Anti-viral and cytotoxic norbisabolane sesquiterpenoid glycosides from Phyllanthus emblica and their absolute configurations

Lv, Jun-Jiang; Yu, Shan; Xin, Ying; Cheng, Rong-Rong; Zhu, Hongtao; Wang, Dong; Yang, Chong‐Ren; Xu, Min; Zhang, Yingjun

doi:10.1016/j.phytochem.2015.06.001

“…It was reported earlier that Procyanidin A2, Procyanidine B1, Cinnamtannin B1 of Twak has been found to have activity against coronavirus (wt SARS-CoV) and SARS-CoV S pseudovirus infections [48]. Phyllaemblicin B and Phyllaemblicin C of Amalaki has been found to have activity against Influenza A virus strain H3N2 causing respiratory infections [42]. Germacrone of Haridra has been found to have activity against H1N1 and H3N2 virus causing respiratory illness [49].…”

Section: Pharmacokinetic Properties Of the Phytochemicalsmentioning

confidence: 95%

Structure-Based Bioactive Phytochemical Design from Ayurvedic Formulations Towards Spike and Mpro Druggable Targets of SARS-CoV-2

Pushkaran¹,

EN²,

Nair³

et al. 2020

Preprint

0

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The present COVID-19 global crisis invoked different disciplines of the biomedical research community to address the contagious human to human viral transmission and infection severity. Traditional or de novo drug discovery approach is a very time consuming process and will conflict with the urgency to discover new anti-viral drugs for combating the present global pandemic. Modern anti-viral drugs are not very effective and show resistance with serious adverse effects. Thus, identifying bioactive natural ingredients (phytochemical) from different medicinal plants or Ayurvedic formulations provides an effective alternative therapy for SARS-CoV-2 viral infections. We performed structure-based phytochemical design studies involving bioactive phytochemicals from medicinal plants towards two key druggable targets, spike glycoprotein and main protease (Mpro) of SARS-CoV-2. Phyllaemblicin class of phytocompounds showed better binding affinity towards both these SARS-CoV-2 targets and its binding mode revealed interactions with critical amino acid residues at its active sites. Also, we have successfully shown that the SARS-CoV-2 spike glycoprotein interaction towards human ACE2 receptor as its port of human cellular entry was blocked due to conformational variations in ACE2 receptor recognition by the binding of the phytocompound, Phyllaemblicin C at the ACE2 binding domain of spike protein. Our study shows that the Phyllaemblicin class of phytochemicals can be a potential dual inhibitor of spike and Mpro proteins of SARS-CoV-2 and could be promising for the treatment of COVID-19.

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“…Among these K417, G446, Y449, N487, Y489, Q493, T500, N501, G502 and Y505 residues made direct hydrogen bonding interactions with the human ACE2 residues [16]. medicinal properties including anti-proliferative and anti-viral activities [42]. Phyllaemblicin C also made strong hydrogen bonding interactions with the Y453, G496, Q498, N501, Y449, S494, Q493, and G498 RBD residues.…”

Section: Molecular Docking Of Bioactive Phytochemicals Towards Sars-cmentioning

confidence: 99%

Structure-Based Bioactive Phytochemical Design from Ayurvedic Formulations Towards Spike and Mpro Druggable Targets of SARS-CoV-2

Anju¹,

Prajeeshnath²,

Nair³

et al. 2020

Preprint

1

0

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The present COVID-19 global crisis invoked different disciplines of the biomedical research community to address the contagious human to human viral transmission and infection severity. Traditional or de novo drug discovery approach is a very time consuming process and will conflict with the urgency to discover new anti-viral drugs for combating the present global pandemic. Modern anti-viral drugs are not very effective and show resistance with serious adverse effects. Thus, identifying bioactive natural ingredients (phytochemical) from different medicinal plants or Ayurvedic formulations provides an effective alternative therapy for SARS-CoV-2 viral infections. We performed structure-based phytochemical design studies involving bioactive phytochemicals from medicinal plants towards two key druggable targets, spike glycoprotein and main protease (Mpro) of SARS-CoV-2. Phyllaemblicin class of phytocompounds showed better binding affinity towards both these SARS-CoV-2 targets and its binding mode revealed interactions with critical amino acid residues at its active sites. Also, we have successfully shown that the SARS-CoV-2 spike glycoprotein interaction towards human ACE2 receptor as its port of human cellular entry was blocked due to conformational variations in ACE2 receptor recognition by the binding of the phytocompound, Phyllaemblicin C at the ACE2 binding domain of spike protein. Our study shows that the Phyllaemblicin class of phytochemicals can be a potential dual inhibitor of spike and Mpro proteins of SARS-CoV-2 and could be promising for the treatment of COVID-19.

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“…There was a significant decrease in inflammation and periodontal destruction with 10% sustained-release gel [43]. Glochicoccinoside D isolated from P. emlica roots displayed strong activity against influenza A virus H3N2 and EV71 virus (hand, foot and mouth virus) [44]. A recent study has reported the presence of eight bisabolane sesquiterpenoid glycoside phyllaemblicins G1-G8, alongwith phyllaemblicin F, phyllaemblic acid and glochicoccin with potential anti-HBV (Hepatitis-B virus) activity [45].…”

Section: Anti-microbial Activitymentioning

confidence: 99%

Nutraceutical and Pharmacological Appraisal of Āmla (Emblica officinalis Gaertn.): A Review

Fazil

¹

,

Nikhat

²

2019

EJMP

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Āmla (Emblica officinalis Gaertn, Family: Euphorbiaceae) is a medicinally important plant indigenous to tropical and sub-tropical regions of South-east Asia. The tree is 5-25 metres tall, deciduous, having deltoid-squamiform leaves and bears pale-green globose fruits 2-4 cm in diameter. In Unani medicine, it is widely used in compound formulations or in raw form in many disorders of central nervous system, gastro-intestinal system, skin, hair, general debility etc. In Ayurveda, it is classified as a rasayana, i.e., drugs which promote longevity and delay ageing. Āmla fruit is one of the richest sources of Vitamin C (478.56 mg/ 100 ml), alongwith important constituents such as gallic acid, ellagic acid, iron, magnesium, phosphorous, potassium etc. recent researches on Āmla have revealed the presence of several biologically active substances with scientifically proven effects as anti-oxidant, anti-ageing, immunomodulatory, memory enhancing, protective towards vital organs such as liver, heart kidneys; anti-depressant, anti-cancer and many more beneficial effects. Most of the experiments have been carried out on Āmla fruit and are dose-dependent. Moreover, no toxic effects have been reported in any of the studies. This review focuses on the various biologically active components of Āmla and its relevance in modern pharmacology.

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Anti-viral and cytotoxic norbisabolane sesquiterpenoid glycosides from Phyllanthus emblica and their absolute configurations

Cited by 44 publications

References 15 publications

Structure-Based Bioactive Phytochemical Design from Ayurvedic Formulations Towards Spike and Mpro Druggable Targets of SARS-CoV-2

Structure-Based Bioactive Phytochemical Design from Ayurvedic Formulations Towards Spike and Mpro Druggable Targets of SARS-CoV-2

Structure-Based Bioactive Phytochemical Design from Ayurvedic Formulations Towards Spike and Mpro Druggable Targets of SARS-CoV-2

Nutraceutical and Pharmacological Appraisal of Āmla (Emblica officinalis Gaertn.): A Review

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