sunnuntai 21. maaliskuuta 2021

Carvativir is science and humanity with a designation of origin

  • Antivirals against coronavirus.
  • Carvativir, a world-class scientific effort.
  • Carvativir saves lives.
  • In silico study the inhibition of angiotensin converting enzyme 2 receptor of COVID-19  - Isothymol present in essential oils of plant as thyme and oregano - PubMed.
  • Then it gets more interesting when you Google #isotimol. You find this direct connection between #Carvativir, the proposed brand name of #isothymol for treatment of #COVID19, posted online by Laboratorio Farmacológico de Venezuela.

 

Carvativir is science and humanity with a designation of origin


 
By
 memesita
 -

Any Venezuelan grandmother can attest to the healing properties of thyme. Its use as a condiment is widespread throughout the world, but also, depending on the disease, in infusion, powder, oil or consumed directly from the plant, it offers relief from various ailments; it is anti-inflammatory, antiseptic, antidiarrheal, bronchodilator and even fungicidal. 

The Egyptians knew of its power, who used it among the antibacterial mixture that helped them embalm their mummies, and today modern pharmaceutical companies use it in at least ten commercially used drugs, according to the Vademecum.

The therapeutic capacity of thyme has been on the lips of many people this week when the presentation of the drug Carvativir, a broad-spectrum antiviral with Venezuelan stamp, capable of attenuating the symptoms of covid-19 and therefore contributing to a faster recovery and even to survival. The essential oil of this plant is its raw material through a phytochemical compound that is also found in oregano: isothymol, in turn placed in squalene, which works as an excipient.

The history of Carvativir began in silence nine months ago, with preclinical trials and clinical studies in patients with mild, moderate and critical symptoms, in sentinel hospitals and in the Poliedro de Caracas. To ensure reliable research results, it was tested at different stages in laboratories in Venezuela, Turkey and the United States. What was discovered more than met expectations and now the country makes this discovery available to the world under the universal precept of solidarity. Let’s delve into this history of science and innovation with a Venezuelan stamp.

Antivirals against coronavirus

Although the development of vaccines against covid-19 has been making headlines for a year, work on formulating antiviral treatments to alleviate the effects of the disease has been less blockbuster news.

At the beginning of the pandemic, drugs already approved for other infections sounded, which according to the scientific community could be effective treatments against this new virus. Chloroquine, originally used against malaria and some autoimmune diseases such as lupus or rheumatoid arthritis, appeared as a promising option; also Remdesivir, a broad spectrum antiviral that is in the clinical trial phase against Ebola. Today both drugs do not have the approval of the WHO with regard to the treatment of the coronavirus.

Another drug is Favipiravir, developed in Japan and approved to treat the flu, from which in turn two Russian-label drugs were born: Avifavir and Coronavir.

As a new drug, this week, in parallel with the announcement of Carvativir, Aplidin was presented in Spain, an antiviral drug made from plitidepsin, isolated from a species of sea squirt called aplidium albicans, which is found in shallow waters. of all the world. This antiviral bears the seal of the PharmaMar laboratory and, they say, reduces the viral load of SARS-Cov-2 by almost one hundred percent.

But unlike the Venezuelan drug, Aplidin has only been tested in two mice, it has not had clinical tests, ergo, its effectiveness in humans is unknown. In this context, the Venezuelan drug appeared.

Carvativir, a world-class scientific effort

Carvativir is produced by Labfarven, Laboratorio Farmacológico de Venezuela CA, and its development was a collective delivery by the Ministry of Science and Technology, the Ministry of Health, the Venezuelan Institute of Scientific Research (Ivic), the Rafael National Institute of Hygiene Rangel and the National Service of Medicine and Forensic Sciences.

The details of this Venezuelan medical innovation are systematized in scientific reports that are awaiting publication in specialized international journals. The drug will be delivered to the World Health Organization (WHO) with the results of the antiviral efficacy and the mechanism of action of the isothymol compound for its respective international certification.

According to the global summary of the investigation, the patent had an approval in formal examination on December 14, 2020. Prior to that, in its preclinical phases of testing, the drug had the in vitro (Petri dish), developed by the Venezuelan Institute of Scientific Research (IVIC) and Laboratorios Carmed (Turkey), which consisted of a test carried out in mice, while the in silico test (test with computer models), was carried out by Autodock Vina (Venezuela), which developed the molecular simulation model.

The report states that clinical phases I and II were carried out between June and July 2020. One hundred patients participated in the clinical trial and safety and dosage were measured. (See below: 'Phase I and II. Isothymol Antiviral Activity in COVID-19 Patients')

In this clinical study on the antiviral and immunomodulatory activity of the recombined isothymol compound against the SARS-CoV-2 agent in covid-19 patients, researchers from the R&D Department, J&R Drugstore, Venezuela Pharmacological Laboratory (Labfarven), Hospital participated. Dr. Domingo Luciani and the National Service of Medicine and Forensic Sciences (Senamecf).

