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Evaluation of current trends and recent development in insulin therapy for management of diabetes mellitus

Nawaz MS, Shah KU, Khan TM, Rehman AU, Rashid HU, Mahmood S, et al.

Diabetes Metab Syndr, 2017 Dec;11 Suppl 2:S833-S839.
PMID: 28709853 DOI: 10.1016/j.dsx.2017.07.003

OBJECTIVE: Diabetes mellitus is a major health problem in developing countries. There are various insulin therapies to manage diabetes mellitus. This systematic review evaluates various insulin therapies for management of diabetes mellitus worldwide. This review also focuses on recent developments being explored for better management of diabetes mellitus.
RESEARCH DESIGN AND METHOD: We reviewed a number of published articles from 2002 to 2016 to find out the appropriate management of diabetes mellitus. The paramount parameters of the selected studies include the insulin type & its dose, type of diabetes, duration and comparison of different insulin protocols. In addition, various newly developed approaches for insulin delivery with potential output have also been evaluated.
RESULTS: A great variability was observed in managing diabetes mellitus through insulin therapy and the important controlling factors found for this therapy include; dose titration, duration of insulin use, type of insulin used and combination therapy of different insulin.
CONCLUSION: A range of research articles on current trends and recent advances in insulin has been summarized, which led us to the conclusion that multiple daily insulin injections or continuous subcutaneous insulin infusion (insulin pump) is the best method to manage diabetes mellitus. In future perspectives, development of the oral and inhalant insulin would be a tremendous breakthrough in Insulin therapy.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Polyphenols: Potential Future Arsenals in the Treatment of Diabetes

Solayman M, Ali Y, Alam F, Islam MA, Alam N, Khalil MI, et al.

Curr Pharm Des, 2016;22(5):549-65.
PMID: 26601968

Diabetes mellitus (DM) is one of the most common endocrine metabolic disorders. In addition to exercise and diet, oral anti-diabetic drugs have been used as a part of the management strategy worldwide. Unfortunately, none of the conventional anti-diabetic drugs are without side effects, and these drugs pose an economic burden. Therefore, the investigation of novel anti-diabetic regimens is a major challenge for researchers, in which nature has been the primary resource for the discovery of potential therapeutics. Many plants have been shown to act as anti-diabetic agents, in which the main active constituents are believed to be polyphenols. Natural products containing high polyphenol levels can control carbohydrate metabolism by various mechanisms, such as protecting and restoring beta-cell integrity, enhancing insulin releasing activity, and increasing cellular glucose uptake. Blackberries, red grapes, apricots, eggplant and popular drinks such as coffee, cocoa and green tea are all rich in polyphenols, which may dampen insulin resistance and be natural alternatives in the treatment of diabetes. Therefore, the aim of this review is to report on the available anti-diabetic polyphenols (medicinal plants, fruits and vegetables), their mechanisms in the various pathways of DM and their correlations with DM. Additionally, this review emphasizes the types of polyphenols that could be potential future resources in the treatment of DM via either novel regimens or as supplementary agents.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Fulltext Computer aided screening of secreted frizzled-related protein 4 (SFRP4): a potential control for diabetes mellitus

Bukhari SA, Shamshari WA, Ur-Rahman M, Zia-Ul-Haq M, Jaafar HZ

Molecules, 2014 Jul 11;19(7):10129-36.
PMID: 25019556 DOI: 10.3390/molecules190710129

Diabetes mellitus is a life threatening disease and scientists are doing their best to find a cost effective and permanent treatment of this malady. The recent trend is to control the disease by target base inhibiting of enzymes or proteins. Secreted frizzled-related protein 4 (SFRP4) is found to cause five times more risk of diabetes when expressed above average levels. This study was therefore designed to analyze the SFRP4 and to find its potential inhibitors. SFRP4 was analyzed by bio-informatics tools of sequence tool and structure tool. A total of three potential inhibitors of SFRP4 were found, namely cyclothiazide, clopamide and perindopril. These inhibitors showed significant interactions with SFRP4 as compared to other inhibitors as well as control (acetohexamide). The findings suggest the possible treatment of diabetes mellitus type 2 by inhibiting the SFRP4 using the inhibitors cyclothiazide, clopamide and perindopril.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Potential effect of herbs on diabetic hypertension: alternative medicine treatment modalities

