scholarly journals Structure-Activity-Relationship and Mechanistic Insights for Anti-HIV Natural Products

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2070
Author(s):  
Ramandeep Kaur ◽  
Pooja Sharma ◽  
Girish K. Gupta ◽  
Fidele Ntie-Kang ◽  
Dinesh Kumar

Acquired Immunodeficiency Syndrome (AIDS), which chiefly originatesfroma retrovirus named Human Immunodeficiency Virus (HIV), has impacted about 70 million people worldwide. Even though several advances have been made in the field of antiretroviral combination therapy, HIV is still responsible for a considerable number of deaths in Africa. The current antiretroviral therapies have achieved success in providing instant HIV suppression but with countless undesirable adverse effects. Presently, the biodiversity of the plant kingdom is being explored by several researchers for the discovery of potent anti-HIV drugs with different mechanisms of action. The primary challenge is to afford a treatment that is free from any sort of risk of drug resistance and serious side effects. Hence, there is a strong demand to evaluate drugs derived from plants as well as their derivatives. Several plants, such as Andrographis paniculata, Dioscorea bulbifera, Aegle marmelos, Wistaria floribunda, Lindera chunii, Xanthoceras sorbifolia and others have displayed significant anti-HIV activity. Here, weattempt to summarize the main results, which focus on the structures of most potent plant-based natural products having anti-HIV activity along with their mechanisms of action and IC50 values, structure-activity-relationships and important key findings.

Author(s):  
Ramanpreet Kaur ◽  
Pooja Sharma ◽  
Girish K. Gupta ◽  
Fidele Ntie-Kang ◽  
Dinesh Kumar

Acquired Immunodeficiency Syndrome (AIDS) which is chiefly originated by a retrovirus named Human Immunodeficiency Virus (HIV), has influenced about 70 million populations worldwide. Even though several advancements have been invented in the field of antiretroviral combination therapy, still HIV has become the dominant reason for death in South Africa, for example. The current antiretroviral therapies have achieved success in providing instant HIV suppression but with countless undesirable adverse effects. In the present day, the biodiversity of the plant kingdom is being explored by several researchers for the discovery of potent anti-HIV drugs with different mechanisms of action. The primary challenge is to afford a treatment that is free from any sort of risk of drug resistance and serious side effects. Hence, there is a strong demand to evaluate the drugs obtained from natural plants as well as the synthetic derivatives that have been derived from the natural compounds by various chemical reactions. Several plants such as Andrographis paniculata, Dioscorea bulbifera, Aegle marmelos, Wistaria floribunda, Lindera chunii, Xanthoceras sorbifolia and others have displayed significant anti-HIV activity showing more potent anti-HIV activity along with their structures, SARs & important key findings.


1990 ◽  
Vol 80 (1) ◽  
pp. 21-25 ◽  
Author(s):  
B Newlin

Although significant advances have been made in the treatment of acquired immunodeficiency syndrome (AIDS), neither a curative therapy nor a vaccine is available. Protecting practitioners, medical staff members, and patients from infection with human immunodeficiency virus (HIV) remains a particularly important issue. Fortunately, this virus is not readily transmitted in the health care setting. Adequate protection can be accomplished through the strict implementation of universal infection control policies in the treatment of all patients. Understanding these procedures, providing access to necessary equipment and supplies, and monitoring adherence to universal infection control measures will minimize the risk of exposure.


2020 ◽  
Vol 66 (2) ◽  
pp. 34-43
Author(s):  
Mohamed Amin El-Ansari ◽  
Lamyaa Fawzy Ibrahim ◽  
Mohamed Sharaf

Summary Acquired immunodeficiency syndrome (AIDS) is an immunosuppressive disease caused by human immunodeficiency virus (HIV). The urgent need for searching novel anti-HIV/AIDS medicines is a global concern. So far, a lot of medicinal and aromatic plants (MAPs) have been analyzed to select those that could assist in the prevention and/or amelioration of the disease. Among biologically active compounds present in these plants, one of the most promising group are phenolics. The purpose of this article was to report anti-HIV activity of selected phenolic compounds of plant origin.


