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

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.

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.


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.


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.


2019 ◽  
Vol 15 (3) ◽  
pp. 252-258 ◽  
Author(s):  
Kalyani Dhirendra Asgaonkar ◽  
Shital Manoj Patil ◽  
Trupti Sameer Chitre ◽  
Vaibhav Nanabhau Ghegade ◽  
Saurabh Radhaji Jadhav ◽  
...  

<P>Background: Acquired immunodeficiency Syndrome (AIDS) is caused by Human immunodeficiency virus type 1 (HIV-1). Pyrazine and Thiazolidinone pharmacophore has diverse biological activities including anti HIV activity. </P><P> Aims and Objectives: To study binding behavior of Pyrazine- thiazolidinone derivatives on four different crystal structures of HIV- 1RT.These molecules which were already reported as anti-TB were investigated for dual activity as Anti-HIV and Anti-TB. </P><P> Materials and Methods: In the present study we describe a comparative docking study of twentythree derivatives of N-(4-oxo-2 substituted thiazolidin-3-yl) pyrazine-2-carbohydrazide. Binding pattern of these derivatives was gauged by molecular docking studies on four different receptors bearing PDB code 1ZD1, 1RT2, 1FKP and 1FK9 of HIV–RT enzyme using V. Life MDS software Genetic algorithm docking method. </P><P> Result and Discussion: The studies revealed hydrogen bonds, hydrophobic interaction and pi-pi interactions playing significant role in binding of the molecules to the enzyme. Conclusion: Most of the molecules have shown good dock score and binding energy with anti-HIV receptors but Molecules 13 and 14 have potential to act as anti-tubercular and Anti HIV and hence can be further explored for dual activity.</P>


2016 ◽  
Vol 88 (11) ◽  
pp. 4-11 ◽  
Author(s):  
V V Pokrovsky

In 2015, the infection caused by human immunodeficiency virus (HIV) (HIV infection) dominated among life-threatening infections in Russians: it was first diagnosed in 98,177 Russians and 15,530 citizens of the Russian Federation died from HIV/AIDS, amounting to 45% of all deaths from infectious diseases in Russia. By the mid-2016, there were a total of 1,062,476 identified HIV-positive Russians, of whom 225,992 people died. The estimated number of HIV-infected patients in Russia approximated to 1% of the population, the highest prevalence of HIV being found in the age group of 30—40 years. The most active and expensive measures against HIV/AIDS in Russia are to examine the population for anti-HIV antibodies (29 million screenings per year) and to use in HIV-positive people antiretroviral therapy that was free of charge to more than 200,000 patients, i.e. nearly 25% of the registered Russians living with the HIV-infected. However, treatment coverage and quality are far from the target indicators that the international experts consider needed to reduce HIV prevalence and mortality. A wider program on HIV/AIDS, which includes a number of preventive measures with proven efficiency, as well as a program of promising researches and developments should be introduced in Russia.


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