-Claret, Moses K. Langat, Jean Claude Ndom, Marcel Frese, Norbert Sewald, Jean Duplex Wansi (2022). Chemical constituents of the Stem bark of the hybrid plant Citrus x paradisi. Macfad. (Rutaceae). Journal of Chemistry and Biodiversity,19. Doi.org/10.1002/cbdv.202101033] the University of Yaounde 1, P.O BOX : 1364 Yaounde-Cameroon E-mail: emfay1@yahoo.fr, jdwansi@yahoo.fr, bikelemama@yahoo.fr
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