Browsing by Author "Aderibigbe, Blessing A. 0000-0003-1157-7481"

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    Novel ferrocenylbisphosphonate hybrid compounds: Synthesis, characterization and potent activity against cancer cell lines
    (2022-02-02) Anusionwu, Chioma G.; Aderibigbe, Blessing A. 0000-0003-1157-7481; Adeyemi, Samson A.; Ubanako, Philemon; Oselusi, Samson O.; Choonara, Yahya E.; Mbianda, Xavier Yangkou
    The toxicity of existing anticancer agents on healthy cells and the emergence of multidrug-resistance cancer cells have led to the search for less toxic anticancer agents with different mechanisms of action. In this study, a novel class of ferrocenylbisphosphonate hybrid compounds (H1-H8) were designed and characterized using NMR, IR and HRMS. The in vitro anticancer activity of the hybrid compounds on HeLa (cervix adenocarcinoma) and A549 (non-small cell lung cancer cell lines) was evaluated. The structure–activity relationship of the hybrid molecules was also studied. The lead compound, tetraethyl (3-(4-oxo-4-ferrocenylbutanamido) propane-1-1-diylbis (phosphonate) (H6) exhibited higher cytotoxicity on A549 (IC50 = 28.15 µM) than cisplatin (IC50 = 58.28 µM), while its activity on HeLa cells (IC50 = 14.69 µM) was equivalent to that of cisplatin 15.10 µM (HeLa cells). H6 (IC50 = 95.58 µM) was also five times less toxic than cisplatin (IC50 = 20.86 µM) on fibroblast NIH3T3 suggesting that H6 can be a future replacement for cisplatin due to its non-toxicity to healthy cells. Interestingly, some ferrocene and bisphosphonate parent compounds exhibited promising anticancer activity with 4-ferrocenyl-4-oxobutanoic acid (FI) exhibiting higher cytotoxic activity (IC50 = 1.73 µM) than paclitaxel (IC50 = 3.5 µM) on A549 cell lines. F1 also exhibited lower cytotoxicity than paclitaxel and cisplatin on the normal murine fibroblast cell line (NIH3T3). The molecular docking studies showed H6 strong binding affinity for the STAT3 signaling pathway in A549 cell line, and the MAdCAM-1 and cellular tumor antigen p53 proteins in HeLa cell lines.
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    Polymer-Based Wound Dressing Materials Loaded with Bioactive Agents: Potential Materials for the Treatment of Diabetic Wounds
    (MDPI, 2021-02-14) Alven, S; Peter, S 0000-0002-6935-905X; Mbese, Z 0000-0002-7576-7754; Aderibigbe, Blessing A. 0000-0003-1157-7481
    Diabetic wounds are severe injuries that are common in patients that suffer from diabetes. Most of the presently employed wound dressing scaffolds are inappropriate for treating diabetic wounds. Improper treatment of diabetic wounds usually results in amputations. The shortcomings that are related to the currently used wound dressings include poor antimicrobial properties, inability to provide moisture, weak mechanical features, poor biodegradability, and biocompatibility, etc. To overcome the poor mechanical properties, polymer-based wound dressings have been designed from the combination of biopolymers (natural polymers) (e.g., chitosan, alginate, cellulose, chitin, gelatin, etc.) and synthetic polymers (e.g., poly (vinyl alcohol), poly (lactic-co-glycolic acid), polylactide, poly-glycolic acid, polyurethanes, etc.) to produce effective hybrid scaffolds for wound management. The loading of bioactive agents or drugs into polymer-based wound dressings can result in improved therapeutic outcomes such as good antibacterial or antioxidant activity when used in the treatment of diabetic wounds. Based on the outstanding performance of polymer-based wound dressings on diabetic wounds in the pre-clinical experiments, the in vivo and in vitro therapeutic results of the wound dressing materials on the diabetic wound are hereby reviewed.