Inhibition Of Alpha-amylase Enzyme Research Articles

Pyrazole-based N-phenyl pyrazolines: Synthesis, docking, and pharmacological evaluation

A series of methoxy substituted pyrazole based pyrazoline derivatives (4a-j) were synthesized in good to excellent yield from corresponding pyrazole-chalcones (3a-j). All synthesized derivatives were characterized and screened for their in vitro anti-inflammatory, antioxidant, antidiabetic, and antibacterial activities. Among the series, compounds 4f, 4j, 4a, and 4i showed better anti-inflammatory activity as compared to diclofenac sodium. In DPPH free radical scavenging assay, all the compounds were shown excellent activity and moderate to good activity in SO and NO free radical scavenging assay as compared to standard ascorbic acid. Antibacterial screening of synthesized pyrazolines showed that compounds 4f and 4j have significant antibacterial activity. The compounds 4j, 4f, 4h, 4a, and 4c have shown comparable inhibition of alpha-amylase enzyme leading to good antidiabetic activity as compared to standard acarbose. Molecular docking studies suggest that these compounds have strong binding with COX-2 and alpha-amylase enzyme due to significant capability of aromatic and hydrophobic interaction. The outstanding results of reported compounds in all biological screening will pave the way for the design of new drug candidate bearing pyrazole moiety.

Evaluation of antioxidant, catalytic and antidiabetic activity of Phaseolus vulgaris (French green bean) mediated nickel oxide and copper doped nickel oxide bimetallic nanoparticles

In this study, nickel oxide nanoparticles (NPs) and copper doped NiO bimetallic nanoparticles (Cu@NiO BMNPs) were synthesized using Phaseolus vulgaris extracts as reducing and stabilizing agents by sol gel methods. The chemical and physical properties of synthesized NiO NPs and Cu@NiO BMNPs were confirmed by various techniques, like UV Visible spectrophotometer (UV–Vis), Fourier transform infrared spectroscopy (FTIR), Scanning Electron Microscope (SEM), Energy Dispersive X-ray (EDX), Transmission Electron Microscope (TEM) and X-ray diffraction (XRD) analysis. The optical properties of both NPs observed by UV–Vis analysis with well-defined peak and band gap value 3.2 eV & 2.62 eV. FTIR analysis confirmed the presence of functional group of NPs with fruits extract. The morphology of NPs was confirmed by SEM and TEM analysis as polygonal, rod and spherical shape. The elements present in NPs were confirmed by EDX analysis. The crystalline size calculated based on the XRD analysis was 49.78 nm and 53.66 nm for NiO and Cu@ NiO NPs respectively which were found to be slightly smaller than particle size determined from SEM and TEM micrograph. Antioxidant activity of NPs was examined using 2,2-Diphenyl-1-picrylhydrazyl (DPPH) scavenging radicals, Catalytic activities were screened by the degradation of Methylene blue (MB) and by the inhibition of alpha-amylase enzyme, antidiabetic activity of NPs were evaluated using acarbose as standard drug. The Cu@NiO BMNPs showed 77.60 % antioxidant, 76.98 % photocatalytic and 88.86 % antidiabetic activity, which were found to be more as compared to NiO NPs. The NiO and Cu@NiO BMNPs were synthesized for the first-time using P. vulgaris extracts. This study clearly showed that P. vulgaris extracts mediated mono- and bimetallic NPs were more stable and biocompatible than their respective bulk particles.

Effect of Curcuma longa Rhizome Powder on Metabolic Parameters and Oxidative Stress Markers in High-Fructose and High-Fat Diet-Fed Rats