Zar CT, Das S

Clin Ter, 2013;164(6):529-35.
PMID: 24424219 DOI: 10.7417/CT.2013.1633

BACKGROUND AND OBJECTIVE: Diabetes mellitus is commonly known to lead to life threatening complications. Among them, hypertension is one complication which may be highlighted. In modern medical society, several drugs and treatment regimen have developed to treat diabetes mellitus. Although they obtain positive impacts, yet there are certain limitations encountered in the management of the disease due to their adverse effects and non-compliance by the patients. Herbs have been valued as a supplement in treating chronic oxidative stress disorder like diabetes mellitus. In the present review, some of the herbs which possess both anti-hyperglycemic and anti-hypertensive properties are being highlighted. Potential herbs which include Andrographis Paniculata, Ammi Visnaga, Allium sativum, Phyllanthus amarus, Ginkgo biloba, Solanum tuberosum, Tuberosum L. Piper sarmentosum and Lamiaceae family are known to possess antihypertensive properties. Various researches have been conducted on these herbs and positive results have been obtained. Based on these results, the present review article discusses the alternative management of diabetic hypertension with the herbal medicine. In conclusion, the present review article stresses on the need to ensure global awareness about the traditional medicines while treating diabetic hypertension.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Design of oral insulin delivery systems

Wong TW

J Drug Target, 2010 Feb;18(2):79-92.
PMID: 19968567 DOI: 10.3109/10611860903302815

The possibility of administering insulin orally in replacement of painful subcutaneous route has been investigated over years but with varying degree of success. Nanoparticles, microparticles, hydrogel, capsule, tablet, and film patch are designed to deliver insulin orally. They are largely formulated with polymeric adhesive, protease inhibitor, insulin aggregation inhibitor, and functional excipients to induce transcellular, paracellular, Peyer's patches, or receptor-mediated transport of insulin in gastrointestinal tract. Superporous matrix, intestinal patches, and charged-coupled micromagnet microparticles are recent formulation strategies to promote oral insulin absorption. The formulation emphasizes on assembly of insulin and excipients into a physical structure which provides an element of drug targeting to maintain stability and increase bioavailability of insulin. The overview of various strategies applied in oral insulin delivery system design denotes the significance of mucoadhesiveness whereby a prolonged retention of dosage form in intestinal tract translates to cumulative insulin release and absorption, overcoming the intestinal transport capacity limit. Synthesis and use of mucoadhesive excipients, chemical modification of insulin to promote its physicochemical and biological stability for encapsulation in dosage form with prolonged retention characteristics and identification of potential insulin adjuncts are efforts needed to accelerate the speed of obtaining a functional oral insulin delivery system.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Fulltext A study of the fasting diabetic patients during the month of Ramadan

Mafauzy M, Mohammed WB, Anum MY, Zulkifli A, Ruhani AH

Med J Malaysia, 1990 Mar;45(1):14-7.
PMID: 2152063

Twenty two Muslim diabetic patients on oral hypoglycaemic agents were studied during the fasting month of Ramadan to determine the effect of fasting on their diabetic control. All the patients completed their fast during the month. Their mean (+/- standard deviation) blood glucose, serum fructosamine and body weight before the fasting month were 10.7 +/- 4.6 mmol/l, 6.64 +/- 3.64 mmol/l and 60.5 +/- 12.6 kg and by the end of the fasting month were 10.9 +/- 4.4 mmol/1,4.34 +/- 1.08 mmol/l and 59.8 +/- 12.3 kg respectively. There was no significant difference between the blood glucose levels but there were significant reductions in the mean body weight and fructosamine values (p = 0.01 and p = 0.03 respectively). The mean decrease in body weight and fructosamine were 0.7 +/- 1.3 kg and 2.29 +/- 3.09 mmol/l respectively. There were also statistically significant differences between the mean daily calorie content before the fasting and during the fasting month (1480 +/- 326 vs 1193 +/- 378 Cal/day - p less than 0.005) and between the mean daily carbohydrate content (389 +/- 298 vs 187 +/- 46 gm/day - p less than 0.005). In conclusion, fasting was safe for diabetic patients on oral hypoglycaemic agents and it was associated with weight reduction and improvement in the overall diabetic control. This was most likely due to decrease in food intake.

