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Antitumor And Anti Hiv Agents From Natural Products
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Book Synopsis Antitumor and Anti-HIV Agents from Natural Products by : Kyoko Nakagawa-Goto
Download or read book Antitumor and Anti-HIV Agents from Natural Products written by Kyoko Nakagawa-Goto and published by . This book was released on 2020-09-16 with total page 338 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cancer is the second leading cause of death worldwide, and was accountable for an estimated 9.6 million deaths in 2018. Nowadays, about 1 in 6 deaths in the world is due to cancer. Another major global public health issue is HIV. Over 70 million people have been infected with the HIV virus and about 35 million people have died of HIV-related illness, since the start of the epidemic. We have been fighting against these two serious diseases by finding successful treatments. The discovery of effective drugs is important for fighting cancer and HIV. Natural products, which are secondary metabolites produced by various living organisms, have been playing a principal role in drug discovery and developments, because of their structural and biological diversity. Many clinically used drugs have come from natural products; for example, more than 60% of anticancer drugs currently in clinical use are derived from natural sources. This Special Issue aims to collect original research and review articles focusing on notable and recent contributions to the discovery and development of novel anticancer and anti-HIV drug candidates from natural sources. Up-to-date knowledge from various research fields is welcome. This could be of great interest for scientists working in different research areas, such as natural product chemistry, including isolation and structural elucidation; phytochemistry; medicinal chemistry, including chemically modified natural compounds with improved biological activity; pharmacology; molecular biology; mechanisms of action study using natural products or related compounds; pharmacognosy, etc. Biological studies of natural extracts without an appropriate chemical characterization may not be considered.
Book Synopsis Natural Products as Antiviral Agents by : C.K. Chu
Download or read book Natural Products as Antiviral Agents written by C.K. Chu and published by Springer Science & Business Media. This book was released on 2013-11-11 with total page 279 pages. Available in PDF, EPUB and Kindle. Book excerpt: During the past fifty years, thousands of natural products have been isolated from plants, fungi, and bacteria. Apart from intense searches by pharmaceutical companies for medicinals and the concentrated effort mounted by the National Cancer Institute, many of these have not been tested in biological systems. The major reasons for this appear to be, at least, twofold. First, individual researchers looking for biologically active natural products will often isolate only small amounts of material sufficient to determine a structure and calculate the specific activity for their particular bioassay systems: insufficient funds preclude re-isolating the compound unless industrial potential is foreseen. Second, the difficulty with which original structures were proved prior to 1972. This required the isolation of relatively large quantities of a natural product and there followed extensive degradation, elemental analyses of the parent and its fragments, then synthesis, piece by piece, of the molecule. All this took time and energy. No wonder that when the structure was proved the chemist was enervated. And coupled to this was the fact that many chemists were not trained to test their materials in biological systems. In contrast, today a natural product can be isolated, its mass and molecular formula determined and, if there is some serendipity, crystals may be obtained for single crystal x-ray analysis. If conditions are near perfect, it is possible to isolate and identify a novel compound in a month.