Metabolic disorders have become a major and growing global health problem, so finding potentially novel solutions with fewer harm is favourable to solving this problem. Thus, this research aimed to determine the effect of a diet supplemented with Curcuma longa rhizome powder on markers of oxidative stress as well as biochemical and haematological parameters of rats with diet-induced metabolic disorders. The powder was obtained from fresh Curcuma longa rhizome for preparation of extracts, which were used for in vitro analysis. After induction of metabolic disorders in male Wistar rats, they were separated into five groups: base, control, and high-fructose and high-fat diet supplemented with Curcuma longa rhizome powder at 2.5%, 5%, and 10%, respectively. The phytochemical analysis of the Curcuma longa rhizome powder extracts revealed the presence of phenols (96.97 ± 0.79 mg GAE/g) and flavonoids (133.19 ± 1.64 mg CE/g) and also showed good activities in DPPH free radical scavenging (79.46 ± 2.12%) and good inhibition of alpha-amylase enzyme (94.12 ± 2.84%). The food supplementation with Curcuma longa rhizome powder lowered Lee index (326.88 ± 3.08 to 262.45 ± 4.71), glycaemia (189.25 ± 5.98 to 120.5 ± 4.91 mg/dl), peritoneal fat deposition (2.18 ± 0.02 to 1.35 ± 0.14 g/100 g of body weight), triglycerides (58.35 ± 5.37 to 109.94 ± 1.42 mg/dl), total cholesterol (208.53 ± 1.53 to 114.18 ± 2.20 mg/dl), LDL-cholesterol (128.73 ± 3.64 to 17.55 ± 1.59 mg/dl), malondialdehyde (67.54 ± 2.48 to 39.75 ± 1.02 nmol/ml), and nitric oxide (27.83 ± 1.44 to 19.36 ± 1.28 nmol/ml) and increased HDL-cholesterol (48.12 ± 1.82 to 74.21 ± 1.04 mg/dl) and catalase activity (4.12 ± 0.56 to 11.58 ± 0.83 U/min/ml) with the best result at 5% supplementation. According to these results, the Curcuma longa rhizome powder supplement is a promising alternative for the treatment of metabolic disorders and oxidative stress.

Cytotoxic, Antibacterial, Antioxidant, Anthelmintic, and Anticoagulant Potential of Phytochemicals from Simarouba glauca Leaf Extract

This study’s primary objectives were to evaluate phytochemical screening and identify therapeutic uses for the herb Simarouba glauca. By employing a Soxhlet apparatus, the leaves were extracted using ethyl acetate. Standard techniques were used for preliminary phytochemical analysis to screen the presence of secondary metabolites. The agar plate method was used to test for antimicrobial activity against Escherichia coli and Bacillus subtilis. The antidiabetic activity aimed to identify the alpha-amylase enzyme inhibition that is most effective at regulating blood glucose levels. The DPPH assay was used to screen the antioxidant activity. The extract’s bioactive components were purified using column and thin-layer chromatography. Simarouba glauca extract was tested for its cytotoxic property on the lung cancer cell line (A549) using the MTT assay. To find the phytocompounds present in the extract, GC-MS analysis was carried out. Anticoagulation activity was carried out to assess the prothrombin time of blood and therapeutic applications such as anthelminthic activity were determined by determining the time of death of parasites like earthworms. The tested extract showed considerable cytotoxic, antibacterial, antioxidant, anthelmintic, and anticoagulant activity.

In vitro antioxidant activity and antidiabetic potential of five spiral ginger (Costus speciosus (J. Koenig) Sm.) populations available in Sri Lanka

Diabetes mellitus has caused millions of deaths worldwide. Costus speciosus leaves are consumed as a green leafy vegetable in Sri Lanka due to their claimed medicinal properties including hypoglycemic effect. This work aimed mainly to evaluate the antioxidant and antidiabetic potential of the five distinct C. speciosus leaves populations (P1, P2, P3, P4, and P5) available in Sri Lanka for future therapeutic food applications. Methanol extracts and hot water infusions of C. speciosus leaves were obtained and the total phenolic content, flavonoid content, total antioxidant capacity, and DPPH radical scavenging activity were determined by colorimetric assays. Moreover, in vitro antidiabetic activity was assessed using alpha-glucosidase and alpha-amylase enzyme inhibition assays. There was a remarkable variation in the functional properties among the five populations of C. speciosus as well as among the five different leaf positions from the apical to the basal part of the twig. The highest total phenolic content, DPPH radical scavenging activity, and total antioxidant capacity were observed in methanol leaf extracts of P3 as 7.49 ± 0.21 mg GAE g-1, 91.57 ± 0.08%, and 10.39 ± 0.50 mg AAE g-1 respectively. Leaf bud contained significantly (p < 0.05) the highest total phenolic content and DPPH radical scavenging activity than the other leaf positions. C. speciosus population 1 exhibited significantly (p < 0.05) the highest antidiabetic activity in terms of alpha-glucosidase enzyme inhibition, with an IC50 value of 2.57 mg mL−1 compared to the standard acarbose (12.85 mg mL−1). In the conclusion of the study, C. specious variety available in Sri Lanka can be considered as a potential candidate for therapeutic food applications.

