Enzymes Amylase Research Articles

Orange peels and acha grain-based cornflakes modulates notable biochemical enzymes in diabetic-hypertensive rats

Cornflakes are popular breakfast cereals however, hypertensive and diabetic patients or diabetic-hypertensive (DBP-HYP) patients on medication are not advised to consume cornflakes as its high calorie content further complicates their condition. The effects of formulated cornflakes produced from yellow corn, acha grains (AG) and orange peel (OP) flour on fasting blood glucose (FBG) levels, glycemic index (GI), α-amylase and hemodynamic blood pressures (BP) in rats treated with acarbose (25 mg/kg) and captopril (25 mg/kg) standard drugs is unknown. Sixty-six adult male rats were randomly divided into eleven groups (n -6). Produced cornflakes from AG and OP was administered to experimental rats at various proportions. GI of cornflakes, BP and FBG levels of rats fed on these functional cornflakes were assessed. Additionally, the antioxidant status of DBP-HYP rats, amylase, arginase, and phosphodiesterase-5 (PDE-5) enzymes activities in the pancreas and heart were recorded. Interestingly, the GI of cornflakes, FBG, BP of DBP-HYP-treated rat groups decreased significantly (P<0.05) while the antioxidant ability and inhibitory effects on the amylase, arginase, and PDE-5 enzymes was elevated in DBP-HYP rats fed with formulated cornflakes. Therefore, OP and AG grain-based cornflakes produced in this study contributed to lowering FBG and BP of drug-managed DBP-HYP conditions in rats.

Using α -amylase enzyme with the seed pre-soaking to develop emergence and yield of triticale

In order to investigate the efficiency of stimulating stored seeds of Triticale (X Triticosecale wittmack) by α -amylase enzyme, a field experiment was carried out using split plot arrangements according to a randomized complete block design in three replications. The storage period of seeds 6 months, 1.5 years, and 2.5 years represented the main plots. The stimulation treatments was secondary plots included dry seeds (control), stimulated seeds with distilled water, 1 and 2 mg L-1 of α -amylase enzyme. The results showed a significant decrease in the percentage of emergence, plant leaf area, plant dry weight, number of tillers m-2, number of spikes m-2, weight of one thousand grains, and grain yield with the increasing of storage period. The enzyme concentration of 1 mg L-1 was the superior in % emergence (85.02), Plant leaf area (244.88) cm2, plant dry weight (2.087) g, number of tillers (448.8) tiller m-2, number of spikes (372.9) spike m-2, number of grains spike-1 (44.13) grain spike-1 and grain yield (5.842) ton h-1. However, there was on significant differences between the two concentration 1 and 2 mg L-1 of enzyme in leaf area, plant dry weight, 1000 grain weight and grain yield.

Development of Technology for the production of finished forms of Medicinal probiotics

The study aimed to develop a technology for the production of a finished form of medicinal probiotic agents against human intestinal infections based on active strains of lactic acid and propionic acid bacteria with a wide range of biological activity and resistance to antibiotics. From the laboratory collection of lactic acid and propionic acid bacteria isolated from the intestines of healthy people, two associations of bacteria were compiled with antagonism against test cultures of Staphylococcus aureus, Salmonella gallinarum, Mycobacterium B5, Candida albicans, Pasteurella multocida, Bacillus subtilis, Escherichia coli 8739, Klebsiella pneumoniae ATCC 700603 and ATCC BAA 2524, Staphylococcus aureus 3316 and 9, Salmonella enteritidis 35382, and Pseudomonas aeruginosa 835, as well as the ability to produce hydrolytic enzymes amylase and proteinase, B vitamins, and essential amino acids. The resistance of the selected associations of lactic acid and propionic acid bacteria to the used antibiotics has been studied, which will allow for using them, if necessary, in the complex therapy of diseases. Technology for the production of probiotic medication from these associations has been developed. It was found that the most active preparation in terms of bacterial titer and antagonistic activity and the most stable one during storage for 6 months was the liquid preparation obtained by growing association No. 2 (L. plantarum 2v/A-6+L. brevis B-3/A-26+L. acidophilus 27w/60+P. shermanii 8) on nutrient medium No. 1 (De Man, Rogosa and Sharpe agar with CoCl2) using 7% sucrose and 1.5% gelatin as a protector. The liquid preparation from association No. 5 grown on medium No. 1 showed a more complete preservation of production-valuable signs during storage compared to the results of using nutrient medium No. 4, while the use of protector No. 1 was more optimal. To test the stability during the storage of dry preparation forms, an accelerated method was used by warming them up for 15 minutes at 60°C. It was found that after warming up, the best preservation of viable bacterial cells was observed in association No. 2 on nutrient media No. 1 and No. 4, in association No. 5 on medium No. 4 dried with protector No. 2 (7% sucrose and 1.5% gelatin + 7% skim milk powder), while the titer of bacteria was equal to 1.2×109, 3.5×108, and 2.0±0.2×108 colony-forming units/g, respectively. Antagonistic activity in these association variants was observed against all test cultures taken into the study with zones of suppression of their growth ranging from 10 to 24 mm.