2021 ◽  
Vol 12 ◽  
Author(s):  
Chengchao Ding ◽  
Darshit Patel ◽  
Yunjing Ma ◽  
Jamie F. S. Mann ◽  
Jianjun Wu ◽  
...  

Despite the discovery that the human immunodeficiency virus 1 (HIV-1) is the pathogen of acquired immunodeficiency syndrome (AIDS) in 1983, there is still no effective anti-HIV-1 vaccine. The major obstacle to the development of HIV-1 vaccine is the extreme diversity of viral genome sequences. Nonetheless, a number of broadly neutralizing antibodies (bNAbs) against HIV-1 have been made and identified in this area. Novel strategies based on using these bNAbs as an efficacious preventive and/or therapeutic intervention have been applied in clinical. In this review, we summarize the recent development of bNAbs and its application in HIV-1 acquisition prevention as well as discuss the innovative approaches being used to try to convey protection within individuals at risk and being treated for HIV-1 infection.


2019 ◽  
Vol 19 (6) ◽  
pp. 510-526 ◽  
Author(s):  
Nisha Chokkar ◽  
Sourav Kalra ◽  
Monika Chauhan ◽  
Raj Kumar

After restricting the proliferation of CD4+T cells, Human Immunodeficiency Virus (HIV), infection persists at a very fast rate causing Acquired Immunodeficiency Syndrome (AIDS). This demands the vigorous need of suitable anti-HIV agents, as existing medicines do not provide a complete cure and exhibit drawbacks like toxicities, drug resistance, side-effects, etc. Even the introduction of Highly Active Antiretroviral Therapy (HAART) failed to combat HIV/AIDS completely. The major breakthrough in anti-HIV discovery was marked with the discovery of raltegravir in 2007, the first integrase (IN) inhibitor. Thereafter, the discovery of elvitegravir, a quinolone derivative emerged as the potent HIV-IN inhibitor. Though many more classes of different drugs that act as anti-HIV have been identified, some of which are under clinical trials, but the recent serious focus is still laid on quinoline and its analogues. In this review, we have covered all the quinoline-based derivatives that inhibit various targets and are potential anti-HIV agents in various phases of the drug discovery.


2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Milena Mazalovska ◽  
J. Calvin Kouokam

Human immunodeficiency virus-acquired immunodeficiency syndrome (HIV/AIDS) remains a global health problem. Current therapeutics specifically target the viral pathogen at various stages of its life cycle, although complex interactions between HIV and other pathogenic organisms are evident. Targeting HIV and concomitant infectious pathogens simultaneously, both by therapeutic regimens and in prevention strategies, would help contain the AIDS pandemic. Lectins, a ubiquitous group of proteins that specifically bind glycosylated molecules, are interesting compounds that could be used for this purpose, with demonstrated anti-HIV properties. In addition, potential coinfecting pathogens, including other enveloped viruses, bacteria, yeasts and fungi, and protozoa, display sugar-coated macromolecules on their surfaces, making them potential targets of lectins. This review summarizes the currently available findings suggesting that lectins should be further developed to simultaneously fight the AIDS pandemic and concomitant infections in HIV infected individuals.


2003 ◽  
Vol 75 (2-3) ◽  
pp. 195-206 ◽  
Author(s):  
Roberto Di Santo ◽  
Roberta Costi ◽  
Marino Artico ◽  
E. Tramontano ◽  
P. La Colla ◽  
...  

Combination therapy using reverse transcriptase (RT) and protease (PR) inhibitors is currently the best clinical approach in combatting acquired immunodeficiency syndrome (AIDS), caused by infection from the human immunodeficiency virus type 1 (HIV-1). However, the emergence of resistant strains calls urgently for research on inhibitors of further viral targets such as integrase (IN), the enzyme that catalyzes the integration of the proviral DNA into the host chromosomes. Recently, we started studies on new IN inhibitors as analogs of natural products, characterized by one or two 3,4-dihydroxycinnamoyl moieties, which were proven to be IN inhibitors in vitro. Then, we designed and synthesized a number of derivatives sharing 3,4 dihydroxycinnamoyl groups, obtaining potent IN inhibitors active at submicromolar concentrations. Unfortunately, these derivatives lacked antiretroviral activity, probably owing to their high cytotoxicity. So we designed a number of 3,4,5-trihydroxycinnamoyl derivatives as less-cytotoxic IN inhibitors, which were proven to be antiretrovirals in cell-based assays. Finally, we designed and synthesized a number of aryldiketohexenoic acids, strictly related to the aryldiketo acid series recently reported by Merck Company, which were shown to be potent antiretroviral agents endowed with anti-IN activities either in 3' processing or in strand transfer steps.