Book Synopsis Medicinal Chemistry of Bioactive Natural Products by : Xiao-Tian Liang
Download or read book Medicinal Chemistry of Bioactive Natural Products written by Xiao-Tian Liang and published by John Wiley & Sons. This book was released on 2006-03-17 with total page 482 pages. Available in PDF, EPUB and Kindle. Book excerpt: Current discoveries and research into bioactive natural products Medicinal Chemistry of Bioactive Natural Products provides a much-needed survey of bioactive natural products and their applications in medicinal chemistry. This comprehensive reference features articles by some of the world's leading scientists in the field on discovery, structure elucidation, and elegant synthetic strategies--developed for natural products--with an emphasis on the structure activity relationship of bioactive natural products. The topics have been carefully chosen on the basis of relevance to current research and to importance as clinicially useful agents. Rather than attempting to be a comprehensive encyclopedia of bioactive natural products, Medicinal Chemistry of Bioactive Natural Products guides the reader to the key developments in the field. By providing not only practical detail but a historical perspective on the chemistry and biology of the compounds under consideration, the book serves as a handy resource for researchers in their own work developing pharmaceuticals, and as an inspiring introduction for young scientists to the dynamic field of bioactive natural products research. Enhanced by examples with updated research results, the discussion covers such topics as: * The chemistry and biology of epothilones * Vancomycin and other glycopeptide antibiotic derivates * Antitumor and other related activities of Taxol and its analogs * The antimalarial properties of the traditional Chinese medicine, Quinghaosu (artemisinin) * Huperzine A: A natural drug for the treatment of Alzheimer's disease * The medicinal chemistry of ginkgolides from Ginkgo biloba * Recent progress in Calophyllum coumarins as potent anti-HIV agents * Plant-derived anti-HIV agents and analogs * Chemical synthesis of annonaceous acetogenins and their structurally modified mimics
Book Synopsis Total Syntheses of Anti-HIV Natural Product Daurichromenic Acid, Rhododaurichromanic Acids A and B ; Syntheses of Anticancer Natural Product OSW-1 and Its Analogs ; and Studies Toward the Total Synthesis of Anticancer Natural Products Superstolide A by : Ying Kang
Download or read book Total Syntheses of Anti-HIV Natural Product Daurichromenic Acid, Rhododaurichromanic Acids A and B ; Syntheses of Anticancer Natural Product OSW-1 and Its Analogs ; and Studies Toward the Total Synthesis of Anticancer Natural Products Superstolide A written by Ying Kang and published by . This book was released on 2005 with total page 434 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Chemical Synthesis of Anti-HIV Compounds Based on the Aryl Naphthalene Lignans Identified from Justicia Plants by : Wanfei Li
Download or read book Chemical Synthesis of Anti-HIV Compounds Based on the Aryl Naphthalene Lignans Identified from Justicia Plants written by Wanfei Li and published by . This book was released on 2019 with total page 241 pages. Available in PDF, EPUB and Kindle. Book excerpt: Background: Natural products have been a rich source for the discovery of lead compounds in modern drug discovery. 6,7’-Cyclolignans are a class of secondary metabolites which are widely distributed in more than 20 families. This important class of lignans continue to attract the interest of the pharmaceutical industry owing to their remarkable biological benefits, particularly for their anti-tumor and antiviral properties. Arylnaphthalene lignans (ANLs) belong to 6,7’-cyclolignans which contain a 2,3-dimethyl-1-phenyl-naphthalene core structure. ANLs are widely distributed in plants. Justicia cf. patentiflora was identified as an anti-HIV (human immunodeficiency virus) plant lead through the screening of more than 3,500 plant extracts. Bioassay-directed fractionation of the methanol extract of the stems and barks of this plant has led to the isolation of three ANL glycoside compounds, which displayed potent inhibitory activity against broad HIV clinical strains with EC50 values in the range of 14-37 nM [Zidovudine (AZT): 77-95 nM]. They also showed significant inhibitory effects against drug-resistance HIV strains. Thus, the ANL glycosides have high potential as lead molecules for the development of new therapeutic drugs for HIV/AIDS. Objectives: 1) To establish an efficient route for the total synthesis of ANL compounds and to synthesize a library of ANL compounds through the established total synthetic approach; 2) To evaluate the cytotoxicities and anti-HIV activities of the synthesized ANLs; 3) To elucidate the structure activity relationship (SAR) of ANLs as a basis for the optimization of drug efficacy, improvement of pharmacokinetic properties as well as minimization of the toxicity of ANLs; 4) To synthesize potent anti-HIV ANL molecules with high selectivity. Methods: To achieve these objectives, a synthetic route for ANL was designed and a broad series of ANL derivatives were synthesized via modifications of rings A and B, as well as the