Evaluation of Anti-Diabetic Activity of Siddha Drug T. Kusta Gaja Kesari by Alpha Glucosidase and Alpha Amylase Enzyme Inhibition Assay: In Vitro Study

Evaluation of Anti-Diabetic Activity of Siddha Drug T. Kusta Gaja Kesari by Alpha Glucosidase and Alpha Amylase Enzyme Inhibition Assay: In Vitro Study

Evaluation of Phytochemical Composition, Antioxidant and anti-Diabetic Activities of Mitragyna speciosa Methanolic Extract (MSME)

Introduction: The therapeutic potential of plant-based or herbal medicine has been widely embraced by the public as a prevention and remedy for many illnesses. Mitragyna speciosa is one of the medicinal plant that exhibit the opioid-like effects of analgesia. This study aimed to evaluate the phytochemical content, antioxidant activity, and alpha-amylase enzyme inhibition of Mitragyna speciosa methanolic extract (MSME). Methods: The phytochemical composition of MSME was analyzed for secondary metabolites using UHPLC-TWIMS-QTOF-MS/MS. The total phenolic content (TPC), total flavonoid content (TFC), antioxidant scavenging activities (2,2-diphenyl-1-picrylhydrazyl [DPPH] and 2,2’-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) [ABTS] assays) and α-amylase enzyme inhibition activities of MSME were analyzed in comparison to positive control Pterostilbene and acarbose, respectively. Results: Analysis of UHPLC-TWIMS-QTOF-MS/MS has characterized the presence of at least five different bioactive compounds, mostly derivatives of flavonoids and polyphenols. A significantly higher level of TFC (347.72±15.97 mg QE/g extract; p = 0.0005), but a significantly lower level of TPC (167.43±13.50 mg GAE/g extract; p = 0.002) was detected in MSME (1 mg/mL) compared to Pterostilbene. MSME presented antioxidant activity which has no significant difference compared to Pterostilbene as determined by DPPH (MSME IC50 = 4.34±1.79 µg/mL; p = 0.727) and ABTS (MSME IC50 = 4.25±1.59 µg/mL; p = 0.311) assays. Moreover, MSME also exhibited anti-diabetic effects through inhibition of α-amylase activity (IC50 = 0.01±7.18 mg/mL) which shows a significant difference (p = 0.009) compared to acarbose. Conclusion: This finding suggests that MSME has bioactive phytochemicals and exhibits potential antioxidant and anti-diabetic properties.

Biogenic synthesis of cerium oxide nanoparticles using petals of Cassia glauca and evaluation of antimicrobial, enzyme inhibition, antioxidant, and nanozyme activities

Cerium oxide nanoparticles (CeO2NPs) are used in different research areas due to their distinctive attributes. This study reports the green synthesis of CeO2NPs using the aqueous extract of Cassia glauca flowers. The XRD analysis confirmed the pure face-centered cubic fluorite structure of the NPs with average size of 3.20 nm. FTIR analysis showed the attachment of functional groups on the surface of NPs. SEM images presented agglomeration of nanoparticles with spherical and irregular structures. The NPs showed moderate total antioxidant capacity (43.5 ± 1.15 μgAAE/mg), reducing potential (40.3 ± 0.85 μgAAE/mg), and DPPH based free radical scavenging potential (40.6 ± 1%). Nanoparticles presented moderate inhibition of alpha-amylase enzyme (18.7 ± 0.65%) but significant inhibition of urease (73.9 ± 1.2%) and lipase (75.9 ± 0.8%) was observed. The NPs exhibited effective peroxidase mimetic activity (1.0 ± 0.04 mM/min/mg) against hydrogen peroxide. Antibacterial results showed weak to mild activity against different bacterial strains. The report concludes that Cassia glauca flowers can synthesize CeO2NPs and the existence of oxygen vacancies in CeO2NPs facilitates the shifting between Ce3+ and Ce4+ by interaction with H2O2, extrapolating the environmental and biological uses of cerium oxide nanoparticles.

