MyMedR

Fulltext Antioxidant and Antidiabetic Effects of Flavonoids: A Structure-Activity Relationship Based Study

Sarian MN, Ahmed QU, Mat So'ad SZ, Alhassan AM, Murugesu S, Perumal V, et al.

Biomed Res Int, 2017;2017:8386065.

PMID: 29318154 DOI: 10.1155/2017/8386065

The best described pharmacological property of flavonoids is their capacity to act as potent antioxidant that has been reported to play an important role in the alleviation of diabetes mellitus. Flavonoids biochemical properties are structure dependent; however, they are yet to be thoroughly understood. Hence, the main aim of this work was to investigate the antioxidant and antidiabetic properties of some structurally related flavonoids to identify key positions responsible, their correlation, and the effect of methylation and acetylation on the same properties. Antioxidant potential was evaluated through dot blot, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, ABTS+ radical scavenging, ferric reducing antioxidant power (FRAP), and xanthine oxidase inhibitory (XOI) assays. Antidiabetic effect was investigated through α-glucosidase and dipeptidyl peptidase-4 (DPP-4) assays. Results showed that the total number and the configuration of hydroxyl groups played an important role in regulating antioxidant and antidiabetic properties in scavenging DPPH radical, ABTS+ radical, and FRAP assays and improved both α-glucosidase and DPP-4 activities. Presence of C-2-C-3 double bond and C-4 ketonic group are two essential structural features in the bioactivity of flavonoids especially for antidiabetic property. Methylation and acetylation of hydroxyl groups were found to diminish the in vitro antioxidant and antidiabetic properties of the flavonoids.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

Fulltext Expediting Multiple Biological Properties of Limonene and α-Pinene: Main Bioactive Compounds of Pistacia lentiscus L., Essential Oils

El Omari N, Mrabti HN, Benali T, Ullah R, Alotaibi A, Abdullah ADI, et al.

Front Biosci (Landmark Ed), 2023 Sep 27;28(9):229.

PMID: 37796709 DOI: 10.31083/j.fbl2809229

BACKGROUND: Screening new natural molecules with pharmacological and/or cosmetic properties remains a highly sought-after area of research. Moreover, essential oils and volatile compounds have recently garnered significant interest as natural substance candidates. In this study, the volatile components of Pistacia lentiscus L. essential oils (PLEOs) isolated from the fruit and its main compounds, alpha-pinene, and limonene, are investigated for antioxidant, antidiabetic, and dermatoprotective activities.

METHODS: In vitro antioxidant activity was investigated using 2,2'-diphenyl-1-picrylhydrazyl (DPPH), fluorescence recovery after photobleaching (FRAP), and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) methods. The antidiabetic and dermatoprotective effects were studied using enzyme inhibitory activities.

RESULTS: Antioxidant tests showed that PLEO has the best activity (ranging from 29.64 ± 3.04 to 73.80 ± 3.96 µg/mL) compared to its main selected molecules (ranging from 74 ± 3.72 to 107.23 ± 5.03 µg/mL). The α-glucosidase and α-amylase assays demonstrated that the elements tested have a promising antidiabetic potential with IC50values ranging from 78.03 ± 2.31 to 116.03 ± 7.42 µg/mL and 74.39 ± 3.08 to 112.35 ± 4.92 µg/mL for the α-glucosidase and α-amylase assays, respectively, compared to the standard drug. For the tyrosinase test, we found that the EOs (IC50 = 57.72 ± 2.86 µg/mL) followed by limonene (IC50 = 74.24 ± 2.06 µg/mL) and α-pinene (IC50 = 97.45 ± 5.22 µg/mL) all exhibited greater inhibitory effects than quercetin (IC50 = 246.90 ± 2.54 µg/mL).

CONCLUSIONS: Our results suggest that the biological activities of PLEO, as well as its main compounds, make them promising candidates for the development of new strategies aimed at improving dermatoprotection and treating diseases associated with diabetes mellitus and oxidative stress.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Fulltext Phytofabrication of Selenium Nanoparticles with Moringa oleifera (MO-SeNPs) and Exploring Its Antioxidant and Antidiabetic Potential

Ahamad Tarmizi AA, Nik Ramli NN, Adam SH, Abdul Mutalib M, Mokhtar MH, Tang SGH

Molecules, 2023 Jul 10;28(14).

