Skip to main content

New Look on Antihypertensive Therapy

 

Angiotensin converting enzyme 2

 

Angiotensin converting enzyme 2, or ACE2, is an exopeptidase expressed primarily by vascular endothelial cells in the heart and kidneys, but also in respiratory epithelia[1] and in the gastrointestinal tract. It is the target of several coronaviruses, including SARS-CoV and SARS-CoV-2.

2 Biochemistry

ACE2 is a transmembrane metallocarboxypeptidase composed of 805 amino acids. Zinc and chloride ions act as cofactors. The extracellular region consists of two domains, a zinc metallopeptidase domain and a C-terminal collectrin homology domain. The enzyme exhibits homology to angiotensin converting enzyme (ACE).

ACE2 is encoded by the ACE2 gene on the X chromosome (gene locus Xp22.2). In addition to being expressed as a transmembrane protein, a soluble form exists in serum.

3 Function

ACE2 cleaves angiotensin II into angiotensin (1-7), which has anti-inflammatory and lung protective effects via MAS and AT2 receptors.

4 Clinical

4.1 Infectiology

ACE2 serves as a major entry point for some coronaviruses. The pathogens bind to the enzyme with their spike proteins and enter the host cell by subsequent fusion.[2] ACE2 expression increases from the pharynx to the alveoli. In addition, SARS-CoV-2 is thought to have a higher affinity for ACE2 than SARS-CoV. This would explain more rapid and effective viral transmission in the COVID-19 pandemic.

Patients taking drugs that increase the expression of ACE2 - for example, ACE inhibitors or sartans, may be at higher risk of infection and should be switched to calcium antagonists, according to some authors.[3][4] In contrast, the relevant professional societies see no need for action at this time (4/2020).[5][6]

4.2 Pharmacology

Human recombinant ACE2 (APN01) is an experimental therapeutic approach being tested in acute respiratory distress syndrome (ARDS) and pulmonary hypertension.[7] Furthermore, it is currently (2020) being tested for the treatment of COVID-19.[8][9]

5 Sources

1. jump up ↑ Hong Peng Jia et al. ACE2 Receptor Expression and Severe Acute Respiratory Syndrome Coronavirus Infection Depend on Differentiation of Human Airway Epithelia, J Virol. 2005 Dec; 79(23): 14614-14621, retrieved 2020 Mar 27.

2. jump up ↑ Kuba K et al. A crucial role of angiotensin converting enzyme 2 (ACE2) in SARS coronavirus-induced lung injury, Nat Med. 2005 Aug;11(8):875-9. epub 2005 Jul 10, retrieved 2020 Mar 30.

3. jump up ↑ Zheng Y et al. COVID-19 and the cardiovascular system, Nat Rev Cardiol (2020), retrieved 30 Mar 2020.

4. jump up ↑ Fang, L. et al. Are patients with hypertension and diabetes mellitus at increased risk for COVID-19 infection?, The Lancet, March 2020, retrieved 27/03/2020.

5. jump up ↑ ESC Position Statement of the ESC Council on Hypertension on ACE Inhibitors and Angiotensin Receptor Blockers, retrieved March 27, 2020.

6. jump up ↑ The Renal Association, UK position statement for patients: novel corona virus infection and the use of blood pressure medications. retrieved 03/27/2020.

7. jump up ↑ Zhang H, Baker A Recombinant human ACE2: acing out angiotensin II in ARDS therapy, Crit Care. 2017 Dec 13;21(1):305, retrieved 2020 Mar 30.

8. jump up ↑ Zhang H et al. Angiotensin-converting enzyme 2 (ACE2) as a SARS-CoV-2 receptor: molecular mechanisms and potential therapeutic target, Intensive Care Med. 2020 Apr;46(4):586-590, retrieved 2020 Mar 30.

9. upjump ↑ clinicaltrials.gov APN01, retrieved 03/30/2020.

 

Mar 19, 2020May 7, 2020

CoViD-19 and ACE inhibitors.

The disease is often moderate or even asymptomatic. However, severe courses can occur, usually manifesting as pneumonia. In some of the seriously ill patients, severe cardiovascular damage is also observed.