In vitro antidiabetic activity of Peperomia pellucida extract and fraction by alpha-amylase inhibition pathway

The development of type 2 diabetes is influenced by the important role of post-prandial blood glucose management. One strategy in controlling post-prandial hyperglycemia can be done by inhibiting the digestion of dietary carbohydrates through inhibition of alpha amylase enzyme. Natural alpha amylase enzyme inhibition strategy that utilizes natural ingredients is an important alternative in the development of antidiabetic drugs. One of the plants that has the potential to be developed as an antidiabetic is Peperomia pellucida . This study aims to examine the effects of antidiabetic extracts and fractions of Peperomia pellucida in inhibiting alpha amylase enzyme. The research was conducted by determining the total flavonoid using quercetin standard. Antidiabetic studies were carried out by looking at the activity of extracts and fractions of Peperomia pellucida in inhibiting alpha amylase enzyme using visible spectrophotometry method. Data analysis was performed by entering the absorbance value into the standard quercetin curve, while the IC50 value of in vitro antidiabetic activity was determined by entering the value 50 on the curve between the sample concentration and % inhibition of the alpha amylase enzyme. The results showed that the total flavonoid values of the ethanol extract and the ethyl acetate fraction of the herb were 88.24 mg QE/g extract and 80.45 mg QE/g fraction, respectively. Based on the results, the inhibition of alpha amylase enzyme showed that the ethanol extract and the ethyl acetate fraction of the herbs had inhibitory activity with the IC50 value of the ethanol extract 1065.54 g/mL and the ethyl acetate fraction 906.53 g/mL. While the control of acarbose showed an IC50 value of 379.45 g/mL. The ethanol extract and the ethyl acetate fraction of Peperomia pellucida herbs have the potential to be developed as antidiabetic agents with the mechanism of action of inhibiting the activity of the alpha amylase enzyme.

In vitro Therapeutic Effect of Spirulina Extract

Recent Research focused on bio therapeutic has wide range of application in medicinal field due to its activity and enormous nutritional values. The main objective of the study is to evaluate the blue green algae, Spirulina for their anti-bacterial, antioxidant, hemolytic, anti-diabetics and screening of phytochemical constituents. By disc diffusion method the four extracts (chloroform, hexane, petroleum ether and acetic acid) of Spirulina were screened for antibacterial activity against four pathogenic micro-organisms. The antioxidant activity was determined by DPPH method (free radical scavenging activity). The hemolytic activity was determined by using ELISA plate assay. In-vitro anti diabetic activity (Alpha amylase enzyme inhibition activity) of potential phytochemical constituents was determined qualitatively. The acetic acid extract of Spirulina showed significant anti-microbial activity among the different extracts tested. The most susceptible microorganism was found to be gram positive bacteria (Staphylococcus sp) and gram negative bacteria (E. coli, Klebsiella sp and Pseudomonas sp). DPPH free radical scavenging activity of Spirulina was found to be increase with its concentration. 2.303 ± 0.5 microgram of Spirulina was found in 20% concentration of ethanol extract. Spirulina was up to inhibit the activity of alpha-amylase that was dose dependent and also exhibits anti-inflammatory activity. Hence the present study shows that all the extracts of blue green algae of Spirulina have wide range of therapeutic effects.

Effect of drying methods and extraction solvents on anti-amylase activity of selected medicinal plants

Presently, there is a blooming recognition in using the herbal medicine to treat the Diabetic mellitus due to the negative side effects of usage in synthetic drugs. The present study was aimed to evaluate the potential of anti-amylase activity of three different leaf extracts of Thebu (Costus speciosus), Kowakka (Coccinia grandis) and Masbadda (Gymnema sylvestre) following different drying techniques i.e; shade drying at room temperature, oven drying at 45 oC and freeze drying. Dried plant leaves were macerated with n-hexane, ethyl acetate and ethanol for 24 hours at room temperature separately. Obtained extracts were used to determine the anti- amylase activity. Results revealed that freeze dried ethanolic leaf extracts of all selected species showed the highest anti- amylase activity compared to the other drying methods. Further, there was a significant effect (p &lt;0.05) on the drying techniques and solvents used to extract in inhibition of alpha amylase activity. Freeze dried C. speciosus and C. grandis ethanolic extracts displayed an effective inhibition against alpha amylase with an IC50 value of 4 mg/ml and 4.16 mg/ml respectively. Therefore, this study revealed that the drying methods significantly affected on the inhibition of alpha amylase enzyme. Freeze-drying was the most promising drying method and ethanol was the best solvent in extracting anti-amylase bioactive compounds from leaf extract of C. speciosus, C. grandis and G. sylvestre.

