Highlights• Cancer is second deadly disease after cardiovascular diseases.• There is a tremendous need to discover novel safer and more effective anticancer agents.• Plants serve as a basis for promising therapeutic agents for cancer treatment.• Important plant derived anticancer agents have been discussed here.• Some potential plant derived lead molecules have also been discussed. *Corresponding author:Centre for Microbial Ecology and Genomics, Graphical abstract
This review attempts to portray the discovery and development of anticancer agents/drugs from diverse natural sources. Natural molecules from these natural sources including plants, microbes and marine organisms have been the basis of treatment of human diseases since the ancient times. Compounds derived from nature have been important sources of new drugs and also serve as templates for synthetic modification. Many successful anti-cancer drugs currently in use are naturally derived or their analogues and many more are under clinical trials. This review aims to highlight the invaluable role that natural products have played, and continue to play, in the discovery of anticancer agents.
Cell wall mycolic acids (MA) from Mycobacterium tuberculosis (M.tb) are CD1b presented antigens that can be used to detect antibodies as surrogate markers of active TB, even in HIV coinfected patients. The use of the complex mixtures of natural MA is complicated by an apparent antibody cross-reactivity with cholesterol. Here firstly we report three recombinant monoclonal scFv antibody fragments in the chicken germ-line antibody repertoire, which demonstrate the possibilities for cross-reactivity: the first recognized both cholesterol and mycolic acids, the second mycolic acids but not cholesterol, and the third cholesterol but not mycolic acids. Secondly, MA structure is experimentally interrogated to try to understand the cross-reactivity. Unique synthetic mycolic acids representative of the three main functional classes show varying antigenicity against human TB patient sera, depending on the functional groups present and on their stereochemistry. Oxygenated (methoxy- and keto-) mycolic acid was found to be more antigenic than alpha-mycolic acids. Synthetic methoxy-mycolic acids were the most antigenic, one containing a trans-cyclopropane apparently being somewhat more antigenic than the natural mixture. Trans-cyclopropane-containing keto- and hydroxy-mycolic acids were also found to be the most antigenic among each of these classes. However, none of the individual synthetic mycolic acids significantly and reproducibly distinguished the pooled serum of TB positive patients from that of TB negative patients better than the natural mixture of MA. This argues against the potential to improve the specificity of serodiagnosis of TB with a defined single synthetic mycolic acid antigen from this set, although sensitivity may be facilitated by using a synthetic methoxy-mycolic acid.
Malaria is one of the oldest infectious diseases that afflict humans and its history extends back for millennia. It was once prevalent throughout the globe but today it is mainly endemic to tropical regions like sub-Saharan Africa and Southeast Asia. Ironically, treatment for malaria has existed for centuries yet it still exerts an enormous death toll. This contradiction is attributed in part to the rapid development of resistance by the malaria parasite to chemotherapeutic drugs. In turn, resistance has been fuelled by poor patient compliance to the relatively toxic antimalarial drugs. While drug toxicity and poor pharmacological potentials have been addressed or ameliorated with various nanomedicine drug delivery systems in diseases like cancer, no clinically significant success story has been reported for malaria. There have been several reviews on the application of nanomedicine technologies, especially drug encapsulation, to malaria treatment. Here we extend the scope of the collation of the nanomedicine research literature to polymer therapeutics technology. We first discuss the history of the disease and how a flurry of scientific breakthroughs in the latter part of the nineteenth century provided scientific understanding of the disease. This is followed by a review of the disease biology and the major antimalarial chemotherapy. The achievements of nanomedicine in cancer and other infectious diseases are discussed to draw parallels with malaria. A review of the current state of the research into malaria nanomedicines, both encapsulation and polymer therapeutics polymer-drug conjugation technologies, is covered and we conclude with a consideration of the opportunities and challenges offered by both technologies.
Although the implementation of blended learning in organic chemistry is rapidly growing, thus far, there are few studies published on the evaluation of supplemental types of blend in organic chemistry. This report covers a phenomenographic study that was designed to evaluate a supplemental type of blended learning approach implemented in a second-year organic chemistry course in a South African context. It offers a unique contribution in terms of catering to the needs of a diverse student body. Three open-ended questionnaires were used to probe: (1) students’ perceptions of the learning support; (2) students’ preferences for different types of learning support offered; and (3) students’ suggestions for improvement. Semi-structured individual interviews were used to obtain clarity on some of the responses from the questionnaires. Analysis of students’ responses revealed that the face-to-face component was highly valued as it gave the students the opportunity to ask questions and obtain answers in real time; the online component, especially Learnsmart, was found helpful for its flexibility and providing limitless opportunities to practice or revisit concepts. The discussion board was the least valued due to the overwhelming number of postings, and the students felt they were forced to participate in order to get marks. The students experienced the course as too fast-paced possibly reflecting cognitive overload, a potential weakness of the supplemental blend. The findings will be useful in many other contexts where the student body is diverse in terms of language proficiency and the level of preparation for the demands of organic chemistry as a discipline.
Moxifloxacin was conjugated to polyethylene glycol to segregate host cell toxicity from antimicrobial activity. The conjugate was then encapsulated into a polycaprolactone nanoparticle to assist the simultaneous delivery of multiple drugs to the site of microbial infection.
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