Analysis of Digestive Enzymes Concentration in Gut of Juvenile and Adult Group of Notopterus notopterus (Notopteridae; Osteoglossiformes)

Analyzing digestive enzyme concentration in the gut is important to know about the digestive physiology of fish. Therefore, we determined concentrations of protease, lipase, and amylase enzyme in gut extracts of juvenile and adult groups of Notopterus notopterus relative to total body length (TBL), body weight (W), gut length (GL), relative gut length (RGL), Zihler's index (ZI) and condition factor (K). A total of 60 N. notopterus specimens (30 juvenile and 30 adult) were collected, the gut of each removed, homogenized, and evaluated for the concentrations of protease, lipase, and amylase. Protease and lipase concentration were observed significantly (P &lt; 0.01) correlated with increased TBL, W, and GL in both juvenile and adult groups of N. notopterus. Amylase concentration significantly (P &lt; 0.01) increases with an increase in TBL, weight, and GL in the juvenile group, whereas amylase concentration significantly (P &lt; 0.01) decreases with an increase in TBL, W, and GL in the adult group. K had a significant (P &lt; 0.01) positive correlation with protease and lipase concentrations in both juvenile and adult groups, whereas K showed a significant (P &lt; 0.01) positive correlation with amylase concentrations in juvenile and significant (P &lt; 0.01) negative correlation in the adult group. Protease and lipase concentration were observed significantly (P &lt; 0.01) correlated with an increase in ZI in the juvenile and adult groups. Amylase concentration significantly (P &lt; 0.01) increases with an increase in ZI in the juvenile group, whereas amylase concentration significantly (P &lt; 0.01) decreases with an increase in ZI in the adult group. The concentrations of protease (344.12 U/mg) and lipase (172.49 U/mg) were observed high in juvenile and adult groups, whereas amylase concentration (3.80 U/mg) was found low in the juvenile and adult N. notopterus groups. Present study results revealed the digestive physiology and carnivorous behavior of N. notopterus. Moreover, information from the present study about digestive enzyme concentration in juvenile and adult species of N. notopterus provides valuable information to understand the digestive physiology of carnivorous fishes.

Assessing the Prevalence of Age-related Enzyme Deficiency in Indian Population and the Efficacy of Supplementing with a Combination of Alpha- Amylase and Papain Enzyme in this Population

Background: Enzymes are crucial for proper bodily functions, but as individuals age or experience medical conditions,their levels decrease, leading to several health issues most common being the gastrointestinal (GI) problems like dyspepsia,constipation and irritable bowel syndrome (IBS). The study assessed age-related enzyme deficiency in the Indian populationand investigated the effectiveness of a combined supplementation of alpha-amylase and papain enzymes. Methods: The studywas a retrospective study in July 2023 used a questionnaire-based survey to assess the prevalence of age-related enzymedeficiency in Indian population and the efficacy of supplementing with a combination of alpha-amylase and papain enzyme inthis population. The study used a validated questionnaire with 18 questions, and data was entered into a software database.Complete cases were analyzed, and missing data was excluded due to low occurrence. The final report was prepared aftercleaning the data. Result: The study included 134 doctors from various medical specializations. Results showed that themajority of doctors were GI specialists, with the highest frequency of patients with age-related enzyme deficits in the 40 to 60 years age groups (55.2%). The combination of alpha-amylase and papain was found to relieve proton pump inhibitor (PPI) overuse adverse effects. The safety profile was neutral (64.9%), with 30.6% stating it as safe and 2.2% as very safe. The combination was found to be neutral (48.5%), effective (45.5%) and very effective (3.7%), with age-related considerations being the main factor. Most doctors rated the combination as neutral (64.9%), with 29.1% giving a good rating and 5.2% giving a very good rating. Conclusion: In conclusion, this study sheds light on the prevalence of age-related enzyme deficiency in the Indian population and provides evidence for the potential efficacy of a combined alpha-amylase and papain enzyme supplement in addressing these deficiencies.