An In-silico and In-vitro Comparative Study of Compounds from Phoenix sylvestris Roxb. For Alpha-Amylase Enzyme Inhibition Involved in Diabetes Mellitus

Identification of potential phytocompound from Phoenix sylvestris RoxB. For anti-diabetic potential and its validation through computational methods. Partially purified fraction evaluated for Alpha-amylase enzyme inhibition and GC-MS identified fraction validated compounds for potential anti-diabetic activity by Auto docking method. The phytocompounds investigation revealed maximum abundance of total phenol (31.55±0.55 μg/mg equivalent to Gallic acid) and flavonoid (52.90±0.08 μg/mg equivalent to quercetin) content in ethyl acetate extract. Ethyl acetate extract interestingly showed maximum alpha-amylase inhibition (71.15 %, IC50- 98.50±0.10 μg/ml), which was a mixed type of inhibition as compared to acarbose (78.64%, IC50- 88.61±0.50 μg/ml), which showed a competitive type of inhibition analyzed by Line weaver-Burk double reciprocal plot versus 1/v and 1/s. The docking study illustrated that Lupenyl acetate compound was the most active compound that showed maximum binding free energy (-7.16 Kcal/mol) and interacted with the Val64, Asn88, Gly90, Asn87, Arg87, Arg10, Gly9, Gln7, Gln5, Thr5, Trp221, Phe222, Asn5, Pro223, Ser3, Ser226, Lys227 and Gly225 amino acid residues which inhibited the alpha-amylase more efficiently than acarbose (binding energy -4.71 Kcal/mol). The present study concluded that the components of ethyl acetate extract had Alpha enzyme inhibition with reducing potential, and it may be due to the synergistic effect. The study suggested ethyl acetate extract as a natural promising therapeutic compound for the treatment of diabetes.

Phytochemical analysis, phytotoxic and alpha amylase inhibition activity of Cyanodondactylon

Herbal medicines that obtained from medicinal plants are safe and oldest natural products used for treatment of different diseases. The present study was undertaken to evaluate the phytochemical analysis, phytotoxic activity and alpha amylase enzyme inhibition activity of methanolic extract of Cyanodondactylon. For this whole plant was collected and shade dried and grinded to get the powder. The extraction was carried out by cold percolation in methanol. The methanolic extract was subjected to phytochemical analysis for the absence or presence of secondary metabolites using standard protocol. In-vitro phytotoxic activity was performed by adopting the standard protocol. The alpha amylase enzyme inhibition activity of plant extract was carried out by using starch as substrate, pancreatic alpha amylase as the enzyme, and acarbose as standard. Phytochemical analysis displayed the presence of different chemical constituents such as alkaloids, flavonoids, tannins, polyphenols, terpenoids etc. The result of in-vitro phytotoxic bioassay revealed that the plant extract showed moderate activity with percentage growth regulation 75% in 1000 µg/ml and 30% in 10 µg/ml. The alpha amylase enzyme inhibition was 96.2% at 1000 µg/ml while 37.06% at 40 µg/ml concentration. The inhibition was found dose dependent.

Antioxidant and Antidiabetic Activities of Fresh Aqueous Pink Petals of Indian Lotus-Nelumbo nucifera Gaertn.

