Cancer is a life-threatening disease and is the second leading cause of death around the world. The increasing threats of drug-resistant cancers indicate that there is an urgent need for the improvement or development of more effective anticancer agents. Curcumin, a phenolic compound originally derived from turmeric plant (Curcuma longa L. (Zingiberaceae family)) widely known as a spice and a coloring agent for food have been reported to possess notable anticancer activity by inhibiting the proliferation and metastasis, and enhancing cell cycle arrest or apoptosis in various cancer cells. In spite of all these benefits, the therapeutic application of curcumin in clinical medicine and its bioavailability are still limited due to its poor absorption and rapid metabolism. Structural modification of curcumin through the synthesis of curcumin-based derivatives is a potential approach to overcome the above limitations. Curcumin derivatives can overcome the disadvantages of curcumin while enhancing the overall efficacy and hindering drug resistance. This article reports a review of published curcumin derivatives and their enhanced anticancer activities.
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.
Skin regeneration after an injury is very vital, but this process can be impeded by several factors. Regenerative medicine is a developing biomedical field with the potential to decrease the need for an organ transplant. Wound management is challenging, particularly for chronic injuries, despite the availability of various types of wound dressing scaffolds in the market. Some of the wound dressings that are in clinical practice have various drawbacks such as poor antibacterial and antioxidant efficacy, poor mechanical properties, inability to absorb excess wound exudates, require frequent change of dressing and fails to offer a suitable moist environment to accelerate the wound healing process. Collagen is a biopolymer and a major constituent of the extracellular matrix (ECM), making it an interesting polymer for the development of wound dressings. Collagen-based nanofibers have demonstrated interesting properties that are advantageous both in the arena of skin regeneration and wound dressings, such as low antigenicity, good biocompatibility, hemostatic properties, capability to promote cellular proliferation and adhesion, and non-toxicity. Hence, this review will discuss the outcomes of collagen-based nanofibers reported from the series of preclinical trials of skin regeneration and wound healing.
Metastatic bone cancer occurs in every type of cancer but is prevalent in lung, breast, and prostate cancers. These metastases can cause extensive morbidity, including a range of skeletal-related events, often painful and linked with substantial hospital resource usage. The treatment used is a combination of chemotherapy and surgery. However, anticancer drugs are still limited due to severe side effects, drug resistance, poor blood supply, and non-specific drug uptake, necessitating high toxic doses. Bisphosphonates are the main class of drugs utilized to inhibit metastatic bone cancer. It is also used for the treatment of osteoporosis and other bone diseases. However, bisphosphonate also suffers from serious side effects. Thus, there is a serious need to develop bisphosphonate conjugates with promising therapeutic outcomes for treating metastatic bone cancer and osteoporosis. This review article focuses on the biological outcomes of designed bisphosphonate-based conjugates for the treatment of metastatic bone cancer and osteoporosis.
Background: The design of hybrid compounds is a distinct approach to developing potent bioactive agents. Carvacrol, an essential oil exhibit antimicrobial, antifungal, antioxidant and anticancer activity, making it a good precursor for the development of compounds with potent biological activities. Some patents have reported carvacrol derivatives with promising biological activities. Objective: To prepare hybrid compounds containing carvacrol scaffold with significant antibacterial and anticancer activity. Methods: Esterification reactions between carvacrol and known pharmacophores were performed at room temperature and characterized using 1H-NMR, 13C-NMR and UHPLC-HRMS. In vitro antibacterial and cytotoxicity evaluations were performed. Results: The FTIR spectra of the carvacrol hybrids revealed prominent bands in the range of 1612-1764 cm-1 and 1014-1280 cm-1 due to (C=O) and (C-O) stretching vibrations, respectively. The structures of the carvacrol hybrids were confirmed by 1H-NMR, 13C-NMR and UHPLC-HRMS analysis. The antibacterial activity was determined using the microdilution assay and compound 5 exhibited superior activity when compared to the hybrid compounds against the strains of bacteria used in the study. The in vitro cytotoxicity evaluation showed that compound 3 induced cytotoxicity in all the cancer cell lines; MDA (16.57 ± 1.14 µM), MCF-7 (0.47 ± 1.14 µM) and DU145 (16.25 ± 1.08 µM) as well as the normal breast cells, MCF-12A (0.75± 1.30 µM). Compound 7 did not induce cytotoxicity in the cell lines tested (IC50 > 200 µM). Conclusion: The modification of carvacrol through hybridization is a promising approach to develop compounds with significant antibacterial and anticancer activity.
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