Evaluation of bergenin in amylase enzyme inhibition and lipid uptake in liver cells

Changes in the global economy contribute to a sedentary lifestyle and higher caloric intake, increasing the incidence of metabolic diseases. It is estimated that the number of individuals diagnosed with metabolic diseases will increase by 25% by 2030 and 51% by 2045. Natural products have been tested in metabolic diseases with positive results, as shown by bergenin. Thus, this work aimed to evaluate the possible effects of bergenin in models of metabolic disease through in silico and in vitro experimental procedures. Bergenin showed the ability to inhibit protein glycation by 19.88 ± 4.22% in the oxidative pathway and 8.32 ± 1.85% in the non-oxidative pathway. This study showed for the first time that bergenin has the potential to inhibit the α-amylase enzyme (33.89 ± 0.96%) using in silico and in vitro assays. Bergenin was not able to significantly inhibit lipid uptake by the Oil Red method. After these results, it is understood that bergenin has the potential to be better studied as a therapeutic option in metabolic diseases. However, additional in vivo studies are needed to better elucidate the possible pharmacological effects of bergenin in metabolic diseases.

Pemanfaatan Bakteri Termofilik Penghasil Amilase Pada Berbagai Pati

Indonesia is a country that produces a lot of starchy materials such as cassava, sago, corn and others. Indonesia has the potential to develop an enzyme-producing industry, especially amylase. The utilization of starchy materials which so far has not been maximized and is still limited to conventional methods can be increased by enzymatic development processes. This will increase its economic value and at the same time increase state income. One of the enzymes that is currently very widely used in the food and beverage industry is amylase. Nin Suharti and Geminsyah Putra 2021 have succeeded in isolating and identifying thermophilic bacteria from the sidedust hot springs of North Sumatra. The advantage of thermophilic bacteria is that they can produce enzymes that are resistant to high temperatures / thermostable enzymes. These enzymes are able to survive and are active at high temperatures. Such properties are highly needed by enzyme-based industries. The use of enzymes that can withstand high temperatures in the field of biotechnology can reduce operating costs and increase reaction speed, this study uses various types of starch including potatoes, cassava and corn as suitable and easily available carbon sources for the production of amylase enzymes. Bacteria in the media with potato starch added can produce the highest amylase enzyme from the three treatments of 65 U/L. For bacteria added with corn starch, the result was 50 U/L of amylase enzyme. Meanwhile, the lowest of the three treatments was media with added sweet potato starch with a content of 39 U/L. The isolates generally had a round shape, jagged edges, grooved, and smooth, white colonies, microscopic bacilli-shaped, endospores and motile, positive for catalase, gelatin and citrate tests. With Gram staining, it generally shows a positive Gram reaction.

Industrially significant biomolecules from recently discovered haloalkaliphiles, inhabitants of the coastal mangrove vegetation in Bordi, India

The coastal Arabian Sea area near Bordi, Maharashtra, India is one of the natural places for mangrove vegetation. This sampling site has been explored for the first time, and to the best of our knowledge, no other researchers have conducted scientific research on the same site prior to this. Water samples from the rhizosphere of the mangrove Avicennia marina were collected and physicochemical examination revealed that the water samples were of saline-alkaline quality. The haloalkaliphiles were isolated by using different microbiological media and characterized by polyphasic approach. Further, the isolates were identified by 16 S rRNA partial gene sequencing and MEGA version 11, a public domain was used for the evolutionary studies. The production of industrially important hydrolytic enzymes amylase, lipase, and protease were optimized in submerged fermentation media using efficient isolates via the OVAT approach, and the enzymes were found to be alkali and salt stable. The carotenoid producer, Planococcus plakortidis BMS5, was deposited at N.C.M.R., Pune, India under accession number MCC5186. The synthesis of carotenoids by Planococcus plakortidis BMS5 was carefully investigated. Thin layer chromatography, UV–VIS spectroscopy, and GC-MS were used to characterise the carotenoids. The hydrolytic enzymes produced by the efficient isolates exhibited great activity and stability over a wide pH (7−12) and temperature (20–50 oC) range. Furthermore, at 10–15% salt, the hydrolytic enzymes were the most stable. The carotenoids produced by haloalkaliphiles were discovered to have antioxidant characteristics and could be exploited in the food and pharmaceutical industries. The haloalkaliphiles' hydrolytic enzymes have the potential to be used in the development of new medicinal formulations. Overall, this study illustrates the potential of employing microbes from extreme environments to produce useful bioactive chemicals with a variety of applications in diverse industries.

