The role played by cinnamic acid derivatives in treating cancer, bacterial infections, diabetes and neurological disorders, among many, has been reported. Cinnamic acid is obtained from cinnamon bark. Its structure is composed of a benzene ring, an alkene double bond and an acrylic acid functional group making it possible to modify the aforementioned functionalities with a variety of compounds resulting in bioactive agents with enhanced efficacy. The nature of the substituents incorporated into cinnamic acid has been found to play a huge role in either enhancing or decreasing the biological efficacy of the synthesized cinnamic acid derivatives. Some of the derivatives have been reported to be more effective when compared to the standard drugs used to treat chronic or infectious diseases in vitro, thus making them very promising therapeutic agents. Compound 20 displayed potent anti-TB activity, compound 27 exhibited significant antibacterial activity on S. aureus strain of bacteria and compounds with potent antimalarial activity are 35a, 35g, 35i, 36i, and 36b. Furthermore, compounds 43d, 44o, 55g–55p, 59e, 59g displayed potent anticancer activity and compounds 86f–h were active against both hAChE and hBuChE. This review will expound on the recent advances on cinnamic acid derivatives and their biological efficacy.
Wound management remains a challenge worldwide, although there are several developed wound dressing materials for the management of acute and chronic wounds. The wound dressings that are currently used include hydrogels, films, wafers, nanofibers, foams, topical formulations, transdermal patches, sponges, and bandages. Hydrogels exhibit unique features which make them suitable wound dressings such as providing a moist environment for wound healing, exhibiting high moisture content, or creating a barrier against bacterial infections, and are suitable for the management of exuding and granulating wounds. Biopolymers have been utilized for their development due to their non-toxic, biodegradable, and biocompatible properties. Hydrogels have been prepared from biopolymers such as cellulose and chitosan by crosslinking with selected synthetic polymers resulting in improved mechanical, biological, and physicochemical properties. They were useful by accelerating wound re-epithelialization and also mimic skin structure, inducing skin regeneration. Loading antibacterial agents into them prevented bacterial invasion of wounds. This review article is focused on hydrogels formulated from two biopolymers—chitosan and cellulose—for improved wound management.
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.
Ursolic acid is a pharmacologically active pentacyclic triterpenoid derived from medicinal plants, fruit, and vegetables. The pharmacological activities of ursolic acid have been extensively studied over the past few years and various reports have revealed that ursolic acid has multiple biological activities, which include anti-inflammatory, antioxidant, anti-cancer, etc. In terms of cancer treatment, ursolic acid interacts with a number of molecular targets that play an essential role in many cell signaling pathways. It suppresses transformation, inhibits proliferation, and induces apoptosis of tumor cells. Although ursolic acid has many benefits, its therapeutic applications in clinical medicine are limited by its poor bioavailability and absorption. To overcome such disadvantages, researchers around the globe have designed and developed synthetic ursolic acid derivatives with enhanced therapeutic effects by structurally modifying the parent skeleton of ursolic acid. These structurally modified compounds display enhanced therapeutic effects when compared to ursolic acid. This present review summarizes various synthesized derivatives of ursolic acid with anti-cancer activity which were reported from 2015 to date.
Some of the currently used wound dressings have interesting features such as excellent porosity, good water-absorbing capacity, moderate water vapor transmission rate, high drug loading efficiency, and good capability to provide a moist environment, but they are limited in terms of antimicrobial properties. Their inability to protect the wound from microbial invasion results in wound exposure to microbial infections, resulting in a delayed wound healing process. Furthermore, some wound dressings are loaded with synthetic antibiotics that can cause adverse side effects on the patients. Natural-based compounds exhibit unique features such as good biocompatibility, reduced toxicity, etc. Curcumin, one such natural-based compound, has demonstrated several biological activities such as anticancer, antibacterial and antioxidant properties. Its good antibacterial and antioxidant activity make it beneficial for the treatment of wounds. Several researchers have developed different types of polymer-based wound dressings which were loaded with curcumin. These wound dressings displayed excellent features such as good biocompatibility, induction of skin regeneration, accelerated wound healing processes and excellent antioxidant and antibacterial activity. This review will be focused on the in vitro and in vivo therapeutic outcomes of wound dressings loaded with curcumin.
Malaria is a vector- and blood-borne infection that is responsible for a large number of deaths around the world. Most of the currently used antimalarial therapeutics suffer from drug resistance. The other limitations associated with the currently used antimalarial drugs are poor drug bioavailability, drug toxicity, and poor water solubility. Combination therapy is one of the best approaches that is currently used to treat malaria, whereby two or more therapeutic agents are combined. Different combination therapy strategies are used to overcome the aforementioned limitations. This review article reports two strategies of combination therapy; the incorporation of two or more antimalarials into polymer-based carriers and hybrid compounds designed by hybridization of two antimalarial pharmacophores.
Wound care is a major biomedical field that is challenging due to the delayed wound healing process. Some factors are responsible for delayed wound healing such as malnutrition, poor oxygen flow, smoking, diseases (such as diabetes and cancer), microbial infections, etc. The currently used wound dressings suffer from various limitations, including poor antimicrobial activity, etc. Wound dressings that are formulated from biopolymers (e.g., cellulose, chitin, gelatin, chitosan, etc.) demonstrate interesting properties, such as good biocompatibility, non-toxicity, biodegradability, and attractive antimicrobial activity. Although biopolymer-based wound dressings display the aforementioned excellent features, they possess poor mechanical properties. Gelatin, a biopolymer has excellent biocompatibility, hemostatic property, reduced cytotoxicity, low antigenicity, and promotes cellular attachment and growth. However, it suffers from poor mechanical properties and antimicrobial activity. It is crosslinked with other polymers to enhance its mechanical properties. Furthermore, the incorporation of antimicrobial agents into gelatin-based wound dressings enhance their antimicrobial activity in vitro and in vivo. This review is focused on the development of hybrid wound dressings from a combination of gelatin and other polymers with good biological, mechanical, and physicochemical features which are appropriate for ideal wound dressings. Gelatin-based wound dressings are promising scaffolds for the treatment of infected, exuding, and bleeding wounds. This review article reports gelatin-based wound dressings which were developed between 2016 and 2021.
Dendrimers are drug delivery systems that are characterized by a three-dimensional, star-shaped, branched macromolecular network. They possess ideal properties such as low polydispersity index, biocompatibility and good water solubility. They are made up of the interior and the exterior layers. The exterior layer consists of functional groups that are useful for conjugation of drugs and targeting moieties. The interior layer exhibits improved drug encapsulation efficiency, reduced drug toxicity, and controlled release mechanisms. These unique properties make them useful for drug delivery. Dendrimers have attracted considerable attention as drug delivery system for the treatment of infectious diseases. The treatment of infectious diseases is hampered severely by drug resistance. Several properties of dendrimers such as their ability to overcome drug resistance, toxicity and control the release mechanism of the encapsulated drugs make them ideal systems for the treatment of infectious disease. The aim of this review is to discuss the potentials of dendrimers for the treatment of viral and parasitic infections.
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