The Anti-HIV Activity and Mechanisms of Action of Pure Compounds Isolated fromRosa damascena

1996 ◽  
Vol 229 (1) ◽  
pp. 73-79 ◽  
Author(s):  
Naheed Mahmood ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Andrew Burke ◽  
Adil I. Khan ◽  
...  
Keyword(s):  
Mechanisms Of Action ◽  
Pure Compounds ◽  
Anti Hiv

scholarly journals Bioactivities and Future Perspectives of Chaetoglobosins

2020 ◽  
Vol 2020 ◽  
pp. 1-10 ◽  
Author(s):  
Jinhua Chen ◽  
Wenzhou Zhang ◽  
Qingfeng Guo ◽  
Weijiang Yu ◽  
Yongna Zhang ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Large Class ◽  
Biological Activities ◽  
Mechanisms Of Action ◽  
Chaetomium Globosum ◽  
Future Perspectives ◽  
Anti Inflammatory ◽  
Anti Hiv ◽  
Fungal Secondary Metabolites

Chaetoglobosins belonging to cytochalasan alkaloids represent a large class of fungal secondary metabolites. To date, around 100 chaetoglobosins and their analogues have been isolated and identified over the years from a variety of fungi, mainly from the fungus Chaetomium globosum. Studies have found that chaetoglobosins possess a broad range of biological activities, including antitumor, antifungal, phytotoxic, fibrinolytic, antibacterial, nematicidal, anti-inflammatory, and anti-HIV activities. This review will comprehensively summarize the biological activities and mechanisms of action of nature-derived chaetoglobosins.

scholarly journals Long-Acting HIV-1 Fusion Inhibitory Peptides and their Mechanisms of Action

Viruses ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 811 ◽  
Author(s):  
Chen Wang ◽  
Shuihong Cheng ◽  
Yuanyuan Zhang ◽  
Yibo Ding ◽  
Huihui Chong ◽  
...  
Keyword(s):  
Half Life ◽  
Mechanisms Of Action ◽  
Effective Concentration ◽  
Fusion Inhibitor ◽  
Inhibitory Peptides ◽  
Long Acting ◽  
Peg Chain Length ◽  
Plasma Half Life ◽  
Anti Hiv ◽  
Hiv 1

The clinical application of HIV fusion inhibitor, enfuvirtide (T20), was limited mainly because of its short half-life. Here we designed and synthesized two PEGylated C34 peptides, PEG2kC34 and PEG5kC34, with the PEG chain length of 2 and 5 kDa, respectively, and evaluated their anti-HIV-1 activity and mechanisms of action. We found that these two PEGylated peptides could bind to the HIV-1 peptide N36 to form high affinity complexes with high α-helicity. The peptides PEG2kC34 and PEG5kC34 effectively inhibited HIV-1 Env-mediated cell–cell fusion with an effective concentration for 50% inhibition (EC50) of about 36 nM. They also inhibited infection of the laboratory-adapted HIV-1 strain NL4-3 with EC50 of about 4–5 nM, and against 47 HIV-1 clinical isolates circulating in China with mean EC50 of PEG2kC34 and PEG5kC34 of about 26 nM and 32 nM, respectively. The plasma half-life (t1/2) of PEG2kC34 and PEG5kC34 was 2.6 h and 5.1 h, respectively, and the t1/2 of PEGylated C34 was about 2.4-fold and 4.6-fold longer than C34 (~1.1 h), respectively. These findings suggest that PEGylated C34 with broad-spectrum anti-HIV-1 activity and prolonged half-life can be further developed as a peptide fusion inhibitor-based long-acting anti-HIV drug for clinical use to treat HIV-infected patients who have failed to respond to current anti-retrovirus drugs.