Matched MeSH terms: Diabetes Mellitus/drug therapy
Synthesis of quinoline derivatives as diabetic II inhibitors and molecular docking studies

Taha M, Sultan S, Imran S, Rahim F, Zaman K, Wadood A, et al.

Bioorg Med Chem, 2019 09 15;27(18):4081-4088.
PMID: 31378594 DOI: 10.1016/j.bmc.2019.07.035

In searchof the potenttherapeutic agent as an α-glucosidase inhibitor, we have synthesized twenty-five analogs (1-25) of quinoline-based Schiff bases as an inhibitoragainst α-glucosidase enzyme under positive control acarbose (IC50 = 38.45 ± 0.80 µM). From the activity profile it was foundthat analogs 1, 2, 3, 4, 11, 12 and 20with IC50values 12.40 ± 0.40, 9.40 ± 0.30, 14.10 ± 0.40, 6.20 ± 0.30, 14.40 ± 0.40, 7.40 ± 0.20 and 13.20 ± 0.40 µMrespectively showed most potent inhibition among the series even than standard drug acarbose (IC50 = 38.45 ± 0.80 µM). Here in the present study analog 4 (IC50 = 6.20 ± 0.30 µM) was found with many folds better α-glucosidase inhibitory activity than the reference drug. Eight analogs like 5, 7, 8, 16, 17, 22, 24 and 25 among the whole series displayed less than 50% inhibition. The substituents effects on phenyl ring thereby superficially established through SAR study. Binding interactions of analogs and the active site of ligands proteins were confirmed through molecular docking study. Spectroscopic techniques like 1H NMR, 13C NMR and ESIMS were used for characterization.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Fulltext A patient-centric approach to optimise insulin therapy in Asia

Goh SY, Ang E, Bajpai S, Deerochanawong C, Hong EG, Hussein Z, et al.

J Diabetes Complications, 2016 08;30(6):973-80.
PMID: 27288201 DOI: 10.1016/j.jdiacomp.2016.05.019
Matched MeSH terms: Diabetes Mellitus/drug therapy*
Fulltext Bioactive Components of Salvia and Their Potential Antidiabetic Properties: A Review

Abd Rashed A, Rathi DG

Molecules, 2021 May 20;26(10).
PMID: 34065175 DOI: 10.3390/molecules26103042

The utilization of therapeutic plants is expanding around the globe, coupled with the tremendous expansion of alternative medicine and growing demand in health treatment. Plants are applied in pharmaceuticals to preserve and expand health-physically, mentally and as well as to treat particular health conditions and afflictions. There are more than 600 families of plants identified so far. Among the plants that are often studied for their health benefit include the genus of Salvia in the mint family, Lamiaceae. This review aims to determine the bioactive components of Salvia and their potential as antidiabetic agents. The search was conducted using three databases (PubMed, EMBASE and Scopus), and all relevant articles that are freely available in the English language were extracted within 10 years (2011-2021). Salvia spp. comprises many biologically active components that can be divided into monoterpenes, diterpenes, triterpenes, and phenolic components, but only a few of these have been studied in-depth for their health benefit claims. The most commonly studied bioactive component was salvianolic acids. Interestingly, S. miltiorrhiza is undoubtedly the most widely studied Salvia species in terms of its effectiveness as an antidiabetic agent. In conclusion, we hope that this review stimulates more studies on bioactive components from medicinal plants, not only on their potential as antidiabetic agents but also for other possible health benefits.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Antidiabetic Potential of Syzygium sp.: An Overview