PMID: 37513196 DOI: 10.3390/molecules28145322

The advancement in nanotechnology is the trigger for exploring the synthesis of selenium nanoparticles and their use in biomedicine. Therefore, this study aims to synthesize selenium nanoparticles using M. oleifera as a reducing agent and evaluate their antioxidant and antidiabetic potential. Our result demonstrated a change in the color of the mixture from yellow to red, and UV-Vis spectrometry of the suspension solution confirmed the formation of MO-SeNPs with a single absorbance peak in the range of 240-560 nm wavelength. FTIR analysis revealed several bioactive compounds, such as phenols and amines, that could possibly be responsible for the reduction and stabilization of the MO-SeNPs. FESEM + EDX analysis revealed that the amorphous MO-SeNPs are of high purity, have a spherical shape, and have a size of 20-250 nm in diameter, as determined by HRTEM. MO-SeNPs also exhibit the highest DPPH scavenging activity of 84% at 1000 μg/mL with an IC50 of 454.1 μg/mL and noteworthy reducing ability by reducing power assay. Furthermore, MO-SeNPs showed promising antidiabetic properties with dose-dependent inhibition of α-amylase (26.7% to 44.53%) and α-glucosidase enzyme (4.73% to 19.26%). Hence, these results demonstrated that M. oleifera plant extract possesses the potential to reduce selenium ions to SeNPs under optimized conditions with notable antioxidant and antidiabetic activities.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Recent advances and structure-activity relationship studies of DPP-4 inhibitors as anti-diabetic agents

Singhal S, Manikrao Patil V, Verma S, Masand N

Bioorg Chem, 2024 May;146:107277.

PMID: 38493634 DOI: 10.1016/j.bioorg.2024.107277

Diabetes mellitus (DM) is one of the largest public health problems worldwide and in the last decades various therapeutic targets have been investigated. For the treatment of type-2 DM (T2DM), dipeptidyl peptidase-4 (DPP-4) is one of the well reported target and has established safety in terms of cardiovascular complexicity. Preclinical and clinical studies using DPP-4 inhibitors have demonstrated its safety and effectiveness and have lesser risk of associated hypoglycaemic effect making it suitable for elderly patients. FDA has approved a number of structurally diverse DPP-4 inhibitors for clinical use. The present manuscript aims to focus on the well reported hybrid and non-hybrid analogues and their structural activity relationship (SAR) studies. It aims to provide structural insights for this class of compounds pertaining to favourable applicability of selective DPP-4 inhibitors in the treatment of T2DM.

Matched MeSH terms: Hypoglycemic Agents/chemistry

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: Hypoglycemic Agents/chemistry*

Fulltext Virtual Screening, Synthesis, and Biological Evaluation of Some Carbohydrazide Derivatives as Potential DPP-IV Inhibitors

Jadhav PB, Jadhav SB, Zehravi M, Mubarak MS, Islam F, Jeandet P, et al.

Molecules, 2022 Dec 24;28(1).

PMID: 36615348 DOI: 10.3390/molecules28010149

Dipeptidyl peptidase-4 (DPP-IV) inhibitors are known as safe and well-tolerated antidiabetic medicine. Therefore, the aim of the present work was to synthesize some carbohydrazide derivatives (1a-5d) as DPP-IV inhibitors. In addition, this work involves simulations using molecular docking, ADMET analysis, and Lipinski and Veber's guidelines. Wet-lab synthesis was used to make derivatives that met all requirements, and then FTIR, NMR, and mass spectrometry were used to confirm the structures and perform biological assays. In this context, in vitro enzymatic and in vivo antidiabetic activity evaluations were carried out. None of the molecules had broken the majority of the drug-likeness rules. Furthermore, these molecules were put through additional screening using molecular docking. In molecular docking experiments (PDB ID: 2P8S), many molecules displayed more potent interactions than native ligands, exhibiting more hydrogen bonds, especially those with chloro- or fluoro substitutions. Our findings indicated that compounds 5b and 4c have IC50 values of 28.13 and 34.94 µM, respectively, under in vitro enzymatic assays. On the 21st day of administration to animals, compound 5b exhibited a significant reduction in serum blood glucose level (157.33 ± 5.75 mg/dL) compared with the diabetic control (Sitagliptin), which showed 280.00 ± 13.29 mg/dL. The antihyperglycemic activity showed that the synthesized compounds have good hypoglycemic potential in fasting blood glucose in the type 2 diabetes animal model (T2DM). Taken all together, our findings indicate that the synthesized compounds exhibit excellent hypoglycemic potential and could be used as leads in developing novel antidiabetic agents.

