scholarly journals 5-amino levulinic acid inhibits SARS-CoV-2 infection in vitro

2020 ◽  
Author(s):  
Yasuteru Sakurai ◽  
Mya Myat Ngwe Tun ◽  
Yohei Kurosaki ◽  
Takaya Sakura ◽  
Daniel Ken Inaoka ◽  
...  
Keyword(s):  
Amino Acid ◽  
Dietary Supplement ◽  
Causative Agent ◽  
Levulinic Acid ◽  
Antiviral Drug ◽  
Anticancer Therapy ◽  
Antiviral Effects ◽  
Amino Levulinic Acid ◽  
High Bioavailability

AbstractThe current COVID-19 pandemic requires urgent development of effective therapeutics. 5-amino levulinic acid (5-ALA) is a naturally synthesized amino acid and has been used for multiple purposes including as an anticancer therapy and as a dietary supplement due to its high bioavailability. In this study, we demonstrated that 5-ALA treatment potently inhibited infection of SARS-CoV-2, a causative agent of COVID-19. The antiviral effects could be detected in both human and non-human cells, without significant cytotoxicity. Therefore, 5-ALA is a candidate as an oral antiviral drug for COVID-19.

scholarly journals 5-amino levulinic acid inhibits SARS-CoV-2 infection in vitro

2021 ◽  
Vol 545 ◽  
pp. 203-207
Author(s):  
Yasuteru Sakurai ◽  
Mya Myat Ngwe Tun ◽  
Yohei Kurosaki ◽  
Takaya Sakura ◽  
Daniel Ken Inaoka ◽  
...  
Keyword(s):  
Levulinic Acid ◽  
Amino Levulinic Acid

The influence of storage conditions on delta amino levulinic acid induced toxicity and phototoxicity in vitro

2006 ◽  
Vol 3 (1) ◽  
pp. 35-45 ◽  
Author(s):  
Aurelie Furiga ◽  
David Olivier ◽  
Marc Baud’huin ◽  
Ludovic Bourre ◽  
Andresz Bugaj ◽  
...  
Keyword(s):  
Levulinic Acid ◽  
Storage Conditions ◽  
Amino Levulinic Acid

Molecular adduct of amantadine ferulate presents a pathway for slowing in vitro/vivo releases and raising synergistic antiviral effects via dual optimization salification strategy

CrystEngComm ◽  
2021 ◽  
Author(s):  
Yuan-Yuan Niu ◽  
Ling-Yang Wang ◽  
Yue-Ming Yu ◽  
Yan-Tuan Li ◽  
Zhi-Yong Wu ◽  
...  
Keyword(s):  
Antiviral Drug ◽  
Antiviral Effects ◽  
Molecular Adduct ◽  
Molecular Salt

The first synthesized antiviral drug-nutriment molecular salt demonstrating simultaneous slowed-release and synergistically enhanced antiviral effects is studied theoretically and experimentally.

scholarly journals Anti-Respiratory Syncytial Virus Activity of Plantago asiatica and Clerodendrum trichotomum Extracts In Vitro and In Vivo

Viruses ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 604 ◽  
Author(s):  
Kiramage Chathuranga ◽  
Myun Soo Kim ◽  
Hyun-Cheol Lee ◽  
Tae-Hwan Kim ◽  
Jae-Hoon Kim ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Antiviral Drug ◽  
A549 Cells ◽  
Phenolic Glycoside ◽  
Antiviral Effects ◽  
Plantago Asiatica ◽  
Syncytial Virus ◽  
Herb Extract

The herbs Plantago asiatica and Clerodendrum trichotomum have been commonly used for centuries in indigenous and folk medicine in tropical and subtropical regions of the world. In this study, we show that extracts from these herbs have antiviral effects against the respiratory syncytial virus (RSV) in vitro cell cultures and an in vivo mouse model. Treatment of HEp2 cells and A549 cells with a non-cytotoxic concentration of Plantago asiatica or Clerodendrum trichotomum extract significantly reduced RSV replication, RSV-induced cell death, RSV gene transcription, RSV protein synthesis, and also blocked syncytia formation. Interestingly, oral inoculation with each herb extract significantly improved viral clearance in the lungs of BALB/c mice. Based on reported information and a high-performance liquid chromatography (HPLC) analysis, the phenolic glycoside acteoside was identified as an active chemical component of both herb extracts. An effective dose of acteoside exhibited similar antiviral effects as each herb extract against RSV in vitro and in vivo. Collectively, these results suggest that extracts of Plantago asiatica and Clerodendrum trichotomum could provide a potent natural source of an antiviral drug candidate against RSV infection.

