Tea Polyphenols as Natural Products for Potential Future Management of HIV Infection - an overview

Belonging to the <em>Lentivirus</em> genus of animal retroviruses, human immunodeficiency virus (HIV) is the etiological agent of acquired immunodeficiency syndrome (AIDS) which attacks cells of the immune system including CD4<sup>+</sup> T lymphocytes, monocytes, macrophages and dendritic cells. A rapid progression to immunodeficiency and the higher transmissibility of HIV-1 compared to HIV-2 are hallmarks of the worldwide spread of AIDS. Conventional HIV treatments are limited by drug toxicity and by multi-drug resistance, caused by the high genetic variability of HIV. This has led researchers into new areas of drug discovery in search of novel therapeutic molecules. Accumulating evidence indicates that tea polyphenols possess a range of beneficial properties including anti-cancer, anti-inflammatory, anti-oxidative, neuro-protective, anti-bacterial, anti-fungal and anti-viral effects. The anti-HIV infection potential of tea polyphenols has been confirmed by several preclinical studies. This suggests that polyphenol-rich extracts of tea could be used as dietary supplements as part of a combined therapeutic regimen with conventional anti-HIV drugs. Phenolic structures may also be considered as backbones for the discovery of a new generation of anti-HIV remedies. This review provides a perspective on the anti-HIV activity of tea polyphenols and their development as a possible source of future drugs for the therapy of HIV/AIDS.

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Recent Advancements in Polythiophene-Based Materials and Their Biomedical, Geno Sensor and DNA Detection

International Journal of Molecular Sciences ◽

10.3390/ijms22136850 ◽

2021 ◽

Vol 22 (13) ◽

pp. 6850

Author(s):

Seyyed Mojtaba Mousavi ◽

Seyyed Alireza Hashemi ◽

Sonia Bahrani ◽

Khadije Yousefi ◽

Gity Behbudi ◽

...

Keyword(s):

Biomedical Engineering ◽

High Efficiency ◽

Polymeric Materials ◽

The Novel ◽

Electrode Coating ◽

Effective Response ◽

Hiv Drugs ◽

New Generation ◽

New Compounds ◽

Anti Hiv

In this review, the unique properties of intrinsically conducting polymer (ICP) in biomedical engineering fields are summarized. Polythiophene and its valuable derivatives are known as potent materials that can broadly be applied in biosensors, DNA, and gene delivery applications. Moreover, this material plays a basic role in curing and promoting anti-HIV drugs. Some of the thiophene’s derivatives were chosen for different experiments and investigations to study their behavior and effects while binding with different materials and establishing new compounds. Many methods were considered for electrode coating and the conversion of thiophene to different monomers to improve their functions and to use them for a new generation of novel medical usages. It is believed that polythiophenes and their derivatives can be used in the future as a substitute for many old-fashioned ways of creating chemical biosensors polymeric materials and also drugs with lower side effects yet having a more effective response. It can be noted that syncing biochemistry with biomedical engineering will lead to a new generation of science, especially one that involves high-efficiency polymers. Therefore, since polythiophene can be customized with many derivatives, some of the novel combinations are covered in this review.

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A New Approach to Developing Long-Acting Injectable Formulations of Anti-HIV Drugs: Poly(Ethylene Phosphoric Acid) Block Copolymers Increase the Efficiency of Tenofovir against HIV-1 in MT-4 Cells

International Journal of Molecular Sciences ◽

10.3390/ijms22010340 ◽

2020 ◽

Vol 22 (1) ◽

pp. 340

Author(s):

Ilya Nifant’ev ◽

Andrei Siniavin ◽

Eduard Karamov ◽

Maxim Kosarev ◽

Sergey Kovalchuk ◽

...