functionalities at C-7. The synthesized compounds had been evaluated for their toxicity and antiviral activities. Cytotoxicity was determined using the SRB (Sulforhodamine B) assay, while anti-HIV activity was evaluated by utilizing the “One-Stone-Two-Birds” protocol. Results: We have accomplished the total synthesis of the key intermediate diphyllin with more than 20 g. Our modification of ANL derivatives focused on substitutions, additions and different configurations of the C-7 position, ring A and ring B. Specifically, the different structural components of the ANLs were systematically modified, resulting in the formation of six groups of compounds. A total of 72 ANL compounds with various functional groups were synthesized. Their structures have been confirmed by the MS and NMR spectral data. All the synthesized ANL compounds were purified to have purity ≥ 95%. The SAR of ANL compounds was revealed based on the analysis of the antiviral and cytotoxicity data of these synthetic analogues. After structural modification, all the modified derivatives based on rings A and B (groups 1 and 2) showed activity reduction in terms of both cytotoxic and anti-HIV activities. However, the modification of C-7 yielded divergent results, which included the groups of 3-6. Most compounds in groups 3-5 displayed comparable inhibitory effect with diphyllin (5). Group 6 represents the largest number of analogues among the six groups. In this group, the stereochemical properties and functionalization of the hydroxy groups on the sugar units are essential for their activities. Among these series of derivatives, compound 17b showed significant high potency of anti-HIV activity with an EC50 value of 2.6 nM and SI of 815. Conclusion: Using the synthesized diphyllin as the key intermediate, a compound library of 72 ANL derivatives was obtained. These compounds have been evaluated for their cytotoxicity and anti-HIV activity. Our bioactivity data revealed that the functionalization of the C-7 hydroxy group could significantly reduce the cytotoxicity and increase anti-HIV activity, while the modification on rings A and B would rather result in the reduction of both cytotoxicity and anti-HIV activity. Subsequently, novel diphyllin glycosides containing various sugar moieties were further synthesized. Several of these ANL analogues showed high anti-HIV activity with EC50 values in the nM range and low cytotoxicity (selective indices > 500). Future Perspective: This study clearly suggests ANLs as anti-HIV lead compounds and they have high potential to be developed as therapeutic drugs for the treatment of HIV. To further confirm the antiviral potential of ANLs, live HIV strains including some drug resistant strains should be further investigated. Although our data have shown that the ANL compounds are targeting the viral post-entry stages, their antiviral molecular targets are still unknown. However, since our SAR information has clearly revealed that the substitution of rings A and B are not involve in the antiviral activity for enhancing ANL compounds, the carbon positions in these rings may be explored to link a biotin unit, which can be used as a viable approach to pull down the antiviral target proteins of ANLs. Once the target proteins are identified, molecular docking is then made possible for a rational synthetic design to fine tune the chemical structures of ANLs in order to improve their antiviral properties such as high antiviral activity, low toxicity and enhanced water solubility. A further step to advance ANLs as anti-HIV drugs is the investigation of their drug properties in in vivo studies including the assessment of their anti-HIV efficacy in the rhesus model as well as obtaining their pharmacokinetic and safety parameters. These studies will help to provide more evidence about the anti-viral properties of ANLs
Book Synopsis Antitumor Potential and other Emerging Medicinal Properties of Natural Compounds by : Evandro Fei Fang
Download or read book Antitumor Potential and other Emerging Medicinal Properties of Natural Compounds written by Evandro Fei Fang and published by Springer Science & Business Media. This book was released on 2013-02-26 with total page 422 pages. Available in PDF, EPUB and Kindle. Book excerpt: The modern unhealthy diet and lifestyle in conjunction with pathogens, environmental carcinogens and multiple other risk factors increase humans’ susceptibility to different diseases exemplified by elevated levels of cancers, cardiovascular and communicable diseases. Screening of potential drugs from medicinal plants and animals provides a promising strategy for the alleviation of the impact of these diseases. Components with potential medicinal applications include RIPs, RNases, lectins, protease inhibitors and numerous small compounds. These compounds have shown both preventive and therapeutic effects for humans. This book is a compilation of articles written by internationally renowned experts exploring the different uses of medicinal compounds in human therapeutics. Here we provide a comprehensive outlook on both qualitative and quantitative studies focusing on medicinal plants and animals, and establishing a link between laboratory research discovery and clinical applications.
