Therapeutic Approach against 2019-nCoV by Inhibition of ACE-2 Receptor

Kumar, Siva; Kumar, Dharmendra; Singh, Netra Pal

doi:10.1055/a-1275-0228

Cited by 20 publications

(15 citation statements)

References 21 publications

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“…Ayurveda is a 5000-year old system of traditional Indian medicine worth considering as an option for treating COVID-19. 8 , 38 …”

Section: Discussionmentioning

confidence: 99%

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Coronil, a Tri-Herbal Formulation, Attenuates Spike-Protein-Mediated SARS-CoV-2 Viral Entry into Human Alveolar Epithelial Cells and Pro-Inflammatory Cytokines Production by Inhibiting Spike Protein-ACE-2 Interaction

Balkrishna¹,

Haldar²,

Singh³

et al. 2021

JIR

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Purpose Coronil is a tri-herbal formulation containing extracts from Withania somnifera, Tinospora cordifolia, and Ocimum sanctum . Recently, it was shown that Coronil rescued humanized zebrafish from SARS-CoV-2 induced pathologies. Based on reported computational studies on the phytochemicals present in Coronil, it could be a potential inhibitor of SARS-CoV-2 entry into the host cell and associated cytokines’ production. Methods Through an ELISA-based biochemical assay, effects of Coronil on interaction between ACE-2 and different mutants of viral spike (S) protein, crucial for viral invasion of host cell, were evaluated. Additionally, using recombinant pseudoviruses having SARS-CoV-2 spike (S) protein in their envelopes and firefly luciferase reporter in their genomes, effects of Coronil on virus entry into human alveolar epithelial cells were evaluated through luciferase assay. UHPLC profiled Coronil also modulated S-protein mediated production of pro-inflammatory cytokines in A549 cells, like interleukin-6 (IL-6), interleukin-1β (IL-1β), and tumor necrosis factor-α (TNF-α), as evaluated through RT-qPCR and ELISA. Results Coronil effectively inhibited the interaction of ACE-2 not only with the wild-type S protein (S WT ) but also with its currently prevalent and more infectious variant (S D614G ) and another mutant (S W436R ) with significantly higher affinity toward ACE-2. Treatment with Coronil significantly reduced the increased levels of IL-6, IL-1β, and TNF-α in A549 cells incubated with different S-protein variants in a dose-dependent manner. Likewise, it also prevented the SARS-CoV-2 S-protein pseudotyped vesicular stomatitis virus (VSVppSARS-2S) mediated cytokine response in these cells by reducing entry of pseudoviruses into host cells. Conclusion Coronil prevented SARS-CoV-2 S-protein mediated viral entry into A549 cells by inhibiting spike protein-ACE-2 interactions. SARS-CoV-2 S protein induced inflammatory cytokine response in these cells was also moderated by Coronil.

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“…Ayurveda is a 5000-year old system of traditional Indian medicine worth considering as an option for treating COVID-19. 8 , 38 …”

Section: Discussionmentioning

confidence: 99%

“…Among various modes of therapeutics, traditional systems of medicines which are mainly composed of herbal and other natural resources provide hope because of their multi-targeted functionality and minimal side effects. 8 …”

Section: Introductionmentioning

confidence: 99%

Coronil, a Tri-Herbal Formulation, Attenuates Spike-Protein-Mediated SARS-CoV-2 Viral Entry into Human Alveolar Epithelial Cells and Pro-Inflammatory Cytokines Production by Inhibiting Spike Protein-ACE-2 Interaction

Balkrishna¹,

Haldar²,

Singh³

et al. 2021

JIR

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“…The major stabilizing interactions of piperine with SARS-CoV-2 RBD Spro were by covalent hydrogen bonding, π–π T-shaped, and van der Waals force of interactions [ 151 ]. Piperine acts on the Nsp15 viral protein and inhibits SARS-CoV-2 replication [ 152 , 153 ]. Furthermore, binding chemistry of piperine and curcumin via π–π intermolecular interactions enhances curcumin’s bioavailability, which facilitates curcumin to bind RBD Spro and ACE-2 receptors of host cell, thereby inhibiting the entry of virus inside the host [ 152 , 153 ].…”

Section: Main Textmentioning

confidence: 99%

Molecular and pharmacological aspects of piperine as a potential molecule for disease prevention and management: evidence from clinical trials