Zulcafli AS, Lim C, Ling AP, Chye S, Koh R

Yale J Biol Med, 2020 Jun;93(2):307-325.
PMID: 32607091

Diabetes, characterized by hyperglycemia, is one of the most significant metabolic diseases, reaching alarming pandemic proportions. It can be due to the defects in insulin action, or secretion, or both. The global prevalence of diabetes is estimated at 425 million people in 2017, and expected to rise to 629 million by 2045 due to an increasing trend of unhealthy lifestyles, physical inactivity, and obesity. Several treatment options are available to diabetics, however, some of the antidiabetic drugs result in adverse side effects such as hypoglycemia. Hence, there has been a proliferation of studies on natural products with antidiabetic effects, including plants from the Myrtaceae family, such as Psidium guajava, Eucalyptus globulus,Campomanesia xanthocarpa, and more significantly, Syzygium sp. Previous studies have shown that a number of Syzygium species had potent antidiabetic effects and were safe for consumption. This review aims to discuss the antidiabetic potential of Syzygium sp., based on in vitro and in vivo evidence.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Prescribing of antidiabetic therapies in Ireland: 10-year trends 2003-2012

Zaharan NL, Williams D, Bennett K

Ir J Med Sci, 2014 Jun;183(2):311-8.
PMID: 24013870 DOI: 10.1007/s11845-013-1011-1

BACKGROUND: Over the last decade there have been significant changes in the prescribing of antidiabetic therapies. It is of interest to know about these trends and variations in the Irish population so that future prescribing patterns can be estimated.
AIMS: To examine the trends in prescribed antidiabetic treatments, including variations across age, gender, socioeconomic status and regions in the Irish population over the last 10 years.
METHODS: The Irish national pharmacy claims database was used to identify patients ≥ 16 years dispensed antidiabetic agents (oral or insulin) from January 2003 to December 2012 through the two main community drug schemes for diabetes. The rate of prescribing per 1,000 population was calculated. Logistic regression was used to examine variations in prescribing in patients with diabetes.
RESULTS: There was a significant increase in the prescribing of fast and long-acting insulin analogues with a rapid decline in the prescribing of human insulin (p < 0.0001). Increased prescribing of metformin, incretin modulators and fixed oral combination agents was observed (p < 0.0001). Females and older aged patients were more likely to be prescribed human insulin than other insulins. Metformin was less likely while sulphonylureas were more likely to be prescribed in older than younger aged patients. Socioeconomic differences were observed in increased prescribing of the newer and more expensive antidiabetic agents in the non-means tested scheme. Regional variations were observed in the prescribing of both insulin and oral antidiabetic agents.
CONCLUSION: There has been an increase over time in the prescribing of both insulin and oral antidiabetic agents in the Irish population with increasing uptake of newer antidiabetic agents. This has implications for projecting future uptake and expenditure of these agents given the rising level of diabetes in the population.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Fulltext Prevalence of diabetes in the Malaysian National Health Morbidity Survey III 2006

Letchuman GR, Wan Nazaimoon WM, Wan Mohamad WB, Chandran LR, Tee GH, Jamaiyah H, et al.

Med J Malaysia, 2010 Sep;65(3):180-6.
PMID: 21939164 MyJurnal

The Malaysian National Health Morbidity Survey III (NHMS III), conducted in 2006, was a cross-sectional household survey of the prevalence of chronic diseases, involving 34,539 respondents of age > or =18 years old, in all states of Malaysia. Data collection was by face-to-face interview. Those who self-professed not to be diabetics underwent finger-prick glucose test following at least 8 hours of fasting. The overall prevalence of diabetes mellitus (known and newly diagnosed) was 11.6%. The Indians had the highest prevalence of 19.9% followed by Malays 11.9% and Chinese 11.4%. The prevalence of people with known diabetes and newly diagnosed diabetes was 7.0% and 4.5% respectively. Impaired Fasting Glycaemia was found to be 4.2%. Majority (73.5%) of the patients used government healthcare facilities for their diabetic care. Usage of insulin alone or in combination was low at 7.2% of patients. Only 45.05% of known diabetics have ever had their eye examined. Amputees formed 4.3% of the patients with known diabetes while 3.4% had suffered a stroke event and 1.6% was on some form of renal replacement therapy.
Study name: National Health and Morbidity Survey (NHMS-2006)

Matched MeSH terms: Diabetes Mellitus/drug therapy
Fulltext An Audit of Diabetes Control and Management (ADCM)

Mastura I, Zanariah H, Fatanah I, Feisul Idzwan M, Wan Shaariah MY, Jamaiyah H, et al.