Matched MeSH terms: Hypoglycemic Agents/chemistry

A potent alpha-glucosidase inhibitor from Myristica cinnamomea King

Sivasothy Y, Loo KY, Leong KH, Litaudon M, Awang K

Phytochemistry, 2016 Feb;122:265-269.

PMID: 26712615 DOI: 10.1016/j.phytochem.2015.12.007

A dimeric acylphenol and a potent α-glucosidase inhibitor, giganteone D (IC50 5.05μM), was isolated and characterized from the bark of Myristica cinnamomea King. The bark also yielded an acylphenol with an unprecedented skeleton for which the name cinnamomeone A (IC50 358.80μM) was proposed. Their structures were established by means of NMR and MS spectrometric analyses. The Lineweaver-Burk plot of giganteone D indicated that it was a mixed-type inhibitor. This is the first report on the α-glucosidase inhibiting potential of acylphenols.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Fulltext Evaluation of antidiabetic and antioxidant properties of Brucea javanica seed

Ablat A, Mohamad J, Awang K, Shilpi JA, Arya A

ScientificWorldJournal, 2014;2014:786130.

PMID: 24688431 DOI: 10.1155/2014/786130

The ethanol extract of B. javanica seed was fractionated with solvents of different polarities and tested for antioxidant activities by several assays including DPPH radical scavenging activity, ferric reducing antioxidant power (FRAP), ferrous ion chelating activity (FCA), and nitric oxide radical scavenging activity (NORSA) along with their polyphenolic contents. Antidiabetic activity was evaluated both in vitro and in vivo using a glycogen phosphorylase α (GPα) inhibition assay and oral glucose tolerance test (OGTT) in nondiabetic rats. The ethyl acetate fraction (EAF), rich in tannin, exhibited the strongest antioxidant activities to DPPH, FRAP, and NORSA, except for FCA. The EAF also exerted a dose-depended inhibition of GPα (IC50 = 0.75 mg/ml). Further evaluation of hypoglycemic effect on OGGT indicated that rats treated with EAF (125 mg/kg bw) showed a 39.91% decrease (P < 0.05) in blood glucose levels at 30 min, and continuous fall (P < 0.05) of 28.89% and 20.29% was observed in the following hours (60 and 90 min) compared to the normal control during OGTT. The EAF was applied to polyamide column chromatography, and the resulting tannin-free fraction was tested for both GPα inhibition and antioxidant (DPPH only) activity. The GP α inhibitory activity was retained, while antioxidant activity was lost (4.6-fold) after tannin removal. These results concluded that the GPα inhibitory activity initially detected was primarily due to the compounds other than tannins, whereas antioxidant activity was mainly due to the tannins.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

Chemical compositions and antioxidative and antidiabetic properties of underutilized vegetable palm hearts from Plectocomiopsis geminiflora and Eugeissona insignis

Ahmad Aufa Z, Hassan FA, Ismail A, Mohd Yusof BN, Hamid M

J Agric Food Chem, 2014 Mar 5;62(9):2077-84.

PMID: 24499380 DOI: 10.1021/jf403481p

Underutilized vegetables are currently studied not only for their nutrient values but also for their health-promoting components for protection against chronic diseases. The present study was performed to evaluate chemical compositions and antioxidant properties of underutilized vegetable palm hearts, namely, lalis (Plectocomiopsis geminiflora) and pantu (Eugeissona insignis). Additionally, the vegetable extracts were evaluated for their activities in the inhibition of digestive enzymes and effects on insulin secretion using BRIN BD11 pancreatic cell lines. Both vegetables contain valuable sources of dietary fiber, potassium, and zinc. For the first time, the phenolic compounds of the vegetables were identified and quantified using HPLC-DAD and LC-ESI-MS. Appreciable amounts of chlorogenic acid were found in the studied vegetables. The sample extracts exhibited potential antioxidant capacities through chemical and biological in vitro assays. High inhibition of α-amylase activity (>50%) was found from the extracts. Thus, it was suggested the vegetable consumption could fulfill the nutrient requirements among local communities.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

Fulltext Antidiabetic and antioxidant properties of Ficus deltoidea fruit extracts and fractions

Misbah H, Aziz AA, Aminudin N

BMC Complement Altern Med, 2013;13:118.

