Mini-Reviews in Organic Chemistry

Editor-in-Chief:

Renato Dalpozzo
University of Calabria
Rende
Italy

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Beneficial and Detrimental Effects of Antioxidants Use in Sports: How it is balanced?

(E-pub Abstract Ahead of Print)

Author(s): Olfa Slimeni, Ali Zaiter*, Patrick Chaimbault, Reem Omar Mohamed Salih, Andrzej Pokrywka, Sondes Sellami, Nicola Bragazzi, Maha Sellami

Journal Name: Current Nutraceuticals

Abstract:

This review aims to summarize the fundamental classes of antioxidants, the utilization of the supplement with antioxidants as ergogenic benefits in exercise and sport, the efficiency, and the consequence of their chronic uses. Antioxidants have been used for a long time in different sports disciplines and at all degrees of rivalry. The supplement with antioxidants anticipates muscle damage by reducing immune dysfunction, inflammation, and fatigue syndrome for athletes. Subsequently, antioxidant supplementation will improve the physical performances and health of athletes. Polyphenol compounds as incredible antioxidants that are abundant in numerous plants. The consumption of antioxidants could be hazardous whenever taken in high dosages. Researchers found that overdoses may cause undesirable symptoms and might grow the risk of death.

Keywords: Vitamin, Polyphenol, Flavonoids, health benefits, ergogenic effect, athletes

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/2665978602666210223150102
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Intracerebral Hemorrhage and Diabetes Mellitus: Blood-Brain Barrier Disruption, Pathophysiology, and Cognitive Impairments

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Author(s): Ghaith A. Bahadar, Zahoor A Shah*

Journal Name: CNS & Neurological Disorders - Drug Targets
Formerly Current Drug Targets - CNS & Neurological Disorders

Abstract:

There is a surge in diabetes incidence with an estimated 463 million individuals been diagnosed worldwide. Diabetes Mellitus (DM) is a major stroke-related comorbid condition that increases the susceptibility of disabling post-stroke outcomes. Although less common, intracerebral hemorrhage (ICH) is the most dramatic subtype of stroke that is associated with higher mortality, particularly in DM population. Previous studies have focused mainly on the impact of DM on ischemic stroke. Few studies have focused on impact of DM on ICH and discussed the blood-brain barrier disruption, brain edema, and hematoma formation. However, more recently, investigating the role of oxidative damage and reactive oxygen species (ROS) production in preclinical studies involving DM-ICH animal models has gained attention. But, little is known about the correlation between neuroinflammatory processes, glial cells activation, and peripheral immune cell invasion with DM-ICH injury. DM and ICH patients experience impaired abilities in multiple cognitive domains by relatively comparable mechanisms, which could get exacerbated in the setting of comorbidities. In this review, we discuss both the pathology of DM as a comorbid condition for ICH and the potential molecular therapeutic targets for the clinical management of the ICH and its recovery.

Keywords: Diabetes Mellitus, Intracerebral hemorrhage, oxidative stress, reactive oxygen species, neuroinflammation

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DOI: 10.2174/1871527320666210223145112
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SARS-CoV-2 proteins: Are they useful as targets for COVID-19 drugs and vaccines?

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Author(s): Mohammed Elimam Ahamed Mohammed*

Journal Name: Current Molecular Medicine

Abstract:

The proteins of coronavirus are classified to nonstructural, structural, and accessory. There are 16 nonstructural viral proteins beside their precursors (1a and 1ab polyproteins). The nonstructural proteins are named as nsp1 to nsp16 and they act as enzymes, coenzymes, and binding proteins to facilitate the replication, transcription, and translation of the virus. The structural proteins are bound to the RNA in the nucleocapsid (N- protein) or to the lipid bilayer membrane of the viral envelope. The lipid bilayer proteins include the membrane protein (M), envelope protein (E), and spike protein (S). Beside their role as structural proteins, they are essential for the host cells binding and invasion. The SARS-CoV-2 contains six accessory proteins which participates in the viral replication, assembly and virus- host interactions. The SARS-CoV-2 accessory proteins are orf3a, orf6, orf7a, orf7b, orf8, and orf10. The functions of the SARS-CoV-2 are not well known, while the functions of their corresponding proteins in SARS-CoV are either well known or poorly studied. Recently, the Oxford University and Pfizer and BioNTech made SARS-CoV-2 vaccines through targeting the spike protein gene. The US Food and Drug Administration (FDA) and the health authorities of the United Kingdom approved and started vaccination using the Pfizer and BioNTech mRNA vaccine. Also, The FDA of USA approved the treatment of COVID-19 using two monoclonal antibodies produced by Regeneron pharmaceuticals to target the spike protein. The SARS-CoV-2 proteins can be used for the diagnosis, as drug targets and in vaccination trials for COVID-19. For future COVID-19 research, more efforts should be done to elaborate the functions and structure of the SARS-CoV-2 proteins so as to use them as targets for COVID-19 drug and vaccines. Special attention should be drawn to extensive research on the SARS-CoV-2 nsp3, orf8, and orf10.

