ChemInform Abstract: Anti‐HIV Activity of Semisynthetic Derivatives of Andrographolide and Computational Study of HIV‐1 gp120 Protein Binding.

Uttekar, Mayur M.; Das, Tiyasa; Pawar, Rohan; Bhandari, Beena; Menon, Vidya V.; Nutan, Nutan; Gupta, Satish Kumar; Bhat, Sujata V.

doi:10.1002/chin.201313186

Cited by 6 publications

(6 citation statements)

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“…In the same year, the main component of A. paniculata, namely, andrographolide, was found to inhibit gp120-mediated cell fusion in HL2/3 cells with an IC 50 value of 0.59 M. Molecular modeling results show that andrographolide binds to the V3 loop of gp120. The andrographolide binding indicates that it could be an HIV infection prevention agent [61]. In addition, andrographolide and 14-deoxy-11,12-didehydroandrographolide showed good anti-HIV activity with EC 50 values of 49.0 and 56.8 µg/mL, respectively [62].…”

Section: Anti-hivmentioning

confidence: 98%

Antiviral Activities of Andrographolide and Its Derivatives: Mechanism of Action and Delivery System

Adiguna

Panggabean

Atikana³

et al. 2021

Pharmaceuticals

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Andrographispaniculata (Burm.f.) Nees has been used as a traditional medicine in Asian countries, especially China, India, Vietnam, Malaysia, and Indonesia. This herbaceous plant extract contains active compounds with multiple biological activities against various diseases, including the flu, colds, fever, diabetes, hypertension, and cancer. Several isolated compounds from A. paniculata, such as andrographolide and its analogs, have attracted much interest for their potential treatment against several virus infections, including SARS-CoV-2. The mechanisms of action in inhibiting viral infections can be categorized into several types, including regulating the viral entry stage, gene replication, and the formation of mature functional proteins. The efficacy of andrographolide as an antiviral candidate was further investigated since the phytoconstituents of A. paniculata exhibit various physicochemical characteristics, including low solubility and low bioavailability. A discussion on the delivery systems of these active compounds could accelerate their development for commercial applications as antiviral drugs. This study critically reviewed the current antiviral development based on andrographolide and its derivative compounds, especially on their mechanism of action as antiviral drugs and drug delivery systems.

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Section: Anti-hivmentioning

confidence: 98%

Antiviral Activities of Andrographolide and Its Derivatives: Mechanism of Action and Delivery System

Adiguna

Panggabean

Atikana³

et al. 2021

Pharmaceuticals

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show abstract

“…This compound modifies the plasma membrane fluidity and prevents viral cell fusion [77]. A diterpene lactone named Andrographolide (2) shown in Figure 3 was obtained from the herb Andrographis paniculata and possesses HIV-1 fusion inhibition propertiesevaluated in vitro using AZT (Zidovudine) as a positive control [78][79][80][81][82]. Several other derivatives have been derived synthetically to exert more potent anti-HIV properties [83,84].…”

Section: Natural Plants According To Their Mechanism Of Actionmentioning

confidence: 99%

“…(+)-Calanolide-A is the most potent compound when compared with Cordatolide A (less active and devoid of the bulky group at the C-4 position). Several furanocoumarins (e.g., bergapten (78) and psolaren) from the roots of Prangos tschimganica, have exhibited significant activities against the HIV virus [306]. Mesuol ( 79) is another coumarin (from the category 4-phenylcoumarin) reported to inhibit the replication of HIV-1through the prohibition of the reverse transcription and phosphorylation of HIV [307].…”

Section: Coumarinsmentioning

confidence: 99%

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

et al. 2020

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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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“…Hence, different drugs act on these different steps of replication and inhibit the further expansion of virus into the body. A group of researchers reported Figure 3 is obtained from the herb Andrographis paniculata possesses HIV-1 fusion inhibition properties [67][68][69][70][71]. Several derivatives of this compound have been produced synthetically to exert more potent anti-HIV properties [72,73].…”

Section: Natural Plants According To Their Mechanism Of Actionmentioning

confidence: 99%

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

Kaur

Sharma

Gupta³

et al. 2020

Preprint

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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.

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ChemInform Abstract: Anti‐HIV Activity of Semisynthetic Derivatives of Andrographolide and Computational Study of HIV‐1 gp120 Protein Binding.

Cited by 6 publications

References 1 publication

Antiviral Activities of Andrographolide and Its Derivatives: Mechanism of Action and Delivery System

Antiviral Activities of Andrographolide and Its Derivatives: Mechanism of Action and Delivery System

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

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

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