In phase III (August-November 2020), the multicenter, randomized, double-blind clinical trial was carried out with placebo (a tool of the scientific method used to prevent the results of an investigation from being influenced by the placebo effect), with the participation of 600 patients. Of this number, half with isothymol (experimental phase) and half with placebo (control phase).

The Bioethics Committee of the Hospital Universitario Periférico Dr. Miguel Ángel Rangel measured the safety, tolerability and antiviral and immunomodulatory activity of the compound. They indicated that in the clinical and preclinical tests performed on the patients are: Complete hematology, Dimero D, Ferritin, Fibrinogen, PT and PTT, IgM, IgG, IL-6, C-reactive protein (CRP), chest X-ray, CT and RT-PCR, which were processed in the Immuno XXI laboratories (Caracas, Venezuela) and Mayo Clinic (Minnesota, USA).

Likewise, the report states that additional tests were carried out on the accelerated stability and the microbiological study of isothymol (Carmed, Turkey) and gas chromatography with mass spectrometry, as well as the infrared absorption spectroscopy FT-IR, in charge of the IVIC .

Carvativir saves lives

In simple words, the Venezuelan drug saves lives because by tackling the symptoms of the disease it does not allow the patient to get worse to the point of no return. It was explained by Raúl Ojeda Rondón, the principal investigator of the project that designed the Carvativir, in recent statements. 


 https://twitter.com/PresidencialVen/status/1373779846090928128?s=20

“Carvativir presents scientifically, with evidence, a therapeutic action. (…) Carvativir reduces hospital recovery time because it accelerates the immune response. That’s part of the Venezuela findings. It was determined that it has antiviral therapeutic activity. The molecule inhibits viral replication in human cells. The viral load is decreasing. It also enhances immunomodulatory powers. It diminishes, what we call in medicine the cytokine storm, which is nothing more than the exaggerated response of the immune system, what is known as lung inflammation through atypical pneumonia due to covid-19. That’s where the intubation process comes in, ”he highlighted.

Now comes phase IV of the drug, which is mass production and pharmacovigilance. The scientific team that built this achievement is inviting the WHO to Venezuela to certify it. “We are going to open ourselves to all the scientific communities of the country and abroad so that they can see what we have obtained up to today,” he said.

Everything was ratified by President Nicolás Maduro when he officially presented the Venezuelan discovery: “The Carvativir passed all the studies; it already has patents and sanitary registration in our country. This drug has been shown to be 100% effective against the virus. ” Carvativir will be distributed throughout the national public system for the treatment of the pandemic virus and constitutes a medical advance that Venezuela wants to share with the world for the joint fight against the new disease that until now has not given respite.

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Carvativir can block the activity of the angiotensin converting enzyme 2 (ACE2)

Who or what’s behind the Carvativir?


January 26, 2021




The Venezuela Pharmacological Laboratory (Labfarven) is behind the research supporting using Carvativir as an efficient drug in opposition to coronavirus. The researchers related to the undertaking: 
Raúl Ojeda, Jheam Campos, Vanesa Martínez, Yanuacelis Cruz, Ángel López and Orlando Salgado are half, along with Labfarven, of the Analysis and Growth Division of the J&R Drugstore Analysis Heart, the Domingo Luciani Hospital and the Nationwide Service of Drugs and Forensic Sciences.

The publications supporting the analysis are from September 2020. They determine the compound isothymol (isothymol), energetic precept of Carvativir, as an efficient antiviral in opposition to the agent Sars-Cov-2, which causes covid-19.

Research point out that the analysis has gone via three phases. And though it appears to be a superb inhibitory drug, there may be nonetheless an extended option to go to ensure its appropriate utility.

It might grow to be, sure, “In a strong immunomodulator, which, along with inhibiting the virus in its preliminary replication section, might counteract its results already put in, to fight not solely replication and its viral motion, but additionally the cytokine storm, which is essentially the most feared complication because the pathophysiological perspective “, as Ricardo León, specialist in Inner Drugs and researcher on the Venezuelan Well being, Surroundings and Social Impression Observatory, factors out in a observe printed by La Radio del Sur.


The energetic precept of Carvativir

“Isothymol (isothymol), the energetic precept of Carvativir, is a selective inhibitor of the primary protease of the virus, and in flip permits highly effective immunomodulatory and anti inflammatory actions (in vivo)”, was laid out in one of many paperwork.

“It was administered off-label to 100 hospitalized sufferers with COVID-19 (50 with supplemental oxygen, 10 with mechanical air flow and 40 asymptomatic), 40 of whom had elevated oxygen necessities initially. Throughout a 7 to 14 day course of therapy, initiation of isothymol (isothymol) therapy was related to higher oxygenation in most sufferers, typically inside 1 to three days, and had no discernible toxicity, “he added.



In September 2020, Maduro spoke for the primary time about Carvativir, which he known as the miraculous droplets. He then introduced them up when discussing the DR10 molecule in October. Mentioned they put 10 drops underneath their tongue, each 4 hours.