For people with heart disease, the disease - which is caused by the SARS-CoV-2 virus - thus appears to be particularly dangerous.

Angiotensin-converting enzyme 2 (ACE2) plays a major role in the body's water balance. ACE inhibitors lower blood pressure and reduce afterload - which also makes them very useful in treating heart failure disease.

ACE2 are particularly abundant in the heart and lungs. Currently, attention is focused on this enzyme because ACE2 has been identified as a functional receptor for the coronaviruses SARS-CoV and SARS-CoV-2.

It appears that the amount of ACE2 increases by taking ACE2 inhibitors in response. Thus, the body responds to inhibition of these receptors by increasing potential docking sites.

It has not yet been proven whether this mechanism promotes or exacerbates the disease!

Up-regulating ACE2 may also have benefits: The enzyme protects the heart and vasculature by cleaving angiotensin II-which promotes hypertension, edema, and tissue damage-and thereby inactivating it.

In SARS-CoV infection, ACE2 is downregulated as an antiviral protective measure: Angiotensin II can then promote severe tissue damage during infection. ACE inhibitors and sartans could therefore be helpful because they slow down angiotensin II formation or block the corresponding receptor, respectively ...

It is a fact that special attention is paid to patients with underlying cardiovascular disease in connection with covid-19 disease. Recently, experts from the U.S. Cardiac Society (ACC) considered the viral epidemic from a cardiology perspective in an official letter of recommendation. The society makes nine recommendations for managing the coronavirus epidemic.

The experts recommend that "consistent use of guideline-based therapy with plaque-stabilizing agents (statins, beta blockers, ACE inhibitors, ASS) provides additional protection for cardiac patients, and such treatment should be tailored to individual patients." Accordingly, these experts do not currently consider ACE inhibitors to be critical.

That this is a preliminary assessment is reflected in point 9 of the recommendation: here, the experts point out that little is currently known about coronavirus and physicians should be prepared for new recommendations as more information becomes available.

Source: www.pharmazeutische-zeitung.de/

 

 

 

 

 

 

 

What Teaches Us the Autoimmune Theory?

 

The members of the family Coronaviridae, a monophyletic cluster in the order Nidovirales, are enveloped, positive stranded RNA viruses of three classes of vertebrates: mammals (corona -and toroviruses), birds (coronaviruses) and fish (bafiniviruses). Virions are spherical, 120–160 nm across (Coronavirinae), bacilliform, 170–200×75–88 nm (Bafinivirus) or found as a mixture of both, with bacilliform particles characteristically bent into crescents (Torovirus). The particles are typically decorated with large, club- or petal-shaped surface projections (the “peplomers” or “spikes”), which in electron micrographs of spherical particles create an image reminiscent of the solar corona. This inspired the name of the “true” coronaviruses (now grouped in the subfamily Coronavirinae), which was later adopted for the whole family. Nucleocapsids are helical and can be released from the virion by treatment with detergents. Whereas the coronavirus nucleocapsid appears to be loosely-wound, those of the Torovirinae are distinctively tubular.

In terms of genome size and genetic complexity, the Coronaviridae are the largest RNA viruses identified so far, rivaled only by the okaviruses, large nidoviruses of invertebrates assigned to the family Roniviridae. Replication has been studied in detail only for coronaviruses, but the limited data available for toro- and bafiniviruses suggest that the latter viruses use essentially similar strategies. Virions attach to dedicated host cell surface receptors via their spikes and release their genome into the target cell via fusion of the viral envelope with the plasma membrane and/or the limiting membrane of an endocytic vesicle. The entire replication cycle takes place in the cytoplasm and involves the production of full-length and subgenome-sized (sg) minus-strand RNA intermediates with the viral genome serving both as mRNA for the replicase polyproteins and as a template for minus-strand synthesis. RNA synthesis is catalyzed by an as yet poorly characterized replication–transcription complex, composed of viral and host proteins and associated (at least in coronaviruses) with an interconnected network of modified intracellular membranes and double-membrane vesicles that are presumably endoplasmic reticulum (ER)-derived.