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
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.

scholarly journals A REVIEW OF BENZOPYRAN DERIVATIVES IN PHARMACOTHERAPY OF BREAST CANCER

2018 ◽  
Vol 11 (7) ◽  
pp. 43 ◽  
Author(s):  
Kumar Piyush ◽  
Singh Kuldeep ◽  
Rahman Md. Azizur ◽  
Hasan Syed Misbahul ◽  
Wal Pranay
Keyword(s):  
Breast Cancer ◽  
Natural Products ◽  
Biological Effects ◽  
Mechanisms Of Action ◽  
Ring System ◽  
Pharmacological Properties ◽  
Substitution Pattern ◽  
Naturally Occurring ◽  
Anti Hiv ◽  
Cancer Activity

One of the naturally occurring compounds containing oxygen moiety is benzopyran. Depending on its substitution pattern, different biological effects are shown. The benzopyran ring system is present in many natural products (such as genistein, hesperidin, and warfarin) as well as synthetic products. It displays pharmacological properties such as antitumor, anti-HIV, antimicrobials, anti-inflammatory, and anticoagulants. The sufficient literature support and the fact that benzopyran has potential as a pharmacophore particularly as anti-breast cancer, etc, current research seemed pertinent keeping in view the mechanism of anti-breast cancer activity. Therefore, the objective of this review is to focus on important benzopyran analogs with anti-breast cancer activity and highlight their mechanisms of action.

Traditional Medicines, HIV, and Related Infections

2011 ◽  
Vol 23 (1) ◽  
pp. 159-164 ◽  
Author(s):  
M. Patel ◽  
P. Bessong ◽  
H. Liu
Keyword(s):  
Clinical Trials ◽  
Immune System ◽  
Ethical Issues ◽  
Mechanisms Of Action ◽  
Antiretroviral Drugs ◽  
In Vivo Studies ◽  
Traditional Medicines ◽  
Anti Hiv

Traditional medicines are an integral part of health care worldwide, even though their efficacy has not been scientifically proven. HIV-infected individuals may use them singularly or in combination with conventional medicines. Many in vitro studies have proven the anti-HIV, anti- Candida, and anti–herpes simplex virus potential of traditional plants and identified some of the mechanisms of action. Very few in vivo studies are available that involve a small number of participants and show controversial results. In addition, knowledge is limited of the role of traditional medicines in the enhancement of the immune system. The use of traditional medicines with antiretroviral drugs (ARVs) has created a problem because drug interactions compromise the efficacy of ARVs. Several currently popular plants have been studied in the laboratory for their interaction with ARVs, with disadvantageous results. Unfortunately, no clinical trials are available. The science of traditional medicines is relatively new and is at present being modernized worldwide. However, there are still ethical issues regarding traditional medicines that need to be addressed—for example, regulations regarding quality control and standardization of medicines, regulation and education of healers who deliver these medicines, and unregulated clinical trials. The workshop addressed the following questions about traditional medicine and their use in HIV infection: What are the mechanisms of action of anti-HIV traditional medicines? Should traditional medicines be used in conjunction with ARV? Do traditional medicines enhance the immune system? Should medicinal plants be used for the control of oral infections associated with HIV? What are the ethical issues surrounding the use of traditional medicines for the treatment of HIV and associated infections?

Chemical Composition and Biological Activities from Croton delpyi Croton decalvatus and Croton caudatus

2020 ◽  
Vol 10 ◽  
Author(s):  
Sakchai Chaibun ◽  
Wilart Pompimon ◽  
Chanika Tidchai ◽  
Noraset Chalaemwongwan ◽  
Jutarut Wongping ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Antibacterial Activities ◽  
Cytotoxic Activities ◽  
Separation And Purification ◽  
Pure Compounds ◽  
Cytotoxicity Activities ◽  
Anti Hiv ◽  
Hiv 1