Book Synopsis Pharmacologically Active Bioproducts by : Vivek Kothari
Download or read book Pharmacologically Active Bioproducts written by Vivek Kothari and published by Daya Books. This book was released on 2007-03 with total page 268 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nature Has Continuously Provided Mankind With A Broad And Structurally Diverse Array Of Pharmacologically Active Compounds That Have Proved To Be Indispensable For The Cure Of Deadly Diseases Or As Lead Structures For Novel Pharmaceuticals. The Importance Of Natural Bioproducts Can Be Realised From Their Prominence In The Over-The-Counter And Prescription Drug Market. The Pharmaceutical Industry Continues To Examine Their Potential As Sources Of Novel Medicinal Compounds To Identify Novel Growth Factor, Immuno-Modulatory And Potential Anti-Microbial Activity. With The Progress Of New Technologies, New Avenues Were Opened To Purify Active Components From Natural Products, To Establish Their Chemical Structure, And Even To Synthesize And/Or Modify Them Chemically. This Book Is Intended To Furnish The Reader With Vital Information On Pharmacologically Active Bioproducts. It Is Hoped That This Book Will Encourage Further Research And Understanding Of All Aspects Of This Intriguing And Complex Field. Contents Chapter 1: Natural Product As Therapeutic Agents; Chapter 2: Isolation Of Bioproducts; Chapter 3: Pharmacopoeial Medicinal Plants; Chapter 4: Pharmacologically Active Marine Products; Chapter 5: Anti-Hiv Bioproducts; Chapter 6: Use Of Pharmacologically Active Bioproducts In Cancer Treatment; Chapter 7: Bioactive Natural Product In The Treatment Of Gastrointestinal Diseases; Chapter 8: Amphiphilic Phenols As Bioactive Compounds; Chapter 9: Herbal Products For Controlling Mosquito Vectors; Chapter 10: Risk Management For Pharamaceutical Compounds; Chapter 11: Pharmaceuticals: Liabilities And Regulatory Concerns.
Book Synopsis Medicinal Chemistry of Anticancer Drugs by : Carmen Avendaño
Download or read book Medicinal Chemistry of Anticancer Drugs written by Carmen Avendaño and published by Elsevier. This book was released on 2015-06-11 with total page 767 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design. Presents information in a clear and concise way using a large number of figures Historical background provides insights on how the process of drug discovery in the anticancer field has evolved Extensive references to primary literature
Book Synopsis Phytochemistry of Medicinal Plants by : John T. Arnason
Download or read book Phytochemistry of Medicinal Plants written by John T. Arnason and published by Springer Science & Business Media. This book was released on 2013-11-11 with total page 369 pages. Available in PDF, EPUB and Kindle. Book excerpt: Phytochemicals from medicinal plants are receiving ever greater attention in the scientific literature, in medicine, and in the world economy in general. For example, the global value of plant-derived pharmaceuticals will reach $500 billion in the year 2000 in the OECD countries. In the developing countries, over-the-counter remedies and "ethical phytomedicines," which are standardized toxicologically and clinically defined crude drugs, are seen as a promising low cost alternatives in primary health care. The field also has benefited greatly in recent years from the interaction of the study of traditional ethnobotanical knowledge and the application of modem phytochemical analysis and biological activity studies to medicinal plants. The papers on this topic assembled in the present volume were presented at the annual meeting of the Phytochemical Society of North America, held in Mexico City, August 15-19, 1994. This meeting location was chosen at the time of entry of Mexico into the North American Free Trade Agreement as another way to celebrate the closer ties between Mexico, the United States, and Canada. The meeting site was the historic Calinda Geneve Hotel in Mexico City, a most appropriate site to host a group of phytochemists, since it was the address of Russel Marker. Marker lived at the hotel, and his famous papers on steroidal saponins from Dioscorea composita, which launched the birth control pill, bear the address of the hotel.