PMID: 23718315 DOI: 10.1186/1472-6882-13-118

Diabetes is a serious metabolic disorder affecting the metabolism of carbohydrate, protein and fat. A number of studies have shown that diabetes mellitus is associated with oxidative stress, leading to an increased production of reactive oxygen species. Ficus deltoidea is traditionally used in Malaysia for regulating blood sugar, blood pressure and cholesterol levels. The use of F. deltoidea as an alternative medicinal herb is increasingly gaining popularity with the sale of F. deltoidea tea bags and capsules in the local market. The present study was undertaken to investigate the antidiabetic and antioxidant activities of the fruits from different varieties of F. deltoidea, employing in vitro methods.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

Fulltext Tropical plant extracts as potential antihyperglycemic agents

Manaharan T, Palanisamy UD, Ming CH

Molecules, 2012;17(5):5915-23.

PMID: 22609782 DOI: 10.3390/molecules17055915

Preliminary investigations on 14 plant extracts (obtained by ethanolic and aqueous extraction) identified those having high antioxidant and a significant total phenolic content. Antihyperglycemic, α-amylase and α-glucosidase inhibition activities were also observed. A correlation between the antihyperglycemic activity, total phenolic content and antioxidant (DPPH scavenging) activity was established. To further substantiate these findings, the possibility of tannins binding non-specifically to enzymes and thus contributing to the antihyperglycemic activity was also investigated. Our study clearly indicated that the antihyperglycemic activity observed in the plant extracts was indeed not due to non-specific tannin absorption.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Fulltext Antihyperglycemic effect of orthosiphon stamineus benth leaves extract and its bioassay-guided fractions

Mohamed EA, Mohamed AJ, Asmawi MZ, Sadikun A, Ebrika OS, Yam MF

Molecules, 2011 May 04;16(5):3787-801.

PMID: 21544041 DOI: 10.3390/molecules16053787

Preliminary investigations were carried out to evaluate the antidiabetic effects of the leaves of O. stamineus extracted serially with solvents of increasing polarity (petroleum ether, chloroform, methanol and water); bioassay-guided purification of plant extracts using the subcutaneous glucose tolerance test (SbGTT) was also carried out. Only the chloroform extract, given at 1 g/kg body weight (b.w.), significantly reduced (P < 0.05) the blood glucose level of rats loaded subcutaneously with 150 mg/kg (b.w.) glucose. The active chloroform extract of O. stamineus was separated into five fractions using a dry flash column chromatography method. Out of the five fractions tested, only chloroform fraction 2 (Cƒ2), at the dose of 1 g/kg (b.w.) significantly inhibited (P < 0.05) blood glucose levels in SbGTT. Active Cƒ2 was split into two sub-fractions Cƒ2-A and Cƒ2-B, using a dry flash column chromatography method. The activities Cƒ2-A and Cƒ2-B were investigated using SbGTT, and the active sub-fraction was then further studied for anti-diabetic effects in a streptozotocin-induced diabetic rat model. The results clearly indicate that Cƒ2-B fraction exhibited a blood glucose lowering effect in fasted treated normal rats after glucose-loading of 150 mg/kg (b.w.). In the acute streptozotocin-induced diabetic rat model, Cƒ2-B did not exhibit a hypoglycemic effect on blood glucose levels up to 7 hours after treatment. Thus, it appears that Cƒ2-B functions similarly to metformin, which has no hypoglycemic effect but demonstrates an antihyperglycemic effect only in normogycemic models. The effect of Cƒ2-B may have no direct stimulatory effects on insulin secretion or on blood glucose levels in diabetic animal models. Verification of the active compound(s) within the active fraction (Cƒ2-B) indicated the presence of terpenoids and, flavonoids, including sinensitin.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

The physicochemical properties of geraniin, a potential antihyperglycemic agent

Elendran S, Wang LW, Prankerd R, Palanisamy UD

Pharm Biol, 2015;53(12):1719-26.