Background: C. delpyi, C. decalvatus and C. caudatus are in the Euphorbiaceae family. The aerial parts; twigs, leaves and barks of these plants were used as traditional medicine such as anti-inflammatory, cytotoxicity, and antifungal properties. Objectives: The aims of this work were 1) to study the chemical composition of C. delpyi, C. decalvatus, and C. caudatus 2) to test their antibacterial, anti-HIV-1 RT, and cytotoxicity activities of crude extracts and pure compounds from these plants. Methods: Extraction, separation and purification of three plants were performed under chromatographic method. The biological activities including antibacterial, anti-HIV-1 RT and cytotoxicity assay of three plants were evaluated by the standard methods. Results: Phytochemical investigation of C. delpyi was founded a new clerodanes diterpenoids; crotondelpyitin A (1). The five known compounds, such as acetyl aleuritolic acid (2), 5-hydroxy-7,4- dimethoxyflavone (3), and pilloin (4) were founded in C. decalvatus and 3α-benzoyloxy-D:A-friedo-oleanan-27,16αlactone (5), and bergenin (6) were founded in C. caudatus. The compound 3 show the most effective antibacterial activities with MIC in range <0.16 -1.25 mg/mL, and MBC in range 0.6 - >5.0 mg/mL. The six compounds were inactive with antiHIV-1 RT. In addition, compound 4 was active for cytotoxic activities on FaDu and KKU-M213 at <4 µg/mL. Conclusion: The present study reveals that the Croton species are sources of diterpenoid-type compounds and significant guide for further research of the chemical constituents from these plants as potential medicines.

scholarly journals Constituents of Cuscuto Reflexa are anti-HIV Agents

1997 ◽  
Vol 8 (1) ◽  
pp. 70-74 ◽  
Author(s):  
N Mahmood ◽  
S Piacente ◽  
A Burke ◽  
Al Khan ◽  
C Pizza
Keyword(s):  
Crude Extract ◽  
Quinic Acid ◽  
Cuscuta Reflexa ◽  
Gp 120 ◽  
Dicaffeoylquinic Acid ◽  
Pure Compounds ◽  
Specific Proteins ◽  
Anti Hiv Agents ◽  
Anti Hiv

Crude water extracts of Cuscuta reflexa exhibited anti-HIV activity. Fractionation of the crude extract led to the isolation of nine pure compounds with closely related structures, showing interesting structure activity relationships. 3,5,7,4′-Tetrahydroxyflavanone (aromadendrin) inhibited infection by binding to V3 loop of gp 120 and inhibiting its interaction with CD4, whereas 3,5,7,3′,4′-pentahydroxyflavanone (taxifolin), with an extra OH group in the 3′ position in ring B was less specific and exhibited less selectivity in cell cultures. In general, flavanones containing an extra OH group in the 3′ position (taxifolin, taxifolin-7-O-β-D-glucopyranoside and coccinoside B) were less specific and inhibited viral protease, reverse transcriptase, CD4 /gp120 interaction in vitro and bound to non specific proteins. Other compounds isolated from C reflexa were derivatives of quinic acids; 3,4-O-dicaffeoylquinic acid was more active than 3-O-caffeoyl quinic acid. The anti-HIV activity of crude extract may be the result of combinatory effects with compounds of different modes of action.

scholarly journals Potent Anti-HIV Activities and Mechanisms of Action of a Pine Cone Extract from Pinus yunnanensis

Molecules ◽  
2012 ◽  
Vol 17 (6) ◽  
pp. 6916-6929 ◽  
Author(s):  
Xuan Zhang ◽  
Liu-Meng Yang ◽  
Guang-Ming Liu ◽  
Ya-Juan Liu ◽  
Chang-Bo Zheng ◽  
...  
Keyword(s):  
Mechanisms Of Action ◽  
Pinus Yunnanensis ◽  
Pine Cone ◽  
Anti Hiv ◽  
Pine Cone Extract

scholarly journals Bifunctional Anti-Human Immunodeficiency Virus Type 1 Small Molecules with Two Novel Mechanisms of Action

2004 ◽  
Vol 48 (2) ◽  
pp. 663-665 ◽  
Author(s):  
Li Huang ◽  
Xiong Yuan ◽  
Christopher Aiken ◽  
Chin Ho Chen
Keyword(s):  
Human Immunodeficiency Virus ◽  
Small Molecules ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Mechanisms Of Action ◽  
Immunodeficiency Virus ◽  
Viral Determinants ◽  
Anti Hiv ◽  
Hiv 1

ABSTRACT A class of betulinic acid derivatives was synthesized to target two critical steps in the human immunodeficiency virus type 1 (HIV-1) replication cycle, entry and maturation. Each mechanism of HIV-1 inhibition is distinct from clinically available anti-HIV therapeutics. The viral determinants of the antientry and antimaturation activities are the bridging sheet of HIV-1 gp120 and the P24/p2 cleavage site, respectively.

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