The announcement of the regime

Nicolás Maduro introduced this Sunday that the regime would start the manufacturing and distribution of Carvativir, a drugs that he described as miraculous to reverse the results of the coronavirus. He stated that it will be mass produced so that every one well being facilities within the nation can have the drug.

The energetic substance in Carvativir is isothymol (isothymol).

In September 2020, Maduro spoke for the primary time about Carvativir, which he known as the miraculous droplets. He then introduced them up when discussing the DR10 molecule in October. He stated they put 10 drops underneath the tongue each 4 hours.

“We have now an antiviral that’s going to be a stick in opposition to the coronavirus. These miraculous droplets which can be in section 3 and molecular testing interval have been those that lifted Castro Soteldo from covid-19 ”, he highlighted.

Maduro affirmed that the Minister of Agriculture and Lands, Wilmar Castro Soteldo, was cured in simply three days.

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Phase I and II. Isothymol Antiviral Activity in COVID-19 Patients (Spanish Edition) Paperback - September 11, 2020

de RAUL OJEDA (Author), Jheam Campos (Author), & 4 más

In the present study, the antiviral and immunomodulatory activity of Isothymol was investigated against the SARS-CoV-2 agent that causes COVID-19 disease in asymptomatic and symptomatic patients (phase I, II and III). Isothymol, is a selective inhibitor of the main protease of the virus, and in turn enables powerful immunomodulatory and anti-inflammatory activities (in vivo).

100 hospitalized COVID-19 patients (50 on supplemental oxygen, 10 on mechanical ventilation, and 40 asymptomatic) were administered off-label, 40 of whom had increased oxygen requirements at baseline. During a 7 to 14 day course of treatment, initiation of isothymol treatment was associated with better oxygenation in most patients, often within 1 to 3 days, and had no discernible toxicity. Measures of inflammation (C-reactive protein and interleukin-6 (IL-6)) rapidly normalized in most patients, as did lymphopenia, in correlation with better oxygenation. At the end of isothymol treatment, 46 of 50 (92%) patients in the supplemental oxygen cohort had been discharged to room air, and 9 of 10 (90%) patients in the mechanical ventilation cohort had been successfully extubated. , with 6 of 8 (75%) discharged in ambient air.

Ex vivo analysis revealed hypersensitivity of inflammatory mediators (macrophages and type I interferons) and significantly elevated histamine production, as evidenced by autophosphorylation, and increased IL-6 production in blood monocytes of severe COVID-19 patients. compared to blood monocytes from healthy volunteers. 

In the case of asymptomatic patients (40 of 40) 14 days after treatment with recombinant isothymol, the positive manifestation of immunoglobulin G (IgG) and negative for immunoglobulin M (IgM) indicative of the disease overcoming, which were confirmed with RT-PCR assays at a mean of 30 days respectively (20 - 40 days).

https://www.amazon.com/-/es/RAUL-OJEDA/dp/B08HTG6K6W

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. 2020 May 14;1-14.

 doi: 10.1080/07391102.2020.1763199. Online ahead of print.

In silico study the inhibition of angiotensin converting enzyme 2 receptor of COVID-19 by Ammoides verticillata components harvested from Western Algeria

Imane Abdelli 1 2, Faiçal Hassani 3, Sohayb Bekkel Brikci 3, Said Ghalem 2
Affiliations 

Free PMC article

Abstract

The objective of this present study is to focus on the in silico study to screen for an alternative drug that can block the activity of the angiotensin converting enzyme 2 (ACE2) as a receptor for SARS-CoV-2, potential therapeutic target of the COVID-19 virus using natural compounds (Isothymol, Thymol, Limonene, P-cymene and γ-terpinene) derived from the essential oil of the antiviral and antimicrobial plant Ammoides verticillata (Desf.) Briq. which is located in the occidental Algeria areas. This study reveals that Isothymol, a major component of this plant, gives the best docking scores, compared to, the co-crystallized inhibitor β-D-mannose of the enzyme ACE2, to Captropil drug as good ACE2 inhibitor and to Chloroquine antiviral drug also involved in other mechanisms as inhibition of ACE2 cellular receptor. In silico (ADME), drug-likeness, PASS & P450 site of metabolism prediction, pharmacophore Mapper showed that the compound Isothymol has given a good tests results compared to the β-D-mannose co-crystallized inhibitor, to Captopril and Chloroquine drugs. Also the other natural compounds gave good results. The Molecular Dynamics Simulation study showed good result for the Isotymol- ACE2 docked complex. This study revealed for the first time that Isothymol is a functional inhibitor of angiotensin converting enzyme 2 activity and the components of essential oils Ammoides verticillata can be used as potential inhibitors to the ACE2 receptor of SARS-CoV-2.Communicated by Ramaswamy H. Sarma.

Keywords: Ammoides verticillata; Angiotensin converting enzyme 2; COVID-19; isothymol; molcular docking.

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