Med J Malaysia, 2008 Sep;63 Suppl C:76-7.
PMID: 19227679

Diabetes is a chronic condition that is one of the major causes of illness, disability, and death in Malaysia. Cost in managing diabetes plus indirect cost of lost work, pain, and suffering have all increased. The optimal management of patients with diabetes require the tracking of patients over time to monitor the progression of the disease, compliance with treatment, and preventive care. Diabetes care can be improved by standardizing access to, and improving the use of, clinical information. Access to timely, accurate and well-organized electronic data will improve the quality of care for patients with diabetes. Clinical Research Center convened an expert workshop to forecast how physicians, hospitals and clinics will employ clinical information technology (IT) applications to diabetes care over the next year. Workshop participants included experts from research organizations, government, and the IT vendor. This is a summary of the workshop organised for the purpose of the Audit of Diabetes Control and Management (ADCM) project. We hope to identify the gaps, if any, that exists in delivering diabetes care and to improve the quality of care. In future, we hope to develop an expansion of this project for the Adult Diabetes Registry that will be implemented for the whole country.

Matched MeSH terms: Diabetes Mellitus/drug therapy
Use Piper sarmentosum as an effective antidiabetic supplement in South East Asia: a review

Zar CT, Teoh SL, Das S, Zaiton Z, Farihah HS

Clin Ter, 2012 Nov;163(6):505-10.
PMID: 23306747

Herbs with antidiabetic activity have a potential role to play. Herbal medicines have been widely used in South East Asia because of lesser side effects and cost effectiveness. The main aim of this review article was to disseminate important information regarding the use of herbal products in oxidative stress involved in diseases like diabetes mellitus. The article highlights some of the traditional medicinal plants which have been widely used in South East Asia with special emphasis on Piper sarmentosum. Piper sarmentosum have been reported to possess varying degree of hypoglycemic, antidiabetic and other additional properties. The antioxidant properties of the herbs may be effective in controlling the oxidative damage produced during diabetes mellitus. The review article highlights the positive role of traditional herbs towards diabetes mellitus and also describes its complications.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Patient satisfaction and medication adherence assessment amongst patients at the diabetes medication therapy adherence clinic

Bakar ZA, Fahrni ML, Khan TM

Diabetes Metab Syndr, 2016 Apr-Jun;10(2 Suppl 1):S139-43.
PMID: 27055354 DOI: 10.1016/j.dsx.2016.03.015

AIMS: To determine the satisfaction and current adherence status of patients with diabetes mellitus at the diabetes Medication Therapy Adherence Clinic and the relationship between patient satisfaction and adherence.
METHODS: This cross-sectional descriptive study was carried out at three government hospitals in the state of Johor, Malaysia. Patient's satisfaction was measured using the Patient Satisfaction with Pharmaceutical Care Questionnaire; medication adherence was measured using the eight-item Morisky Medication Adherence Scale.
RESULTS: Of n=165 patients, 87.0% of patients were satisfied with DMTAC service (score 60-100) with mean scores of 76.8. On the basis of MMAS, 29.1% had a medium rate and 26.1% had a high rate of adherence. Females are 3.02 times more satisfied with the pharmaceutical service compared to males (OR 3.03, 95% CI 1.12-8.24, p<0.05) and non-Malays are less satisfied with pharmaceutical care provided during DMTAC compared to Malays (OR 0.32, 95% CI 0.12-0.85, p<0.05). Older patients age group ≥60 years were 3.29 times more likely to adhere to their medications (OR 3.29, 95% CI 1.10-9.86, p<0.05). Females were the most adherent compared to males (OR 2.33, 95%CI 1.10-4.93, p<0.05) and patients with secondary level of education were 2.72 times more adherent to their medications compared to those in primary school and no formal education (OR 2.72, 95%CI 1.13-6.55, p<0.05). There is a significant (p<0.01), positive fair correlation (r=0.377) between satisfaction and adherence.
CONCLUSION: Patients were highly satisfied with DMTAC service, while their adherence levels were low. There is an association between patient satisfaction and adherence.
Keyword: Diabetes medication therapy adherence clinic (DMTAC)
Study site: Medication Therapy Adherence Clinic, Pharmacy, Hospitals, Johor, Malaysia