Keywords: nsp3, spike protein, orf3, orf8, orf10, SARS-CoV.

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1566524021666210223143243
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Latest advances in hydrogel-based drug delivery systems for optimization of metabolic syndrome treatment

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Author(s): Diego Arauna, Sekar Vijayakumar, Esteban Durán-Lara*

Journal Name: Current Medicinal Chemistry

Abstract:

Background: Drug delivery systems such as hydrogels have become relevant in cardiovascular and metabolic therapies due to their sustained and controlled release properties of drugs, versatile polymer structures, safety and biodegradability.

Results: The literature presented demonstrates that a hydrogel-based controlled release system increases the therapeutic efficacy in different components of the metabolic syndrome. Hypertension has been the most explored component with advances in vitro and murine models. However, clinical evidence in humans is scarce, and more translational studies are needed. Hydrogel-based systems for diabetes, obesity, and dyslipidemia have been little explored. Observations mainly demonstrated an increase in therapeutic efficacy, in vitro and in vivo, for the use of insulin, leptin, and natural components, such as epigallocatechin gallate. In all cases, the hydrogel systems achieve better plasma levels of the loaded compound, higher bioavailability, and low cytotoxicity; compared to conventional systems. Also, the evidence existing suggests that the development of an injectable hydrogel system for controlled release of drugs or therapeutic compounds is presented as an attractive option for MeS treatment, due to the possibility of sustained pharmacological release, no need for repeated doses, and a safe administration route.

Conclusion: The following review aims to evaluate the use of the hydrogel systems in the therapy of diabetes, obesity, hypertension, and dyslipidemia, which are the main components of metabolic syndrome.

Keywords: Hydrogel, drug delivery, injectable hydrogel, metabolic syndrome, cardiovascular diseases, biomaterials

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DOI: 10.2174/0929867328666210223141555
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Health Insurance Status of Pregnant Women and the Likelihood of Receipt of Antenatal Screening for HIV in sub-Saharan Africa

(E-pub Abstract Ahead of Print)

Author(s): Muhammad Ragaa Hussein, Deepa Dongarwar*, Rafeek A. Yusuf, Zenab Yusuf, Gambo Gumel Aliyu, Hamisu M. Salihu, George Ryan Elmessan

Journal Name: Current HIV Research

Abstract:

Background: We investigated if initiating preventive care against HIV vertical transmission by antenatal HIV screening is independent of the patients’ source of financial reimbursement for the care received in sub-Saharan Africa.

Methods: Using information from the WHO’s Global Health Expenditure Database and the Demographic Health Surveys Database for 27 sub-Saharan countries, we used Spearman’s correlation and adjusted survey logistic regression to determine the potential relationship between enrollment in health insurance and the likelihood that expectant mothers would be offered antenatal HIV screening.

Results: We found that expectant mothers covered by health insurance were more than twice as likely to be offered antenatal screening for HIV compared to the uninsured. The likelihood differed by the type of insurance plan the expectant mother carried.

Discussion: Health insurance is more of a financial tool that this study finds to be necessary to boost the uptake of preventive and therapeutic HIV care in SSA.

Conclusion: The ensuing disparity in receiving proper care could hinder achieving the goals of the 90-90-90 and the forthcoming 95-95-95 plan in SSA.

Keywords: Antenatal screening, health insurance, HIV, HIV screening, Sub-Saharan Africa; Demographic Health Survey (DHS)

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DOI: 10.2174/1570162X19666210223124835
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Laurus nobilis Linn. Inhibits Polyol Pathway Enzymes: Strategy for Managing Diabetic Complications

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Author(s): Habeeb Adebodun Bankole, Azeez Ayomide Fatai, Sulihat Motunrayo Aleshe, Mutiu Idowu Kazeem*, Abidemi Paul Kappo

Journal Name: Current Enzyme Inhibition

Abstract:

Background: The rising incidence of diabetic complications necessitate the continuous search for safer, cheaper and effective pharmacological agents. Polyol pathway is an underlying process implicated in the pathogenesis of diabetic complications. Inhibition of enzymes in the polyol pathway is a veritable means of ameliorating diabetic complications.

Objective: This study evaluated the inhibitory potential of some spicy plants on the activities of polyol pathway enzymes (aldose reductase and sorbitol dehydrogenase).

Method: Aqueous extracts of Laurus nobilis (bay), Cinnamomum zeylanicum (cinnamon), Murraya koenigii (curry), Thymus vulgaris (thyme) and Curcuma longa (turmeric) were incubated with appropriate enzymes and substrates, and percentages inhibition determined.

Results: Results showed that bay extract had effective IC50 for inhibition of both aldose reductase (174.87 µg/mL) and sorbitol dehydrogenase (37.08 µg/mL). It also revealed that bay extract inhibited aldose reductase and sorbitol dehydrogenase in a non-competitive and competitive manner respectively.