Keyword(s):

Controlled Release ◽

Block Copolymers ◽

Phosphoric Acid ◽

Hiv Infection ◽

Targeted Delivery ◽

Release Formulation ◽

Poly Ethylene ◽

Long Acting ◽

Hiv Drugs ◽

Anti Hiv

Despite the world’s combined efforts, human immunodeficiency virus (HIV), the causative agent of AIDS, remains one of the world’s most serious public health challenges. High genetic variability of HIV complicates the development of anti-HIV vaccine, and there is an actual clinical need for increasing the efficiency of anti-HIV drugs in terms of targeted delivery and controlled release. Tenofovir (TFV), a nucleotide-analog reverse transcriptase inhibitor, has gained wide acceptance as a drug for pre-exposure prophylaxis or treatment of HIV infection. In our study, we explored the potential of tenofovir disoproxil (TFD) adducts with block copolymers of poly(ethylene glycol) monomethyl ether and poly(ethylene phosphoric acid) (mPEG-b-PEPA) as candidates for developing a long-acting/controlled-release formulation of TFV. Two types of mPEG-b-PEPA with numbers of ethylene phosphoric acid (EPA) fragments of 13 and 49 were synthesized by catalytic ring-opening polymerization, and used for preparing four types of adducts with TFD. Antiviral activity of [mPEG-b-PEPA]TFD or tenofovir disoproxil fumarate (TDF) was evaluated using the model of experimental HIV infection in vitro (MT-4/HIV-1IIIB). Judging by the values of the selectivity index (SI), TFD exhibited an up to 14-fold higher anti-HIV activity in the form of mPEG-b-PEPA adducts, thus demonstrating significant promise for further development of long-acting/controlled-release injectable TFV formulations.

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Risk of Myocardial Infarction in Patients with HIV Infection Exposed to Specific Individual Antiretroviral Drugs from the 3 Major Drug Classes: The Data Collection on Adverse Events of Anti‐HIV Drugs (D:A:D) Study

The Journal of Infectious Diseases ◽

10.1086/649897 ◽

2010 ◽

Vol 201 (3) ◽

pp. 318-330 ◽

Cited By ~ 407

Author(s):

Signe Westring Worm ◽

Caroline Sabin ◽

Rainer Weber ◽

Peter Reiss ◽

Wafaa El‐Sadr ◽

...

Keyword(s):

Myocardial Infarction ◽

Data Collection ◽

Adverse Events ◽

Hiv Infection ◽

Antiretroviral Drugs ◽

Drug Classes ◽

Specific Individual ◽

Hiv Drugs ◽

Anti Hiv ◽

Major Drug

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

Molecules ◽

10.3390/molecules25092070 ◽

2020 ◽

Vol 25 (9) ◽

pp. 2070

Author(s):

Ramandeep Kaur ◽

Pooja Sharma ◽

Girish K. Gupta ◽

Fidele Ntie-Kang ◽

Dinesh Kumar

Keyword(s):

Natural Products ◽

Mechanisms Of Action ◽

Structure Activity ◽

Immunodeficiency Virus ◽

Ic50 Values ◽

Acquired Immunodeficiency ◽

Hiv Drugs ◽

Immunodeficiency Syndrome ◽

Anti Hiv ◽

Made In

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.

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Comparative Molecular Transporter Properties of Cyclic Peptides Containing Tryptophan and Arginine Residues Formed through Disulfide Cyclization

Molecules ◽

10.3390/molecules25112581 ◽

2020 ◽

Vol 25 (11) ◽

pp. 2581

Author(s):

Eman H. M. Mohammed ◽

Dindyal Mandal ◽

Saghar Mozaffari ◽

Magdy Abdel-Hamied Zahran ◽

Amany Mostafa Osman ◽

...

Keyword(s):