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Quality of life: an assessment of the state of psychosocial rehabilitation of patients with schizophrenia in the community

Hasanah CI, Razali MS

J R Soc Promot Health, 2002 Dec;122(4):251-5.
PMID: 12557735

The subjective quality of life (QOL) of diabetic patients on oral hypoglycaemics was compared to schizophrenic patients who were well controlled with their antipsychotic medications. This comparison was made using the generic quality of life questionnaire produced by the World Health Organization QOL (WHOQOL) group, namely the WHOQOL-100. Statistical analysis showed that there was no significant difference in the psychological well-being and level of independence between the two groups. However, such measures revealed that the most impaired aspect of well-being in the schizophrenic group was the social relationship. Subjective QOL assessment is able to reveal deficits or handicaps that are obscure and probably difficult to appreciate on objective social and clinical evaluation. Such findings are valuable in planning the rehabilitative need of schizophrenic patients in the community.

Matched MeSH terms: Diabetes Mellitus/drug therapy
Fulltext Development of a PATIENT-Medication Adherence Instrument (P-MAI) and a HEALTHCARE PROFESSIONAL-Medication Adherence Instrument (H-MAI) using the nominal group technique

Goh SSL, Lai PSM, Liew SM, Tan KM, Chung WW, Chua SS

PLoS One, 2020;15(11):e0242051.
PMID: 33175871 DOI: 10.1371/journal.pone.0242051

To date, several medication adherence instruments have been developed and validated worldwide. However, most instruments have only assessed medication adherence from the patient's perspective. The aim was to develop and validate the PATIENT-Medication Adherence Instrument (P-MAI) and the HEALTHCARE PROFESSIONAL-Medication Adherence Instrument (H-MAI) to assess medication adherence from the patient's and healthcare professional (HCP)'s perspectives. The P-MAI-12 and H-MAI-12 were developed using the nominal group technique. The face and content validity was determined by an expert panel and piloted. The initial version of these instruments consisted of 12 items were validated from October-December 2018 at a primary care clinic in Malaysia. Included were patients aged ≥21 years, diagnosed with diabetes mellitus, taking at least one oral hypoglycaemic agent and who could understand English. The HCPs recruited were family medicine specialists or trainees. To assess validity, exploratory factor analysis (EFA) and concurrent validity were performed; internal consistency and test-retest were performed to assess its reliability. A total of 120/158 patients (response rate = 75.9%) and 30/33 HCPs (response rate = 90.9%) agreed to participate. EFA found three problematic items in both instruments, which was then removed. The final version of the P-MAI-9 and the HMAI-9 had 9 items each with two domains (adherence = 2 items and knowledge/belief = 7 items). For concurrent validity, the total score of the P-MAI-9 and the H-MAI-9 were not significantly different (p = 0.091), indicating that medication adherence assessed from both the patient's and HCP's perspectives were similar. Both instruments achieved acceptable internal consistency (Cronbach's α: P-MAI-9 = 0.722; H-MAI-9 = 0.895). For the P-MAI-9, 7/9 items showed no significant difference between test and retest whereas 8/9 items in the H-MAI-9 showed significant difference at test and retest (p>0.05). In conclusion, the P-MAI-9 and H-MAI-9 had low sensitivity and high specificity suggesting that both instruments can be used for identifying patients more likely to be non-adherent to their medications.

Matched MeSH terms: Diabetes Mellitus/drug therapy*
Synthesis of benzotriazoles derivatives and their dual potential as α-amylase and α-glucosidase inhibitors in vitro: Structure-activity relationship, molecular docking, and kinetic studies

Hameed S, Kanwal, Seraj F, Rafique R, Chigurupati S, Wadood A, et al.