A MINI REVIEW ON ZINGIBERACEAE FAMILY AS ANTIDIABETIC PLANTS: ACTIVE INGREDIENTS AND MECHANISMS OF ACTIONS

Diabetes mellitus (DM) is a group of metabolic diseases characterized by hyperglycemia that occurs due to abnormalities in insulin secretion. Therapy using conventional anti-diabetic drugs is associated with serious side effects, and herbs to maintain chronic disease if conventional drugs not adequate. The purpose of this article review is to find out information about plants of the Zingiberaceae family that have anti-diabetic activity with the mechanism of action of ? -glucosidase enzyme inhibition, ? -amylase enzyme inhibition, and increased GLP-1 levels. The sources used consisted of 27 journals and reviewed 9 research journals originating from Google Scholar, Pubmed, NCBI, Elsevier, Science Direct with a span of under 10 years. The articles were then analyzed using the systematic literature review method, by collecting, evaluating, and developing research on a particular topic. From several studies conducted, the results showed that plants from the family that have antidiabetic activity include Zingiber officinale (ginger), Curcuma longa (turmeric rhizome), Curcuma aeruginosa (temu hitam), Curcuma zanthorrhiza (curcuma), Zingiber cassumunar (bangle), Kaempferia galanga (kencur), Alpinia galanga (lengkuas), Etlingera elatior (kecombrang, honje), and Elettaria cardamomum (kapulaga). Keywords: Antidiabetic; Diabetes Mellitus; Zingiberaceae

Isolation and Screening of Amilolytic Bacteria Isolate from Cassava (Manihot utilissima)

Amylase is an enzyme capable of hydrolyzing starch into simpler sugars. The use of amylase enzymes is urgently needed in various industrial fields, therefore the search for sources of amylase enzyme producers continues to be carried out for sources of amylase enzyme producers. Each industrial field has specific requirements for amylase enzymes. This study aims to isolate bacteria capable of producing amylase enzyme and to determine the amylase activity of bacteria isolated from cassava (Manihot utilissima) when incubated at different temperatures (room temperature and 30℃) and pH levels (7, 8, 9, and 10). The research involved bacterial isolation, testing the amylase activity of the isolated amylolytic bacteria at varying pH and temperatures, and characterizing the amylolytic bacteria. The amylolytic bacterial activity was qualitatively measured based on the clear zone's area formed around the colony. From this study 5 isolates showing amylolytic activity were obtained. The amylolytic activity index varied among the isolates, ranging from 0.12 to 0.59. The highest amylolytic activity index (0.59) was performed by S4 isolate on pH 10 medium incubated at 30℃. Microscopic and gram staining analysis suggest that two isolates were gram-negative coccus bacteria and three of them were gram-positive coccobaccilus bacteria.

Probiotics: an innovative approach to enhancing aquaculture productivity

Probiotics refer to live beneficial microorganisms introduced into the digestive system via food or water, contributing to overall well-being by promoting a balanced internal microbial environment. These probiotic microorganisms produce a variety of substances, including bacteriocins, siderophores, lysozymes, proteases, and hydrogen peroxide, which effectively inhibit the growth of harmful pathogens. Furthermore, these beneficial bacteria generate a diverse set of enzymes, including amylase enzymes produced by Aeromonas spp., Bacillus subtilis, Bacteroidaceae, Clostridium spp., Lactobacillus plantarum, and Staphylococcus sp., as well as protease and cellulase enzymes produced by B. subtilis, L. plantarum, and Staphylococcus sp. In aquaculture, probiotics have several advantages and play a crucial role in improving fish growth rates, disease resistance, immunity, maintaining health, intestinal epithelial integrity, supporting gut microbiota, and enhancing water quality. Furthermore, the practical application of probiotics in fish diets can reduce the negative impact of antibiotics. The incorporation of these supplements into fish feeds would contribute to improving their productivity and efficient feeds utilization, thereby increasing fish production and safeguarding human health. This article provides an overview of the use of probiotic preparations in aquaculture. It presents information about the composition of the innate microflora in fish, as well as historical facts regarding the development of probiotics in aquaculture. The data analysis indicates that probiotics are effective and environmentally friendly, making them suitable for the entire aquaculture system, including primary and supplementary feeding, as well as water purification. They have a positive impact on the health of aquatic organisms and consumers. Additionally, the article discusses the appropriateness of probiotic use in aquaculture for dynamic and environmentally safe fish farming development, aiming to reduce the spread of antibiotic and chemical resistance and address disease treatment and prevention in fish farms.

