Technological prospection of Diminazene Aceturate, an Angiotensin II Converting Enzyme activator, in front of diarrheic disorders

Diarrhea, which is a gastrointestinal disease, has as its main characteristic the rapid passage of gastric contents through the intestine, which leads to the loss of water and electrolytes and consequent dehydration. The most common fluid replacement is the use of oral rehydration solution (ORS) together with the use of the drug loperamide. However, the use of this medication can cause severe bacteremia followed by sepsis and even death. Currently, there is no effective pharmacological treatment for diarrhea, therefore, it is noted the importance of seeking new therapeutic targets for the treatment of this disease. Thus, the aim of the present study was to conduct a research on the biological activities already described for Diminazene Aceturate with a special focus on antidiarrheal agents. For this, a survey was carried out, through patent filing searches, in the USPTO, EPO, WIPO and INPI databases, using keywords and Boolean operators. Thus, it was found in the international patent databases the number of documents referring to the use of Diminazene Aceturate in several areas, mainly in the pharmaceutical industry, but with a relatively low number of documents regarding the description of possible antidiarrheal action of the compound under study , which reinforces the innovative character of research involving the use of Diminazene Aceturate as an antidiarrheal agent.

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Bioactive Secondary Metabolites from Endophytic Fungi

Current Medicinal Chemistry ◽

10.2174/0929867326666190916144709 ◽

2020 ◽

Vol 27 (11) ◽

pp. 1836-1854 ◽

Cited By ~ 5

Author(s):

Elena Ancheeva ◽

Georgios Daletos ◽

Peter Proksch

Keyword(s):

Secondary Metabolites ◽

Endophytic Fungi ◽

Host Plants ◽

Biological Activities ◽

Cytotoxic Agents ◽

Special Focus ◽

Plant Metabolites ◽

Direct Production ◽

Bioactive Secondary Metabolites ◽

Fungal Genes

Background: Endophytes represent a complex community of microorganisms colonizing asymptomatically internal tissues of higher plants. Several reports have shown that endophytes enhance the fitness of their host plants by direct production of bioactive secondary metabolites, which are involved in protecting the host against herbivores and pathogenic microbes. In addition, it is increasingly apparent that endophytes are able to biosynthesize medicinally important “phytochemicals”, originally believed to be produced only by their host plants. Objective: The present review provides an overview of secondary metabolites from endophytic fungi with pronounced biological activities covering the literature between 2010 and 2017. Special focus is given on studies aiming at exploration of the mode of action of these metabolites towards the discovery of leads from endophytic fungi. Moreover, this review critically evaluates the potential of endophytic fungi as alternative sources of bioactive “plant metabolites”. Results: Over the past few years, several promising lead structures from endophytic fungi have been described in the literature. In this review, 65 metabolites are outlined with pronounced biological activities, primarily as antimicrobial and cytotoxic agents. Some of these metabolites have shown to be highly selective or to possess novel mechanisms of action, which hold great promises as potential drug candidates. Conclusion: Endophytes represent an inexhaustible reservoir of pharmacologically important compounds. Moreover, endophytic fungi could be exploited for the sustainable production of bioactive “plant metabolites” in the future. Towards this aim, further insights into the dynamic endophyte - host plant interactions and origin of endophytic fungal genes would be of utmost importance.

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Issues and Controversies in the Evolution of Oral Rehydration Therapy (ORT)

Tropical Medicine and Infectious Disease ◽

10.3390/tropicalmed6010034 ◽

2021 ◽

Vol 6 (1) ◽

pp. 34

Author(s):

David Nalin

Keyword(s):

Pediatric Patients ◽

Oral Rehydration Therapy ◽

Sodium Balance ◽

Plain Water ◽

Oral Glucose ◽

Oral Rehydration ◽

Low Sodium ◽

Current Review ◽

The Subject ◽

Rehydration Solution

The original studies demonstrating the efficacy of oral glucose-electrolytes solutions in reducing or eliminating the need for intravenous therapy to correct dehydration caused by acute watery diarrheas (AWD) were focused chiefly on cholera patients. Later research adapted the oral therapy (ORT) methodology for treatment of non-cholera AWDs including for pediatric patients. These adaptations included the 2:1 regimen using 2 parts of the original WHO oral rehydration solution (ORS) formulation followed by 1 part additional plain water, and a “low sodium” packet formulation with similar average electrolyte and glucose concentrations when dissolved in the recommended volume of water. The programmatic desire for a single ORS packet formulation has led to controversy over use of the “low sodium” formulations to treat cholera patients. This is the subject of the current review, with the conclusion that use of the low-sodium ORS to treat cholera patients leads to negative sodium balance, leading to hyponatremia and, in severe cases, particularly in pediatric cholera, to seizures and other complications of sodium depletion. Therefore it is recommended that two separate ORS packet formulations be used, one for cholera therapy and the other for non-cholera pediatric AWD.

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Are oral rehydration solutions optimized for treating diarrhea?

Nutrition and Health ◽

10.1177/0260106021991641 ◽

2021 ◽

pp. 026010602199164

Author(s):

Samuel N Cheuvront ◽

Robert W Kenefick ◽

Laura Luque ◽

Katherine M Mitchell ◽

Sadasivan Vidyasagar

Keyword(s):

Water Absorption ◽

Intestinal Absorption ◽

Turning Point ◽

Oral Rehydration Solution ◽

Salt Water ◽

Food Science ◽

Oral Rehydration ◽

Rehydration Solutions ◽

Rehydration Solution ◽

Stool Volume

Background: A historical turning point occurred in the treatment of diarrhea when it was discovered that glucose could enhance intestinal sodium and water absorption. Adding glucose to salt water (oral rehydration solution, ORS) more efficiently replaced intestinal water and salt losses. Aim: Provide a novel hypothesis to explain why mainstream use of ORS has been strongly recommended, but weakly adopted. Methods: Traditional (absorptive) and novel (secretory) physiological functions of glucose in an ORS were reviewed. Results: Small amounts of glucose can stimulate both intestinal absorption and secretion. Glucose can exacerbate a net secretory state and may aggravate pathogen-induced diarrhea, particularly for pathogens that affect glucose transport. Conclusion: A hypothesis is made to explain why glucose-based ORS does not appreciably reduce diarrheal stool volume and why modern food science initiatives should focus on ORS formulations that replace water and electrolytes while also reducing stool volume and duration of diarrhea.

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