Eur J Med Chem, 2019 Dec 01;183:111677.
PMID: 31514061 DOI: 10.1016/j.ejmech.2019.111677

Benzotriazoles (4-6) were synthesized which were further reacted with different substituted benzoic acids and phenacyl bromides to synthesize benzotriazole derivatives (7-40). The synthetic compounds (7-40) were characterized via different spectroscopic techniques including EI-MS, HREI-MS, 1H-, and 13C NMR. These molecules were examined for their anti-hyperglycemic potential hence were evaluated for α-glucosidase and α-amylase inhibitory activities. All benzotriazoles displayed moderate to good inhibitory activity in the range of IC50 values of 2.00-5.6 and 2.04-5.72 μM against α-glucosidase and α-amylase enzymes, respectively. The synthetic compounds were divided into two categories "A" and "B", in order to understand the structure-activity relationship. Compounds 25 (IC50 = 2.41 ± 1.31 μM), (IC50 = 2.5 ± 1.21 μM), 36 (IC50 = 2.12 ± 1.35 μM), (IC50 = 2.21 ± 1.08 μM), and 37 (IC50 = 2.00 ± 1.22 μM), (IC50 = 2.04 ± 1.4 μM) with chloro substitution/s at aryl ring were found to be most active against α-glucosidase and α-amylase enzymes. Molecular docking studies on all compounds were performed which revealed that chloro substitutions are playing a pivotal role in the binding interactions. The enzyme inhibition mode was also studied and the kinetic studies revealed that the synthetic molecules have shown competitive mode of inhibition against α-amylase and non-competitive mode of inhibition against α-glucosidase enzyme.

Matched MeSH terms: Diabetes Mellitus/drug therapy
Review on rosmarinic acid extraction, fractionation and its anti-diabetic potential

Ngo YL, Lau CH, Chua LS

Food Chem Toxicol, 2018 Nov;121:687-700.
PMID: 30273632 DOI: 10.1016/j.fct.2018.09.064

Rosmarinic acid is a bioactive phytochemical that can be found in many herbs as ethnomedicines. It possesses remarkable pharmacological activities, and thus leading to its exploration as a therapeutic drug in diabetes treatment recently. This article reviews the extraction and fractionation techniques for plant-based natural rosmarinic acid and its anti-diabetic potential based on literature data published in journals, books, and patents from 1958 to 2017. Factors affecting the performance of rosmarinic acid extraction and fractionation such as operating temperature, time, solvent to sample ratio and eluent system are compiled and discussed in detail. The inhibitory action of rosmarinic acid against sugar digestive enzymes, and protective action towards pancreatic β-cell dysfunction and glucolipotoxicity mediated oxidative stress are also critically reviewed. The optimal parameters are largely dependent on the applied extraction and fractionation techniques, as well as the nature of plant samples. Previous studies have proven the potent role of rosmarinic acid to control plasma glucose level and increase insulin sensitivity in hyperglycemia. Although rosmarinic acid is readily absorbed by human body, its mechanism after consumption is remained unclear. Intensive studies should be well planned to determine the dosage and toxicity level of rosmarinic acid for efficacy and safe consumption.

Matched MeSH terms: Diabetes Mellitus/drug therapy
A contemporary biological pathway of islet amyloid polypeptide for the management of diabetic dementia

Sah SK, Samuel VP, Dahiya S, Singh Y, Gilhotra RM, Gupta G, et al.

Chem Biol Interact, 2019 Jun 01;306:117-122.
PMID: 31004596 DOI: 10.1016/j.cbi.2019.04.022

Major challenges of dealing elder patients with diabetes mellitus (DM) are the individualization of consideration in persons with various comorbid types of conditions. In spite of the fact that microvascular and macrovascular problems associated with DM are well documented, there is only a few numbers of reports viewing different conditions, for example, cognitive dysfunction. Cognitive dysfunction is of specific significance due to its effect on self-care and quality of life. All in all, the etiology of cognitive dysfunction in the maturing populace is probably going to be the grouping of ischemic and degenerative pathology. It is likewise trusted that Hyperglycemia is engaged with the system of DM-related cognitive dysfunction. At present, it isn't certain in the case of enhancing glycemic control or utilizing therapeutic agents can enhance the risk of cognitive decay. Amylin was later characterized as an amyloidogenic peptide, confined from a beta cell tumor and called islet amyloid polypeptide (IAPP), and after that, amylin. Conversely, we investigate the beneficial role and hypothesizing the mechanism of amylin related expanding the level and activation of CGRP receptor to enhance the cognition declination amid diabetic dementia.

Matched MeSH terms: Diabetes Mellitus/drug therapy*

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