Implantable HDAC-inhibiting chemotherapeutics derived from hydrophobic amino acids for localized anticancer therapy

2021 ◽  
Vol 9 (1) ◽  
pp. 261-271
Author(s):  
Somnath Dharmaraj Bhagat ◽  
Abhishek Chanchal ◽  
Mansi Gujrati ◽  
Aditi Banerjee ◽  
Ram Kumar Mishra ◽  
...  
Keyword(s):  
Amino Acids ◽  
Amino Acid ◽  
Cancer Cells ◽  
Anticancer Therapy ◽  
Amino Acid Derivatives ◽  
Hdac Inhibition ◽  
Strong Potential ◽  
Hydrophobic Amino Acids

Amino acid derivatives with potent HDAC inhibition and hydrogelation abilities show strong potential against a variety of cancer cells in vitro.

scholarly journals The Petasites hybridus CO2-extract (Ze 339) blocks SARS-CoV-2 replication in vitro

2021 ◽  
Author(s):  
Lorena Urda ◽  
Matthias Heinrich Kreuter ◽  
Jürgen Drewe ◽  
Georg Boonen ◽  
Veronika Butterweck ◽  
...  
Keyword(s):  
Therapeutic Option ◽  
Antiviral Drug ◽  
Plaque Reduction Assay ◽  
Virus Variant ◽  
Antiviral Effects ◽  
Antiviral Activities ◽  
Pre Treatment ◽  
Novel Coronavirus ◽  
Original Virus

AbstractThe coronavirus disease 2019 (COVID-19), caused by a novel coronavirus (SARS-CoV-2), has spread worldwide, affecting over 250 million people and resulting in over five million deaths. Antivirals that are effective are still limited. The antiviral activities of the Petasites hybdridus CO2-extract Ze 339 were previously reported. Thus, to assess the anti-SARS-CoV-2 activity of Ze 339 as well as isopetasin and neopetasin as major active compounds, a CPE- and plaque reduction assay in Vero E6 cells was used for viral output. Antiviral effects were tested using the original virus (Wuhan) and the Delta variant of SARS-CoV-2. The antiviral drug remdesivir was used as control. Pre-treatment with Ze 339 in SARS-CoV-2 infected Vero E6 cells with either virus variant significantly inhibited virus replication with IC50 values of 0.10 and 0.40 μg/mL, repectively. The IC50 values obtained for isopetasin ranged between 0.37-0.88 μM for both virus variants, that of remdesivir between 1.53-2.37 μM. In conclusion, Ze 339 as well as the petasins potently inhibited SARS-Cov-2 replication in vitro of the Wuhan and Delta variants. Since time is of essence in finding effective treatments, clinical studies will have to demonstrate if Ze339 can become a therapeutic option to treat SARS-CoV-2 infections.

scholarly journals Combination Therapy with Fluoxetine and the Nucleoside Analog GS-441524 Exerts Synergistic Antiviral Effects against Different SARS-CoV-2 Variants In Vitro

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1400
Author(s):  
Linda Brunotte ◽  
Shuyu Zheng ◽  
Angeles Mecate-Zambrano ◽  
Jing Tang ◽  
Stephan Ludwig ◽  
...  
Keyword(s):  
Antiviral Treatment ◽  
Treatment Options ◽  
Combined Treatment ◽  
Antiviral Drug ◽  
Treatment Strategies ◽  
Antiviral Agent ◽  
Life Time ◽  
Adenosine Kinase ◽  
Antiviral Effects

The ongoing SARS-CoV-2 pandemic requires efficient and safe antiviral treatment strategies. Drug repurposing represents a fast and low-cost approach to the development of new medical treatment options. The direct antiviral agent remdesivir has been reported to exert antiviral activity against SARS-CoV-2. Whereas remdesivir only has a very short half-life time and a bioactivation, which relies on pro-drug activating enzymes, its plasma metabolite GS-441524 can be activated through various kinases including the adenosine kinase (ADK) that is moderately expressed in all tissues. The pharmacokinetics of GS-441524 argue for a suitable antiviral drug that can be given to patients with COVID-19. Here, we analyzed the antiviral property of a combined treatment with the remdesivir metabolite GS-441524 and the antidepressant fluoxetine in a polarized Calu-3 cell culture model against SARS-CoV-2. The combined treatment with GS-441524 and fluoxetine were well-tolerated and displayed synergistic antiviral effects against three circulating SARS-CoV-2 variants in vitro in the commonly used reference models for drug interaction. Thus, combinatory treatment with the virus-targeting GS-441524 and the host-directed drug fluoxetine might offer a suitable therapeutic treatment option for SARS-CoV-2 infections.