The genus Nelumbo is endowed with a number of medicinally important activities antidiabetic, antipyretic, anti-inflammatory, anti-cancerous, antimicrobial, antiviral and anti-obesity properties. Furthermore, Nelumbo nucifera flowers are served as healthy beverages to treat hypertension, cancer, diarrhea, fever, weakness, infection and body heat imbalance. It has been widely used in folk medicine for the treatment of various inflammatory and infectious diseases. Current research studies were carried out for evaluating the antioxidant, antidiabetic and antibacterial activities of fresh aqueous pink petals of Nelumbo nucifera. Antioxidant activities such as DPPH˙ radical, Superoxide (O2.-) radical, ABTS●+ radical cation, phosphomolybdenum reduction and Fe3+ reduction were carried out for fresh aqueous pink petals of Nelumbo nucifera. The maximum DPPH˙ radical scavenging activity was 88.33±0.47% at 300 µg/mL concentration and the IC50 value was 131.68 µg/mL concentration. The maximum superoxide (O2.-) radical scavenging activity was 86.76±0.31% at 120 µg/mL concentration and the IC50 value was 21.31 µg/mL concentration. The maximum ABTS●+ radical cation scavenging activity was 69.55±0.26% at 30 µg/mL concentration and the IC50 value was 10.82 µg/mL concentration respectively. The maximum Mo6+ reduction was 84.54±0.21% at 45 µg/mL concentration and the RC50 value of Mo6+ reduction was 25.79 µg/mL concentration. The maximum Fe3+ reduction was 56.00±0.38% at 300 µg/mL concentration and the RC50 value of Fe3+ reduction was 177.30 µg/mL concentration respectively. The maximum alpha amylase enzyme inhibition was 66.37±0.10% at 300 µg/mL concentration and the IC50 value was 63.84 µg/mL concentration respectively. The antibacterial activity of fresh aqueous pink petals of Nelumbo nucifera showed maximum zone of inhibition of 14 mm for B. subtilis and minimum zone of inhibition of 10 mm for E. coli at 375 µg/mL concentration. &#x0D; Keywords: Antioxidant, Superoxide (O2.-) radical, ABTS●+ radical cation, Fe3+ reduction and alpha-amylase.

Studi Kandungan Fitokimia Ekstrak Etanol Daun Gambir Asal Aceh Tenggara Sebagai Anti Diabetes

Indonesia is one of tropical countries that rich in natural resources. It has more than a thousand of medicinal plants. This study focused on assessing the potential of phytochemical content gambir leaves from Southeast Aceh as an alternative of antidiabetes through inhibition of alpha amylase enzyme. Steps of research to be conducted consist of: (1) Making dry simplisia from gambir leaves; extraction of gambir leaves by maceration for 2x24 hours and screening done every 24 hours, and solvent evaporation to obtain the dry extract of gambir; (2) Analysis of phytochemical (phenolic, flavonoid and tannin) content of ethanol extract of gambir leaves; and (3) Analysis of chemical components using GC-MS. The results showed that the moisture content of powder gambir leaves was 3,017%, which is still below the national standard. The ethanol extract contained a rendement of 2,47 gr / gr of dry weight. The inhibition activity of alpha amylase enzyme was obtained at a sample concentration of 1000 ppm , e.i 88.22%. The more active a sample in inhibiting the action of the alpha-amylase enzyme, the less the 3-amino-5-nitrosalisilic acid formed in the second stage of enzyme activation. The results of phytochemicalanalysis of ethanol extract of gambir leaves from Southeast Aceh showed secondary metabolite content such as Total Phenolic, Total Flavonoid, and Tanin respectively of 71, 80; 32, 06 and 58.39%. The chemical components, e.i the total phenolics, flavonoids and tannins have been reported to have antidiabetic activity by lowering blood sugar levels after inhibition testing via the alpha amylase enzyme.

Studies on &lt;i&gt;in vitro&lt;/i&gt; evaluation of antidiabetic potentials of watermellon and pomegranate peels

Diabetes is a metabolic disorder which results due to deficiency in insulin and its metabolism. At present, the prevalence of Diabetes has increased worldwide and predicted to increase to greater extent in future generations. Among various therapeutic approaches implemented to prevent diabetes is to regulate the blood glucose levels by various mechanisms. This is being assessed by in vitro antidiabetic assays such as inhibition of carbohydrate digesting enzymes and non-enzymatic glycosylation of haemoglobin. Inhibition of alpha-amylase enzyme suppresses the level of production of glucose and by inhibiting glycosylation of haemoglobin the level of blood glucose is maintained. Hence the current work focuses on investigating the anti-diabetic activity of fruit peel of Citrullus lanatus (watermelon) and Punica granatum (pomegranate) using the above mentioned assays. Our results suggested that methanol extract of Citrullus lanatus and Punica granatum peels showed potential anti-diabetic activity in vitro which indicates that these extracts can be taken further for in vivo studies.Keywords: fruit peels, antidiabetic activity, α-amylase enzyme, glycosylated haemoglobin