The conclusion is that Corona viruses are wide spread in nature, affect animals and humans. They enter the cells through a receptor ACE 2 which is found on endothelial cells of blood vessels, which is amongst all also responsible for regulating blood pressure.

So if we consume those animals our immune system gets in contact with those receptors which are big protein molecules and our immune system produces antibodies against those receptors. And this way of thinking could explain the origin of essential hypertension.

We know that ACE-blockers are an antihypertensive therapy because they block the converting of angiotensin I into angiotensin II. The angiotensin II formed interacts with angiotensin II receptors (AT receptors). Activation of the AT1 receptor can cause contraction primarily in blood vessels. In the kidney, constriction of efferent blood vessels keeps the glomerular filtration rate as constant as possible. In the adrenal gland, angiotensin II stimulates aldosterone and epinephrine release, and in the pituitary gland, a release of vasopressin. The sensation of thirst is also attributed to acute stimulation of AT1 receptors in the hypothalamus. Chronic stimulation of the AT1 receptor, on the other hand, leads to stimulation of mitogenic effects and thus, for example, to hypertrophy of the heart. Acute and chronic effects of angiotensin II on the AT1 receptor can be suppressed indirectly by ACE inhibitors and directly by AT1 receptor antagonists (sartans) or saralasin.

 

Angiotensin II also shows a high affinity for AT2 receptors. The importance of these receptors in the effects mediated by angiotensin II, however, is controversial. Animal studies in mice provided evidence that the action at AT2 receptors has an attenuating influence on the effects at AT1 receptors in the sense of counteracting them.

 

Angiotensinamide, a derivative of angiotensin II, is a cardiostimulatory and blood pressure-increasing drug.

 

Through the knowledge which we acquired reading “The Theory Of Autoimmunity” we suspect that anti ACE 2 receptor antibodies could activate the ACE 2 receptor thus causing essential arterial hypertension and this is a question that affects major part of the population on Earth.


For more: https://www.amazon.com/dp/B09NGSF57G/ref=mp_s_a_1_2?crid=PDMS10VW4812&keywords=tanya+guleria&qid=1639247917&sprefix=tanya+gul%2Caps%2C178&sr=8-2

 

 

 

 

 

 

 

 

Comments

Popular posts from this blog

In Search of The Perfect Sleep Aid

 For many years, modern medicine has been searching for the perfect sleeping pills. Sleeping pills are a special topic in medicine because they have a lot to do with addiction medicine. Of course, not every sleeping pill can cause addiction, but lighter sleeping pills such as valerian tablets, doxylamine succinate (contained in Schlafsterne), melatonin (or Circadin) have short and insufficient effects. Benzodiazepines, on the other hand, relieve anxiety, which often leads to sleep disorders and are often used by GPs as sleeping pills, although this is not correct. Antidepressants such as mirtazapine are more often used as sleeping pills, but patients often complain of fatigue and drowsiness after their use, which is incompatible with driving, for example. Z-drugs are the 3rd choice of sleep medicine, they have a long and sufficient effect, but can be very addictive. There are patients who struggle for years with addiction to zolpidem, or zopiclone. Many GPs give up in this fight and pr

Factors influencing Osteoclasts and Osteoblasts

Hormones are possibly the most crucial modulators of bone formation. It is well established that estrogen, parathyroid hormone, and to a lesser extent testosterone, are essential for optimal bone development and maintenance. Of these, estrogen is now believed to have the most direct effect on bone cells, interacting with specific proteins, or receptors, on the surface of osteoblasts and osteoclasts. This interaction sets off a complex chain of events within the cells, increasing osteoblast activity while at the same time interfering with osteoblast-osteoclast communication – one of the ironies of bone remodeling is that the osteoblasts release factors that stimulate osteoclasts and drive bone resorption, as we shall see below. Estrogen effects are mediated through one specific type of cell surface receptor called the estrogen receptor alpha (ERα), which binds and transports the hormone into the nucleus of the cell where the receptor-hormone complex acts as a switch to turn on s