Enzyme activity, DNA degradation and drying times of semen, saliva and vaginal material

The stability of enzyme activity and the amount of detectable DNA within liquid samples of semen, saliva and vaginal material were tested across a number of days. The concentration of DNA within neat semen and saliva samples fell significantly after one week of refrigeration. No apparent change in acid phosphatase or amylase enzyme activity was observed in neat semen and saliva samples over 96 or 72 h respectively. Changes in the enzyme activity of most of the dilute semen and saliva samples, as well as the neat vaginal material sample, were noted after 24 h. The drying times and sizes of stains produced from various volumes of neat semen, saliva and vaginal material were tested on porous and non-porous surfaces at room temperature. Larger volumes of body fluid took longer to dry and generally resulted in larger stains. Body fluids on a non-porous surface took longer to dry than on the porous surface tested.

Exploring hostel kitchen waste as feedstock for bioethanol and biogas production in a biorefinery setup

Waste to wealth is today’s need, as waste generation has become humongous challenge for mankind now. In the present study kitchen waste from the Institute, hostel mess is used as raw material for ethanol, biogas, and manure production in a bio-refinery system. In the first step of the biorefinery the kitchen waste, which contains approximately 35% carbohydrates, was pretreated with 0.5 % H2SO4 to release sugars required for fermentation and 3.6 mg/ml of reducing sugars, and 0.46 mg/ml of pentose sugar. Enzymatic hydrolysis of the un-hydrolyzed biomass remnant after acid pretreatment at 30 °C with crude amylase (enzyme activity: 45.36 U/min/ml) obtained from Aspergillus niger followed by hydrolysis at 55 °C with crude cellulase (enzyme activity: 36.25 U/min/ml) and xylanase activity (activity: 11.25 U/min/ml) obtained from Trichoderma reesei produced 1.64 mg/ml and 1.66 mg/ml hexose and pentose sugar, respectively. Fermentation of the hydrolysate with S. cerevisiae and Pistia stipitis produced a 2.43% (v/v) ethanol yield. Anaerobic digestion of the unutilized solid biomass produced 270 ml/Kg biogas and 63.35 gm/Kg dry soil nutrient enhancer. The study suggested that the kitchen waste-based economically viable bio-refinery setup can be developed for the eco-friendly management and production of various valuable products from kitchen waste.

Structural and functional integrity of endocrine pancreas post administration of Karwinskia humboldtiana fruit to Wistar rats: a possible therapeutic application for cancer of exocrine origin.

Pancreatic adenocarcinoma represents a therapeutic challenge due to the high toxicity of antineoplastic treatments and secondary effects of pancreatectomy. T-514, a toxin isolated from Karwinskia humboldtiana (Kh) has shown antineoplastic activity on cell lines. In acute intoxication with Kh, we reported apoptosis on the exocrine portion of pancreas. One of the mechanisms of antineoplastic agents is the induction of apoptosis, therefore our main objective was to evidence structural and functional integrity of the islets of Langerhans after the administration of Kh fruit in Wistar rats. TUNEL assay and immunolabelling against activated caspase-3 were used to detect apoptosis. Also, immunohistochemical tests were performed to search for glucagon and insulin. Serum amylase enzyme activity was also quantified as a molecular marker of pancreatic damage. Evidence of toxicity on the exocrine portion, by positivity in the TUNEL assay and activated caspase-3, was found. On the contrary, the endocrine portion remained structurally and functionally intact, without apoptosis, and presenting positivity in the identification of glucagon and insulin. These results demonstrated that Kh fruit induces selective toxicity on the exocrine portion and establish a precedent to evaluate T-514 as a potential treatment against pancreatic adenocarcinoma without affecting the islets of Langerhans.