2018 ◽  
Vol 7 ◽  
pp. 131
Author(s):  
Riry Febrina Ersha ◽  
Armen Ahmad

Acquired Immunodeficiency Syndrome (AIDS) adalah infeksi yang disebabkan oleh Human Immunodeficiency Virus (HIV) yang menyebabkan suatu penyakit yang menyerang sel-sel kekebalan tubuh. Sebuah temuan baru yang mengarah pada pertumbuhan, isolasi dan karakterisasi dari sebuah virus herpes baru yang dikenal dengan kaposi’s sarcoma-associated herpes virus (KSHV) atau human herpes virus type 8 (HHV-8) dari lesi sarkoma kaposi (SK). Sarkoma kaposi adalah kanker yang berkembang dari sel-sel yang melapisi kelenjar getah bening atau pembuluh darah. Seseorang yang terinfeksi HIV mempunyai risiko 100 hingga 300 kali lebih sering terkena SK. Lesi awal SK-AIDS tampak sebagai makula keunguan berbentuk oval kecil yang berkembang dengan cepat menjadi plak dan nodul kecil, yang seringkali timbul di seluruh bagian tubuh dan memiliki kecenderungan mengalami progresivitas yang cepat. Telah dilaporkan kasus seorang laki-laki imunokompromais berusia 27 tahun datang dengan keluhan lemah letih lesu dan bentol-bentol berwarna merah keunguan di dada, perut, punggung dan belakang telinga sejak 3 bulan sebelum masuk rumah sakit. Pemeriksaan lebih lanjut menunjukkan adanya HIV-AIDS dengan TB paru, candidiasis oral dan sarkoma kaposi. Diagnosis pada pasien ini ditegakkan berdasarkan keluhan dan data klinis yaitu anti HIV positif dengan CD4 49 u/L dan biopsi kulit dengan hasil sesuai dengan gambaran sarkoma kaposi. Penatalaksanaan pada pasien ini yaitu dengan pemberian OAT kategori I, ARV dan anti jamur. Pemberian ARV yang adekuat untuk HIV-AIDS merupakan kunci dalam tatalaksana SK-AIDS.


Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3821 ◽  
Author(s):  
Petrou ◽  
Eleftheriou ◽  
Geronikaki ◽  
Akrivou ◽  
Vizirianakis

Background: HIV is the causative agent of Acquired Immunodeficiency Syndrome (AIDS), an infectious disease with increasing incidence worldwide. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) play an important role in the treatment of AIDS. Although, many compounds are already being used as anti-HIV drugs, research for the development of new inhibitors continues as the virus develops resistant strains. Methods: The best features of available NNRTIs were taken into account for the design of novel inhibitors. PASS (Prediction of activity spectra for substances) prediction program and molecular docking studies for the selection of designed compounds were used for the synthesis. Compounds were synthesized using conventional and microwave irradiation methods and HIV RT inhibitory action was evaluated by colorimetric photometric immunoassay. Results: The evaluation of HIV-1 RT inhibitory activity revealed that seven compounds have significantly lower ΙC50 values than nevirapine (0.3 μΜ). It was observed that the activity of compounds depends not only on the nature of substituent and it position in benzothiazole ring but also on the nature and position of substituents in benzene ring. Conclusion: Twenty four of the tested compounds exhibited inhibitory action lower than 4 μΜ. Seven of them showed better activity than nevirapine, while three of the compounds exhibited IC50 values lower than 5 nM. Two compounds 9 and 10 exhibited very good inhibitory activity with IC50 1 nM.


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