Other substances

Cepharanthine

An anti-inflammatory isoquinoline alkaloid.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

Supporting references

Contradictory references

AI-suggested references

Clinical trials

General information

Cepharanthine is a bisbenzylisoquinoline alkaloid used for restoration of lymphatic system's immunologic properties after antineoplastic treatment (ChEBI). It has been reported to act as a calcium channel blocker and shown to possess anti-SARS-CoV-2 activity in vitro (He et al., 2021).

Cepharanthine on PubChem
Cepharanthine on Wikipedia

Synonyms

Cepharanthin; O-Methylcepharanoline; SC9

CN1CCC2=CC3=C(C4=C2[C@@H]1CC5=CC=C(C=C5)OC6=C(C=CC(=C6)C[C@@H]7C8=CC(=C(C=C8CCN7C)OC)O4)OC)OCO3

Supporting references

Link	Tested on	Impact factor	Notes	Publication date
Repurposing of clinically approved drugs for treatment of coronavirus disease 2019 in a 2019-novel coronavirus (2019-nCoV) related coronavirus model.	Similar viruses		Two libraries of 2406 clinically approved drugs were screened for their ability to inhibit cytopathic effects on Vero E6 cells by GX_P2X (2019-nCoV related) infection	Mar/06/2020
Multidrug treatment with nelfinavir and cepharanthine against COVID-19	VERO E6 cell cultures		better in combination with nelfinavir	Apr/15/2020
Identifying SARS-CoV-2 entry inhibitors through drug repurposing screens of SARS- S and MERS-S pseudotyped particles Preprint Screening	VERO E6 cell cultures			Jul/11/2020
Comparative analysis of antiviral efficacy of FDA-approved drugs against SARS-CoV-2 in human lung cells: Nafamostat is the most potent antiviral drug candidate Preprint	Calu-3 human airway epithelial cells		higher IC50 value in Calu-3 cells than VERO E6 cells	May/12/2020
Identification of existing pharmaceuticals and herbal medicines as inhibitors of SARS-CoV-2 infection 3CLpro PapainLpro Enzyme assay Animal model In vitro In silico	in silico; in vitro enzyme assay; Vero E6 cells; golden Syrian hamsters; SARS-CoV-2 clinical isolate hCoV-19/Taiwan/4/2020	9.41	Inhibited SARS-CoV-2 infection in Vero E6 cells (selectivity index of ca. 4.6).	Jan/15/2021
Identification of bis-benzylisoquinoline alkaloids as SARS-CoV-2 entry inhibitors from a library of natural products Small molecule In vitro Mechanism	in vitro binding assay; 293T-ACE2 cells; Calu-3 cells; A549 cells; Vero E6 cells; (HIV-1) SARS-CoV-2 Spike (D614/G614/B.1.1.7/B.1.351); SARS-CoV-2 live virus	13.49	Cepharanthine inhibited lentiviral SARS-CoV-2 Spike-pseudotyped virus infection in 293T-ACE2 (EC50 of 0.315 μM or lower, SI > 158), Calu-3 and A549 cells. It displayed efficacy also against pseudoviruses with Spike protein of G614, B.1.1.7, B.1.351, SARS, and MERS viruses/strains. The experimental findings suggest that the compound blocks coronavirus entry into host cells by inhibition of calcium ion channels. The compound was also shown to protect Vero E6 cells from SARS-CoV-2 live virus-induced cytopathogenic effect (>99.9% inhibition at 10 μM).	Mar/23/2021

AI-suggested references

Link	Publication date
SARS-CoV-2 and SARS-CoV: Virtual screening of potential inhibitors targeting RNA-dependent RNA polymerase activity (NSP12)	Jul/09/2020
Repurposing of clinically approved drugs for treatment of coronavirus disease 2019 in a 2019-novel coronavirus-related coronavirus model	Nov/03/2022
ACE2 : S1 RBD Interaction-Targeted Peptides and Small Molecules as Potential COVID-19 Therapeutics	Jan/05/2022
Potential anti-COVID-19 agents, cepharanthine and nelfinavir, and their usage for combination treatment.	Mar/26/2021
Antiviral drugs against severe acute respiratory syndrome coronavirus 2 infection triggering the coronavirus disease-19 pandemic	Dec/04/2020
Transcriptome analysis of cepharanthine against a SARS-CoV-2-related coronavirus	Sep/14/2021
Docking Analysis of Some Bioactive Compounds from Traditional Plants against SARS-CoV-2 Target Proteins	Apr/20/2022
Cepharanthine: a review of the antiviral potential of a Japanese-approved alopecia drug in COVID-19	Jun/10/2020
Bioavailability Enhancement of Cepharanthine via Pulmonary Administration in Rats and Its Therapeutic Potential for Pulmonary Fibrosis Associated with COVID-19 Infection	Mar/23/2022
In Silico Screening of Natural Products as Potential Inhibitors of SARS-CoV-2 Using Molecular Docking Simulation	Mar/15/2022
Structural insights into SARS-CoV-2 spike protein and its natural mutants found in Mexican population	Apr/30/2022
Identifying SARS-CoV-2 Entry Inhibitors through Drug Repurposing Screens of SARS-S and MERS-S Pseudotyped Particles.	Oct/19/2020
Large Screening Identifies ACE2 Positively Correlates With NF-kappaB Signaling Activity and Targeting NF-kappaB Signaling Drugs Suppress ACE2 Levels	Nov/19/2021
Evaluating cepharanthine analogues as natural drugs against SARS-CoV-2	Dec/09/2021
Comparison of viral RNA-host protein interactomes across pathogenic RNA viruses informs rapid antiviral drug discovery for SARS-CoV-2	Nov/04/2021
Natural Products, Alone or in Combination with FDA-Approved Drugs, to Treat COVID-19 and Lung Cancer.	Jun/18/2021

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