Book Synopsis Anticancer Agents from Natural Products by : Gordon M. Cragg
Download or read book Anticancer Agents from Natural Products written by Gordon M. Cragg and published by CRC Press. This book was released on 2005-06-13 with total page 610 pages. Available in PDF, EPUB and Kindle. Book excerpt: Plants, marine organisms, and microorganisms have evolved complex chemical defense and signaling systems that are designed to protect them from predators and provide other biological benefits. These organisms thus produce substances containing novel chemotypes that may have beneficial effects for humans. As collection methods improve and new screen
Book Synopsis Bioactive Compounds from Plants by : Derek J. Chadwick
Download or read book Bioactive Compounds from Plants written by Derek J. Chadwick and published by John Wiley & Sons. This book was released on 2008-04-30 with total page 254 pages. Available in PDF, EPUB and Kindle. Book excerpt: Useful throughout history for their medical as well as other benefits, plant-derived compounds have gained particular importance recently, due to environmental factors. The isolation and characterization of plant products, the identification of their role in the plant, and ways of synthesizing identical compounds or more potent analogues are covered. Also includes methods of culturing plant tissues and genetic engineering as a means of increasing the yield of desired substances from plants. Special emphasis is placed on plants previously unknown to Western scientists.
Book Synopsis Bioactive Natural Products by : Steven M. Colegate
Download or read book Bioactive Natural Products written by Steven M. Colegate and published by CRC Press. This book was released on 2007-12-14 with total page 624 pages. Available in PDF, EPUB and Kindle. Book excerpt: Bioactive natural products are proving to be a rich source of novel therapeutics to both protect against and combat diseases, as well as serve as lead compounds in crop protection. Following the successful format of the first edition, this volume brings together collective research from many new contributors and emphasizes the rationale behind the
Book Synopsis Biotechnology of Isoprenoids by : Jens Schrader
Download or read book Biotechnology of Isoprenoids written by Jens Schrader and published by Springer. This book was released on 2015-05-19 with total page 470 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book review series presents current trends in modern biotechnology. The aim is to cover all aspects of this interdisciplinary technology where knowledge, methods and expertise are required from chemistry, biochemistry, microbiology, genetics, chemical engineering and computer science. Volumes are organized topically and provide a comprehensive discussion of developments in the respective field over the past 3-5 years. The series also discusses new discoveries and applications. Special volumes are dedicated to selected topics which focus on new biotechnological products and new processes for their synthesis and purification. In general, special volumes are edited by well-known guest editors. The series editor and publisher will however always be pleased to receive suggestions and supplementary information. Manuscripts are accepted in English.
Book Synopsis Biomedical Index to PHS-supported Research by :
Download or read book Biomedical Index to PHS-supported Research written by and published by . This book was released on 1987 with total page 1398 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Biomedical Index to PHS-supported Research: pt. A. Subject access A-H by :
Download or read book Biomedical Index to PHS-supported Research: pt. A. Subject access A-H written by and published by . This book was released on 1992 with total page 1064 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Biologically Active Natural Products by : Stephen J. Cutler
Download or read book Biologically Active Natural Products written by Stephen J. Cutler and published by CRC Press. This book was released on 1999-07-27 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: Biologically Active Natural Products: Pharmaceuticals demonstrates the connections between agrochemicals and pharmaceuticals and explores the use of plants and plant products in the formulation and development of pharmaceuticals. Experts from around the world examine a multitude of topics, including evaluation of extracts from tropical plants for p
Download or read book Natural Products written by Lixin Zhang and published by Springer Science & Business Media. This book was released on 2007-11-17 with total page 380 pages. Available in PDF, EPUB and Kindle. Book excerpt: A fresh examination of the past successes of natural products as medicines and their new future from both conventional and new technologies. High-performance liquid chromatography profiling, combinatorial synthesis, genomics, proteomics, DNA shuffling, bioinformatics, and genetic manipulation all now make it possible to rapidly evaluate the activities of extracts as well as purified components derived from microbes, plants, and marine organisms. The authors apply these methods to new natural product drug discoveries, to microbial diversity, to specific groups of products (Chinese herbal drugs, antitumor drugs from microbes and plants, terpenoids, and arsenic compounds), and to specific sources (the sea, rainforest, and endophytes). These new opportunities show how research and development trends in the pharmaceutical industry can advance to include both synthetic compounds and natural products, and how this paradigm shift can be more productive and efficacious.