Simultaneous-HPLC Quantification of Phenolic Acids in Traditionally used Ayurvedic Herb Diplocyclos palmatus (L.) Jeffry

Introduction:The present study deals with the simultaneous HPLC-quantification of phenolic acid(s) in the aerial parts of Diplocyclos palmatus (Cucurbitaceae) and evaluation of their bioactivity potential through in vitro antioxidant assay’s. Method: The HPLC elution was done using C18 column using gradient (binary phases) solvent system at a flow rate of 0.6 ml/min. Total phenolic and, flavonoid contents were determined and the antioxidant potential was estimated by four assay’s viz. DPPH radical scavenging assay, ferric reducing power assay, total antioxidant capacity and 2-deoxy ribose assay. Results: The species is rich in three phenolic acids, among which gallic acid (1708 ug/g) is in maximum concentration followed by caeffic acid (437 ug/g) and protocateuchic acid (337.7 ug/g). Total phenolic content was higher (10.5 mg/g) than flavonoid content (3.78 mg/g) and TAC was found at 0.137 mg/g ASE (ascorbic acid equivalent). IC50 of D. palmatus extract for scavenging of hydroxyl radical by 2-deoxy ribose and DPPH was at concentration of 125.61 ± 0.834 (μg/ml) and 353.71 ± 0.663 (μg/ml) respectively. In vitro antidiabetiv potential, via inhibition of alpha amylase enzyme through starch iodine and 3,5- DNS assay reveals the IC50 of extract at 146.31 ± 0.415 ug/ml and 286.23 ± 0.671 ug/ ml respectively. Conclusion: The species (aerial part) was rich in phenolic acid with potential bioactivity, identified leads will be useful in further chemical characterization and pharmacological validation.

Pharmacological characterization of liquiritigenin, a chiral flavonoid in licorice.

Liquiritigenin is a chiral flavonoid present in plant based food, nutraceuticals, and traditional medicines. It is also an important ingredient present in licorice. The purpose of this study is to explore the pharmacological activity of racemic liquiritigenin utilizing several in vitro assays with relevant roles in colon cancer and diabetes. Where possible, the pure enantiomers were tested to identify the stereospecific contribution to the activity. In vitro antioxidant, anticancer, anti-inflammatory activities (cyclooxygenase inhibition), antidiabetic activities (alpha-amylase and alpha-glucosidase inhibition) as well as cytochrome P450 (CYP450) inhibitory activities were assessed. Racemic liquiritigenin demonstrated a dose-dependent inhibition of alpha-amylase enzyme whereas its pure enantiomers did not. Racemic liquiritigenin showed moderate antiproliferative activity on a HT-29 (human colorectal adenocarcinoma) cancer cell line that was dose-dependent and potent inhibitory effects on the cyclooxygenase-2 enzyme. The flavonoid did not inhibit the activity of cytochrome CYP2D6 over the concentration range studied but was a potent antioxidant. The current study demonstrated the importance of understanding the stereospecific pharmacological effects of liquiritigenin enantiomers in alpha-amylase inhibition.

In vitro alpha-amylase inhibition and in vivo antioxidant potential of Amaranthus spinosus in alloxan-induced oxidative stress in diabetic rats

Amaranthus spinosus Linn. (Amaranthaceae), commonly known as “Mulluharivesoppu” in Kannada, is used in the Indian traditional system of medicine for the treatment of diabetes. The present study deals with the scientific evaluation of alpha amylase and the antioxidant potential of methanol extract of A. spinosus (MEAS) . The aim of this study was to investigate in vitro alpha-amylase enzyme inhibition by CNPG3 (2-chloro-4-nitrophenol α- d-maltotrioside) and in vivo antioxidant potential of malondialdehyde (MDA), glutathione (GSH), catalase (CAT) and total thiols (TT) in alloxan-induced diabetic rats of a methanolic extract of A. spinosus. Blood sugar was also determined in MEAS-treated alloxan-induced diabetic rats. MEAS showed significant inhibition of alpha-amylase activity and IC 50 46.02 μg/ml. Oral administration of MEAS (200 and 400 mg/kg) for 15 days showed significant reduction in the elevated blood glucose, MDA and restores GSH, CAT and TT levels as compared with a diabetic control. The present study provides evidence that the methanolic extract of A. spinosus has potent alpha amylase, anti-diabetic and antioxidant activities.