PMID: 25853977 DOI: 10.3109/13880209.2014.1003356

Natural products play a vital role in the discovery of leads for novel pharmacologically active drugs. Geraniin (GE) was identified as the major compound in the rind of Nephelium lappaceum L. (Sapindaceae), while ellagic and gallic acids have been shown to be its main metabolites. GE and its metabolites possess a range of bioactive properties including being an anti-infective, anticarcinogenic, antihyperglycemic, and antihypertensive.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

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: Hypoglycemic Agents/chemistry

Fulltext Optimization of Hyperglycemic Induction in Zebrafish and Evaluation of Its Blood Glucose Level and Metabolite Fingerprint Treated with Psychotria malayana Jack Leaf Extract

Benchoula K, Khatib A, Quzwain FMC, Che Mohamad CA, Wan Sulaiman WMA, Abdul Wahab R, et al.

Molecules, 2019 Apr 17;24(8).

PMID: 30999617 DOI: 10.3390/molecules24081506

A standard protocol to develop type 1 diabetes in zebrafish is still uncertain due to unpredictable factors. In this study, an optimized protocol was developed and used to evaluate the anti-diabetic activity of Psychotria malayana leaf. The aims of this study were to develop a type 1 diabetic adult zebrafish model and to evaluate the anti-diabetic activity of the plant extract on the developed model. The ability of streptozotocin and alloxan at a different dose to elevate the blood glucose levels in zebrafish was evaluated. While the anti-diabetic activity of P. malayana aqueous extract was evaluated through analysis of blood glucose and LC-MS analysis fingerprinting. The results indicated that a single intraperitoneal injection of 300 mg/kg alloxan was the optimal dose to elevate the fasting blood glucose in zebrafish. Furthermore, the plant extract at 1, 2, and 3 g/kg significantly reduced blood glucose levels in the diabetic zebrafish. In addition, LC-MS-based fingerprinting indicated that 3 g/kg plant extract more effective than other doses. Phytosterols, sugar alcohols, sugar acid, free fatty acids, cyclitols, phenolics, and alkaloid were detected in the extract using GC-MS. In conclusion, P. malayana leaf aqueous extract showed anti-diabetic activity on the developed type 1 diabetic zebrafish model.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Centrifugal air-assisted melt agglomeration for fast-release "granulet" design

Wong TW, Musa N

Int J Pharm, 2012 Jul 1;430(1-2):184-96.

PMID: 22531845 DOI: 10.1016/j.ijpharm.2012.04.026

Conventional melt pelletization and granulation processes produce round and dense, and irregularly shaped but porous agglomerates respectively. This study aimed to design centrifugal air-assisted melt agglomeration technology for manufacture of spherical and yet porous "granulets" for ease of downstream manufacturing and enhancing drug release. A bladeless agglomerator, which utilized shear-free air stream to mass the powder mixture of lactose filler, polyethylene glycol binder and poorly water-soluble tolbutamide drug into "granulets", was developed. The inclination angle and number of vane, air-impermeable surface area of air guide, processing temperature, binder content and molecular weight were investigated with reference to "granulet" size, shape, texture and drug release properties. Unlike fluid-bed melt agglomeration with vertical processing air flow, the air stream in the present technology moved centrifugally to roll the processing mass into spherical but porous "granulets" with a drug release propensity higher than physical powder mixture, unprocessed drug and dense pellets prepared using high shear mixer. The fast-release attribute of "granulets" was ascribed to porous matrix formed with a high level of polyethylene glycol as solubilizer. The agglomeration and drug release outcomes of centrifugal air-assisted technology are unmet by the existing high shear and fluid-bed melt agglomeration techniques.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

Animal models and natural products to investigate in vivo and in vitro antidiabetic activity

Hasan MM, Ahmed QU, Mat Soad SZ, Tunna TS

Biomed Pharmacother, 2018 May;101:833-841.