Conclusion: It is therefore concluded that bay extract effectively inhibited activities of polyol pathway enzymes, and may contribute to the amelioration of diabetic complications.

Keywords: Aldose reductase, sorbitol dehydrogenase, diabetes mellitus, spices, bay, phytochemicals

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DOI: 10.2174/1573408017666210223124126
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Current Organic Chemistry

Editor-in-Chief:

György Keglevich
Budapest University of Technology and Economics
Budapest
Hungary

 

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Are our diabetic patients’ adherent to the treatment?

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Author(s): Avinash Kumar*, Dhruv Indiresh Hejmady, Unnikrishnan B, Rekha Thapar, Nithin Kumar, Ramesh Holla, Darshan BB, Vishnu J Shetty, I S Divya Charitha, Rakshith Hegde K

Journal Name: Current Diabetes Reviews

Abstract:

Aim: To estimate the adherence to treatment among type 2 diabetic patients.

Background: Treatment adherence is a complex process which is controlled by multiple factors. Lack of treatment adherence is common with patients who suffer from type 2 diabetes and is becoming a very prevalent problem especially with the patients who suffer from non-communicable diseases (NCD) worldwide.

Objective: To estimate the adherence to treatment among type 2 diabetic patients, and the perception and practice of self-management among them

Methodology: A cross sectional study using a questionnaire was conducted amongst the patients in Kasturba Medical College, Mangalore, a coastal city of southern India. The questionnaire consisted of Medical Adherence Rating Scale (MARS) to assess how adherent the patient is to the treatment and the Diabetes Self-care Questionnaire (DSMQ) for assessing the various self-care practices employed by diabetic patients. The data obtained was entered and the analysis was done by using the Statistical Package for the Social Science (SPSS) version 25.0.

Results: The study involved 95 patients and the mean age was found to be 50.71 ± 12.633 years. More than 60% of the study population were male and 78.9% were literate. Nearly half of the patients (49.5%) had been on treatment for a duration of >5 years. Eighty-two percent population (82.1%) were adherent to their medications. Adherence was found to be nearly eighty percent (79.5%) among the literates. Conclusion: Adherence was more among the males as compared to the females. Most patients in the study had been adherent towards their medications prescribed to them. Most of them were on oral drugs only. The majority of the patients who had diabetes mellitus were found to have inadequate self-care management for diabetes mellitus.

Keywords: Adherence, self-care management, Medical Adherence rating scale, treatment, diabetes, non-communicable diseases.

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DOI: 10.2174/1573399817666210223114010
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Absorption, Metabolism, Distribution, and Excretion of Letermovir

(E-pub Abstract Ahead of Print)

Author(s): Karsten Menzel*, Prajakti Kothare, Jacqueline B. McCrea, Xiaoyan Chu, Dirk Kropeit

Journal Name: Current Drug Metabolism

Abstract:

Background: Letermovir is approved for prophylaxis of cytomegalovirus infection and disease in cytomegalovirus-seropositive hematopoietic stem-cell transplant (HSCT) recipients.

Objective: HSCT recipients are required to take many drugs concomitantly. The pharmacokinetics, absorption, distribution, metabolism, and excretion of letermovir and its potential to inhibit metabolizing enzymes and transporters In vitro were investigated to inform on the potential for drug‒drug interactions (DDIs).

Methods: A combination of in vitro and in vivo studies described the absorption, distribution, metabolism, and routes of elimination of letermovir, as well as the enzymes and transporters involved in these processes. The effect of letermovir to inhibit and induce metabolizing enzymes and transporters were evaluated In vitro and its victim and perpetrator DDI potentials were predicted by applying the regulatory guidance for DDI assessment.

Results: Letermovir was a substrate of CYP3A4/5 and UGT1A1/3 in vitro. Letermovir showed concentration-dependent uptake into organic anionic transporting polypeptide (OATP)1B1/3-transfected cells and was a substrate of P-glycoprotein (P-gp). In a human ADME study, letermovir was primarily recovered as unchanged drug and minor amounts of a direct glucuronide in feces. Based on the metabolic pathway profiling of letermovir, there were few oxidative metabolites in human matrix. Letermovir inhibited CYP2B6, CYP2C8, CYP3A, and UGT1A1 in vitro, and induced CYP3A4 and CYP2B6 in hepatocytes. Letermovir also inhibited OATP1B1/3, OATP2B1, OAT3, OCT2, BCRP, BSEP, and P-gp.

Conclusion: The body of work presented in this manuscript informed on the potential for DDIs when letermovir is administered both intravenously and orally in HSCT recipients.

Keywords: drug metabolizing enzymes, drug‒drug interactions, human ADME study, in vitro; In vivo, letermovir, OATP1B, transporters

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1389200222666210223112826
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