In vivo inhibitory effect of Panicum maximum root extract on alpha amylase and alpha glucosidase enzymes of rats

Panicum maximum Jacq, (Poaceae) a medicinal plant used traditionally in the treatment of diseases including diabetes was evaluated for effect on alpha amylase and alpha glucosidase enzymes in vivo. The leaf extract (137, 273, and 547 mg/kg) of Panicum maximum were investigated in vivo for inhibitory effect on alpha amylase and alpha glucosidase enzymes using starch, sucrose and maltose as substrates. Acarbose was used as reference drug. The leaf extract non dose-dependently caused significant (p&lt;0.05) reduction in blood glucose levels of treated rats with the various substrates used. The results suggest that the leaf extract of Panicum maximum have the potentials to inhibit alpha amylase and glucosidase in rats.

Seleksi dan Karakterisasi Bakteri Halotoleran Penghasil Enzim Amilase Dari Produk Fermentasi Ikan-Inasua

Fish-inasua fermented food is a potential source to obtain halotolerant bacteria-producing amylase. Previously, four bacterial isolates such as IG12, IG6, IG66, and IG31, isolated from this food, have been reported to be able to produce protease and lipase enzyme, but their potential as amylase enzyme producers have not been studied. This study aims to characterize and test the potential of halotolerant bacteria isolated from this food in producing amylase enzymes. Based on Gram staining, four bacterial isolates were Gram-positive. The qualitative test of amylase on NA medium with the addition of 1% starch showed four bacteria were able to produce amylase in NaCl (0 to 5%)-containing medium. IG66 isolate was the most potential isolate because it had the highest enzyme activity in a medium with 5% NaCl concentration, which was 0.095 U/ml. The amylase activity was produced maximum at the 8th hour, which is the early stationary phase. Its maximum activity in the 5% NaCl-containing medium was at the 10th hour. In addition, amylase produced by IG66 isolate reached optimum activity at a temperature of 50°C and pH 7. This study concluded that IG66 isolate was the most potential halotolerant isolate that could be developed as an amylase-producing agent.

Elucidation of chemical compounds in different extracts of two Lavandula taxa and their biological potentials: Walking with versatile agents on the road from nature to functional applications

Due to their health-promoting and nutraceutical properties, lavenders are frequently employed in the food and pharmaceutical industries. Here, we focused on investigate the chemical profile of hexane, MeOH, and water extracts of leaf, flower, and root of L. pedunculata and L. stoechas and to assess their antioxidant, enzyme inhibitory, and antibacterial properties. The highest total polyphenolic and flavonoids contents were recorded from the water and MeOH extracts of the leaf and flower of L. stoechas, respectively. Our HPLC/MS/MS analysis detected over 90 secondary metabolites, consisting of both known and novel terpenoids, polyphenols, flavonoids, and their derivative. Water leaf extract of L. stoechas displayed significantly (p < 0.05) the highest antiradical, Cu2+ and Fe3+ reducing capacity while hexane extract of the leaf and MeOH extract of the flower of L. pedunculata revealed the best metal chelating ability and total antioxidant activity respectively. The hexane extract of the leaf of L. pedunculata exerted the highest acetylcholinesterase and tyrosinase inhibition activity, whereas the hexane extracts from L. stoechas leaf and L. pedunculata root recorded the highest ability to inhibit the butyrylcholinesterase and ⍺-amylase enzymes respectively. The water extracts of the leaf of the two species, besides the hexane extract of the leaf of L. pedunculata exerted the best inhibition effect against the α-glucosidase. The sensitivities of Gram-positive and Gram-negative bacteria species against different extracts at two different concentrations were tested based on agar well diffusion assay. According to the result, we found that the n-hexane extract of L. stoechas-flowers showed the highest antibacterial activity. In conclusion, the results suggest that both Lavandula species have promising potential as sources of bioactive agents for various industrial applications.

Synthesis, Spectral Characterization, Thermal Investigation, Computational Studies, Molecular Docking, and In Vitro Biological Activities of a New Schiff Base Derived from 2-Chloro Benzaldehyde and 3,3'-Dimethyl-[1,1'-biphenyl]-4,4'-diamine.