PMID: 29635892 DOI: 10.1016/j.biopha.2018.02.137

Diabetes mellitus is a chronic disease which has high prevalence. The deficiency in insulin production or impaired insulin function is the underlying cause of this disease. Utilization of plant sources as a cure of diabetes has rich evidence in the history. Recently, the traditional medicinal plants have been investigated scientifically to understand the underlying mechanism behind antidiabetic potential. In this regard, a substantial number of in vivo and in vitro models have been introduced for investigating the bottom-line mechanism of the antidiabetic effect. A good number of methods have been reported to be used successfully to determine antidiabetic effects of plant extracts or isolated compounds. This review encompasses all the possible methods with a list of medicinal plants which may contribute to discovering a novel drug to treat diabetes more efficaciously with the minimum or no side effects.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Ion-pair vortex assisted liquid-liquid microextraction with back extraction coupled with high performance liquid chromatography-UV for the determination of metformin in plasma

Alshishani A, Makahleh A, Yap HF, Gubartallah EA, Salhimi SM, Saad B

Talanta, 2016 Dec 01;161:398-404.

PMID: 27769423 DOI: 10.1016/j.talanta.2016.08.067

A new sample preparation method, ion-pair vortex assisted liquid-liquid microextraction (VALLME-BE), for the determination of a highly polar anti-diabetic drug (metformin) in plasma sample was developed. The VALLME-BE was performed by diluting the plasma in borate buffer and extracted to 150µL 1-octanol containing 0.2M di-(2-ethylhexyl)phosphoric acid as intermediate phase. The drug was next back-extracted into 20µL of 0.075M HCl solution. The effects of pH, ion-pair concentration, type of organic solvent, volume of extraction phases, ionic strength, vortexing and centrifugation times on the extraction efficiency were investigated. The optimum conditions were at pH 9.3, 60s vortexing and 2min centrifugation. The microextract, contained metformin and buformin (internal standard), was directly injected into a HPLC unit using C1 column (250mm×4.6mm×10µm) and detected at 235nm. The method was validated and calibration curve was linear with r2>0.99 over the range of 20-2000µgL-1. The limits of detection and quantitation were 1.4 and 4.1µgL-1, respectively. The accuracy was within 94.8-108% of the nominal concentration. The relative standard deviation for inter- and intra-day precision was less than 10.8%. The method was conveniently applied for the determination of metformin in plasma samples.

Matched MeSH terms: Hypoglycemic Agents/chemistry

A QSAR model for predicting antidiabetic activity of dipeptidyl peptidase-IV inhibitors by enhanced binary gravitational search algorithm

Al-Fakih AM, Algamal ZY, Lee MH, Aziz M, Ali HTM

SAR QSAR Environ Res, 2019 Jun;30(6):403-416.

PMID: 31122062 DOI: 10.1080/1062936X.2019.1607899

Time-varying binary gravitational search algorithm (TVBGSA) is proposed for predicting antidiabetic activity of 134 dipeptidyl peptidase-IV (DPP-IV) inhibitors. To improve the performance of the binary gravitational search algorithm (BGSA) method, we propose a dynamic time-varying transfer function. A new control parameter,
μ
, is added in the original transfer function as a time-varying variable. The TVBGSA-based model was internally and externally validated based on

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, Y-randomization test, and applicability domain evaluation. The validation results indicate that the proposed TVBGSA model is robust and not due to chance correlation. The descriptor selection and prediction performance of TVBGSA outperform BGSA method. TVBGSA shows higher

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compared to obtained results by BGSA, indicating the best prediction performance of the proposed TVBGSA model. The results clearly reveal that the proposed TVBGSA method is useful for constructing reliable and robust QSARs for predicting antidiabetic activity of DPP-IV inhibitors prior to designing and experimental synthesizing of new DPP-IV inhibitors.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

The biological activities of the spiderworts (Tradescantia)

Tan JBL, Kwan YM

Food Chem, 2020 Jul 01;317:126411.

PMID: 32087517 DOI: 10.1016/j.foodchem.2020.126411

Widely used throughout the world as traditional medicine for treating a variety of diseases ranging from cancer to microbial infections, members of the Tradescantia genus show promise as sources of desirable bioactive compounds. The bioactivity of several noteworthy species has been well-documented in scientific literature, but with nearly seventy-five species, there remains much to explore in this genus. This review aims to discuss all the bioactivity-related studies of Tradescantia plants and the compounds discovered, including their anticancer, antimicrobial, antioxidant, and antidiabetic activities. Gaps in knowledge will also be identified for future research opportunities.

Matched MeSH terms: Hypoglycemic Agents/chemistry

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