Cyclic Peptides ◽

Solid Phase ◽

Solid Phase Peptide Synthesis ◽

Cell Penetrating Peptides ◽

Molecular Transporters ◽

Arginine Residues ◽

Significant Uptake ◽

Hiv Drugs ◽

New Generation ◽

Anti Hiv

We have previously reported cyclic cell-penetrating peptides [WR]5 and [WR]4 as molecular transporters. To optimize further the utility of our developed peptides for targeted therapy in cancer cells using the redox condition, we designed a new generation of peptides and evaluated their cytotoxicity as well as uptake behavior against different cancer cell lines. Thus, cyclic [C(WR)xC] and linear counterparts (C(WR)xC), where x = 4–5, were synthesized using Fmoc/tBu solid-phase peptide synthesis, purified, and characterized. The compounds did not show any significant cytotoxicity (at 25 µM) against ovarian (SK-OV-3), leukemia (CCRF-CEM), gastric adenocarcinoma (CRL-1739), breast carcinoma (MDA-MB-231), and normal kidney (LLCPK) cells after 24 and 72 h incubation. Both cyclic [C(WR)5C] and linear (C(WR)5C) demonstrated comparable molecular transporter properties versus [WR]5 in the delivery of a phosphopeptide (F′-GpYEEI) in CCRF-CEM cells. The uptake of F′-GpYEEI in the presence of 1,4-dithiothreitol (DTT) as the reducing agent was significantly improved in case of l(C(WR)5C), while it was not changed by [C(WR)5C]. Fluorescence microscopy also demonstrated a significant uptake of F′-GpYEEI in the presence of l(C(WR)5C). Cyclic [C(WR)5C] improved the uptake of the fluorescent-labeled anti-HIV drugs F′-d4T, F′-3TC, and F′-FTC by 3.0–4.9-fold. These data indicate that both [C(WR)5C] and linear (C(WR)5C) peptides can act as molecular transporters.

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Anti-HIV Activity of Medicinal Herbs: Usage and Potential Development

The American Journal of Chinese Medicine ◽

10.1142/s0192415x01000083 ◽

2001 ◽

Vol 29 (01) ◽

pp. 69-81 ◽

Cited By ~ 105

Author(s):

Ji An Wu ◽

Anoja S. Attele ◽

Liu Zhang ◽

Chun-Su Yuan

Keyword(s):

Hiv Infection ◽

Herbal Medicines ◽

Immune Functions ◽

Scutellaria Baicalensis Georgi ◽

Potential Development ◽

Research Findings ◽

Acquired Immunodeficiency ◽

Immunodeficiency Syndrome ◽

Anti Hiv Agents ◽

Anti Hiv

The acquired immunodeficiency syndrome (AIDS) is a result of human immunodeficiency virus (HIV) infection which subsequently leads to significant suppression of immune functions. AIDS is a significant threat to the health of mankind, and the search for effective therapies to treat AIDS is of paramount importance. Several chemical anti-HIV agents have been developed. However, besides the high cost, there are adverse effects and limitations associated with using chemotherapy for the treatment of HIV infection Thus, herbal medicines have frequently been used as an alternative medical therapy by HIV positive individuals and AIDS patients. The aim of this review is to summarize research findings for herbal medicines, which are endowed with the ability to inhibit HIV. In this article, we will emphasize a Chinese herbal medicine. Scutellaria baicalensis Georgi and its identified components (i.e. baicalein and baicalin) which have been shown to inhibit infectivity and replication of HIV. Potential development of anti-AIDS compounds using molecular modeling methods will also be discussed.

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Therapeutic potential of indole derivatives as anti-HIV agents: A mini-review

Current Topics in Medicinal Chemistry ◽

10.2174/1568026621666211012111901 ◽

2021 ◽

Vol 21 ◽

Author(s):

Qingtai Chen ◽

Chongchong Wu ◽

Jinjin Zhu ◽

Enzhong Li ◽

Zhi Xu

Keyword(s):

Therapeutic Potential ◽

Treatment Options ◽

Multidrug Resistant ◽

Bioactive Molecules ◽

Indole Derivatives ◽

Chemical Structures ◽

Hiv Drugs ◽

Immunodeficiency Syndrome ◽

Anti Hiv Agents ◽

Anti Hiv

: Acquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus (HIV), is one of the leading causes of human deaths. The advent of different anti-HIV drugs over different disease progress has made AIDS/HIV from a deadly infection to chronic and manageable disease. However, the development of multidrug-resistant viruses, together with the severe side effects of anti-HIV agents, compromised their efficacy and limited the treatment options. Indoles, the most common frameworks in the bioactive molecules, represent attractive scaffolds for the design and development of novel drugs. Indole derivatives are potential inhibitors of HIV enzymes such as reverse transcriptase, integrase and protease, and some indole-based agents like Delavirdine have already been applied in clinics or under clinical evaluations for the treatment of AIDS/HIV, revealing that indole moiety is a useful template for the development of anti-HIV agents. This review focuses on the recent advancement of indole derivatives including indole alkaloids, hybrids, and dimers with anti-HIV potential, covering articles published between 2010 and 2020. The chemical structures, structure-activity relationship and mechanisms of action are also discussed.

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