The current research involves the synthesis of a new Schiff base through the reaction between 2-chlorobenzaldehyde and 3,3'-dimethyl-[1,1'-biphenyl]-4,4'-diamine by using a natural acid catalyst and a synthesized compound physicochemically characterized by X-ray diffraction, Fourier transform infrared spectroscopy, 1H- and 13C-nuclear magnetic resonance, and liquid chromatography-mass spectrometry. Thermal studies were conducted using thermogravimetric, differential thermal analysis, and differential thermogravimetric curves. These curves were obtained in an inert nitrogen environment from ambient temperature to 1263 K using heating rates of 10, 15, and 20 K·min-1. Using thermocurve data, model-free isoconversional techniques such as Kissinger-Akahira-Sunose, Flynn-Wall-Ozawa, and Friedman are used to determine kinetic parameters. These parameters include activation energy, phonon frequency factor, activation enthalpy, activation entropy, and Gibb's free energy change. All of the results have been thoroughly investigated. The molecule's anti-inflammatory and antidiabetic properties were also examined. To learn more about the potential of the Schiff base and how successfully it can suppress the amylase enzyme, a molecular docking experiment was also conducted. For in silico research, the Swiss Absorption, Distribution, Metabolism, Excretion, and Toxicity algorithms were used to calculate the theoretical pharmacokinetic properties, oral bioavailability, toxic effects, and biological activities of the synthesized molecule. Moreover, the cytotoxicity tests against a human lung cancer cell line (A549) using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay demonstrated that the synthesized Schiff base exhibited significant anticancer properties.

Some morpholine tethered novel aurones: Design, synthesis, biological, kinetic and molecular docking studies

Enzymes are the biological macromolecules that have emerged as an important drug target as their upregulation/imbalance leads to various pathological conditions, such as inflammation, parasitic infection, Alzheimer’s, cancer, and many others. Here, we designed and synthesized some morpholine tethered novel aurones and evaluated them as potential inhibitors for CTSB, α-amylase, lipase and activator for trypsin. All the newly synthesized compounds were fully characterized by various spectroscopic techniques (1H NMR, 13C NMR, HRMS) and the Z-configuration to them was assigned based on single crystal XRD data and 1H NMR chemical shift values. Further, the hybrids were evaluated for their intracellular (cathepsin B) and extracellular (trypsin, lipase, amylase) enzyme inhibition potencies. The in-vitro inhibition screening against cathepsin B revealed that most of the synthesized compounds are good competitive inhibitors (% inhibition = 22.91–75.04), with 6q (% inhibition = 75.04) and 6r (% inhibition = 71.13) as the eminent inhibitors of the series. At the same time, they exhibited weak to moderate inhibition towards amylase (% inhibition = 7.22–22.48) and lipase (% inhibition = 16.29–54.83). A significant trypsin activation (% activation = 107.42–196.47) was observed even at the micromolar concentration of the compounds. Furthermore, the drug-modeling studies showed a good correlation between the in-vitro experimental results and the calculated binding affinity of the screened compounds with all the tested enzymes. These findings are expected to provide a new lead in drug development for different pathological disorders wherever these enzymes are involved.

Antioxidant and Enzyme Inhibitory Activities of Rhoifolin Flavonoid: In Vitro and in Silico Studies.

Rhoifolin (apigenin-7-O-β-neohesperidoside) belongs to the class of flavonoids and was reported to exhibit anti-inflammatory, cytotoxic, antidiabetic, hepatoprotective, and cardioprotective activities. The current study presents the in-vitro evaluation of the antioxidative effects of rhoifolin by many assays, namely DPPH, CUPRAC, ABTS, phosphomolybdenum, and FRAP. Enzyme inhibitory potential was also evaluated for acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, amylase, and glucosidase enzymes. While results revealed weak antioxidant activities for rhoifolin, the compound demonstrated some promising enzyme inhibitory effects against BChE (4.03 mg GALAE/g) and tyrosinase (7.44 mg KAE/g) but was not active on AChE. Regarding anti-diabetic enzymes, the compound was active on amylase but did not show any inhibition effect on glucosidase. In-silico molecular docking study was performed for rhoifolin on the active site of NADPH oxidase, BChE, and amylase enzymes to verify the observed enzyme inhibitory effect. Good binding affinities were observed for rhoifolin on all the docked enzymes, revealing numerous hydrogen bonds, carbon-hydrogen, van der Waals interactions. This is the first study to evaluate the enzyme inhibition potential of rhoifolin. We concluded that the increase in the degree of glycosylation might decrease the antioxidant abilities of flavonoids and that rhoifolin had moderate enzyme inhibition abilities to be investigated in future studies.