Tripathi

Ray

Mishra

2022

Beni-Suef Univ J Basic Appl Sci

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Background Piperine is a type of amide alkaloid that exhibits pleiotropic properties like antioxidant, anticancer, anti-inflammatory, antihypertensive, hepatoprotective, neuroprotective and enhancing bioavailability and fertility-related activities. Piperine has the ability to alter gastrointestinal disorders, drug-metabolizing enzymes, and bioavailability of several drugs. The present review explores the available clinical and preclinical data, nanoformulations, extraction process, structure–activity relationships, molecular docking, bioavailability enhancement of phytochemicals and drugs, and brain penetration properties of piperine in the prevention, management, and treatment of various diseases and disorders. Main body Piperine provides therapeutic benefits in patients suffering from diabetes, obesity, arthritis, oral cancer, breast cancer, multiple myeloma, metabolic syndrome, hypertension, Parkinson's disease, Alzheimer’s disease, cerebral stroke, cardiovascular diseases, kidney diseases, inflammatory diseases, and rhinopharyngitis. The molecular basis for the pleiotropic activities of piperine is based on its ability to regulate multiple signaling molecules such as cell cycle proteins, anti-apoptotic proteins, P-glycoprotein, cytochrome P450 3A4, multidrug resistance protein 1, breast cancer resistance protein, transient receptor potential vanilloid 1 proinflammatory cytokine, nuclear factor-κB, c-Fos, cAMP response element-binding protein, activation transcription factor-2, peroxisome proliferator-activated receptor-gamma, Human G-quadruplex DNA, Cyclooxygenase-2, Nitric oxide synthases-2, MicroRNA, and coronaviruses. Piperine also regulates multiple signaling pathways such as Akt/mTOR/MMP-9, 5′-AMP-activated protein kinase-activated NLR family pyrin domain containing-3 inflammasome, voltage-gated K+ current, PKCα/ERK1/2, NF-κB/AP-1/MMP-9, Wnt/β-catenin, JNK/P38 MAPK, and gut microbiota. Short conclusion Based on the current evidence, piperine can be the potential molecule for treatment of disease, and its significance of this molecule in the clinic is discussed. Graphical abstract

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“…As a result, consuming black pepper or piperine can aid in virus management. Specific laboratory and clinical investigations, however, are needed to back up the conclusions of the study [ 94 , 95 ].…”

Section: Other Floras and Dietary Supplements As Anti-virals Against ...mentioning

confidence: 99%

Perspectives on nano-nutraceuticals to manage pre and post COVID-19 infections

Dubey

Chaudhry

Singh

et al. 2022

Biotechnology Reports

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Optimized therapeutic bio-compounds supported by bio-acceptable nanosystems (i.e., precise nanomedicine) have ability to promote health via maintaining body structure, organ function, and controlling chronic and acute effects. Therefore, nano-nutraceuticals (designed to neutralize virus, inhibit virus bindings with receptors, and support immunity) utilization can manage COVID-19 pre/post-infection effects. To explore these approaches well, our mini-review explores optimized bio-active compounds, their ability to influence SARS-CoV-2 infection, improvement in performance supported by precise nanomedicine approach, and challenges along with prospects. Such optimized pharmacologically relevant therapeutic cargo not only affect SARS-CoV-2 but will support other organs which show functional alternation due to SARS-CoV-2 for example, neurological functions. Hence, coupling the nutraceuticals with the nano-pharmacology perspective of higher efficacy via targeted delivery action can pave a novel way for health experts to plan future research needed to manage post COVID-19 infection effect where a longer efficacy with no side-effects is a key requirement.

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Therapeutic Approach against 2019-nCoV by Inhibition of ACE-2 Receptor

Cited by 20 publications

References 21 publications

Coronil, a Tri-Herbal Formulation, Attenuates Spike-Protein-Mediated SARS-CoV-2 Viral Entry into Human Alveolar Epithelial Cells and Pro-Inflammatory Cytokines Production by Inhibiting Spike Protein-ACE-2 Interaction

Coronil, a Tri-Herbal Formulation, Attenuates Spike-Protein-Mediated SARS-CoV-2 Viral Entry into Human Alveolar Epithelial Cells and Pro-Inflammatory Cytokines Production by Inhibiting Spike Protein-ACE-2 Interaction

Molecular and pharmacological aspects of piperine as a potential molecule for disease prevention and management: evidence from clinical trials

Perspectives on nano-nutraceuticals to manage pre and post COVID-19 infections

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