scholarly journals Studies on the Biosynthesis of Heme from Iron and Protoporphyrin

Blood ◽  
1959 ◽  
Vol 14 (4) ◽  
pp. 486-497 ◽  
Author(s):  
H. C. SCHWARTZ ◽  
G. E. CARTWRIGHT ◽  
EMIL L. SMITH ◽  
M. M. WINTROBE
Keyword(s):  
Particulate Matter ◽  
Levulinic Acid ◽  
Reduced Glutathione ◽  
Enzyme Concentration ◽  
Chicken Erythrocyte ◽  
Heme Synthesis ◽  
Enzyme Solution ◽  
Optimal Stability ◽  
Amino Levulinic Acid

Abstract 1. Additional evidence has been presented that the formation of heme in vitro from iron and protoporphyrin is enzyme dependent. 2. An enzyme solution was prepared from the active particulate matter of a chicken erythrocyte hemolysate. The enzyme is soluble in 0.15 M KCl and optimally active at pH 7.9. 3. The rate of heme synthesis was constant over the first 30 minutes and approached maximal values at 3 to 4 hours. At optimal concentrations of protoporphyrin and iron the rate of heme synthesis over the first 30 minutes was proportional to enzyme concentration. 4. The enzyme solution was 89 per cent inactivated after heating at 56 C. for 30 minutes. Optimal stability for 3 hours was at pH 7.4. It was unstable when lyophilized or on storage at 5 C. or -30 C. 5. The enzyme was inhibited by 1 x 10-2 M p-chloromercuriphenylsulfonate and 1 x 10-2 M iodoacetamide. 6. There was a 70 per cent loss of activity after dialysis of the enzyme solution for 22 hours against water. The dialyzed enzyme solution was reactivated with either reduced glutathione or cysteine. 7. The enzyme solution augmented heme synthesis in vitro from δ-amino-levulinic acid, porphobilinogen and protoporphyrin, but not from glycine.

scholarly journals A Novel Protein Drug, Novaferon, as the Potential Antiviral Drug for COVID-19

2020 ◽  
Author(s):  
Fang Zheng ◽  
Yanwen Zhou ◽  
Zhiguo Zhou ◽  
Fei Ye ◽  
Baoying Huang ◽  
...  
Keyword(s):  
Viral Replication ◽  
Antiviral Drug ◽  
Protein Drug ◽  
Clearance Rates ◽  
Open Label ◽  
Antiviral Effects ◽  
Parallel Group ◽  
Antiviral Activities ◽  
Novel Protein

AbstractBackgroundNovaferon, a novel protein drug approved for the treatment of chronic hepatitis B in China, exhibits potent antiviral activities. We aimed to determine the anti-SARS-CoV-2 effects of Novaferon in vitro, and conducted a randomized, open-label, parallel group study to explore the antiviral effects of Novaferon for COVID-19.MethodsIn laboratory, the inhibition of Novaferon on viral replication in cells infected with SARS-CoV-2, and on SARS-CoV-2 entry into healthy cells was determined. Antiviral effects of Novaferon were evaluated in COVID-19 patients with treatment of Novaferon, Novaferon plus Lopinavir/Ritonavir, or Lopinavir/Ritonavir. The primary endpoint was the SARS-CoV-2 clearance rates on day 6 of treatment, and the secondary endpoint was the time to the SARS-CoV-2 clearance in COVID-19 patientsResultsNovaferon inhibited the viral replication in infected cells (EC50=1.02 ng/ml), and protected healthy cells from SARS-CoV-2 infection (EC50=0.1 ng/ml). Results from the 89 enrolled COVID-19 patients showed that both Novaferon and Novaferon plus Lopinavir/Ritonavir groups had significantly higher SARS-CoV-2 clearance rates on day 6 than the Lopinavir/Ritonavir group (50.0% vs.24.1%, p = 0.0400, and 60.0% vs.24.1%, p = 0.0053). Median time to SARS-CoV-2 clearance were 6 days, 6 days, and 9 days for three groups respectively, suggesting a 3-dayreduction of time to SARS-CoV-2 clearance in both Novaferon and Novaferon plus Lopinavir/Ritonavir groups compared with Lopinavir/Ritonavir group.ConclusionsNovaferon exhibited anti-SARS-CoV-2 effects in vitro and in COVID-19 patients. These data justified the further evaluation of Novaferon.

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