{"title":"The Stability Improvement of <i>Aspergillus fumigatus α</i>-Amylase by Immobilization onto Chitin-Bentonite Hybrid.","authors":"Ezra Rheinsky Tiarsa, Yandri Yandri, Tati Suhartati, Heri Satria, Bambang Irawan, Sutopo Hadi","doi":"10.1155/2022/5692438","DOIUrl":"https://doi.org/10.1155/2022/5692438","url":null,"abstract":"<p><p>Enzyme immobilization is a powerful method to improve the stability, reuse, and enzymatic properties of enzymes. The immobilization of the <i>α</i>-amylase enzyme from <i>Aspergillus fumigatus</i> on a chitin-bentonite (CB) hybrid has been studied to improve its stability. Therefore, this study aims to obtain the higher stability of <i>α</i>-amylase enzyme to reduce industrial costs. The procedures were performed as follows: production, isolation, partial purification, immobilization, and characterization of the free and immobilized enzymes. The CB hybrid was synthesized by bentonite, chitin, and glutaraldehyde as a cross-linker. The free enzyme was immobilized onto CB hybrid using 0.1 M phosphate buffer pH 7.5. The free and immobilized enzymes were characterized by optimum temperature, Michaelis constant (<i>K</i> <sub>M</sub>), maximum velocity (<i>V</i> <sub>max</sub>), thermal inactivation rate constant (<i>k</i> <sub><i>i</i></sub> ), half-life (<i>t</i> <sub>1/2</sub>), and transformation of free energy because of denaturation (Δ<i>G</i> <sub><i>i</i></sub> ). The free enzyme has optimum temperature of 55°C, <i>K</i> <sub><i>M</i></sub> = 3.04 mg mL<sup>-1</sup> substrate, <i>V</i> <sub>max</sub>=10.90 <i>μ</i>molemL<sup>-1</sup>min<sup>-1</sup>, <i>k</i> <sub><i>i</i></sub> = 0.0171 min<sup>-1</sup>, <i>t</i> <sub>1/2</sub> = 40.53 min, and Δ<i>G</i> <sub><i>i</i></sub> = 104.47 kJ mole<sup>-1</sup>. Meanwhile, the immobilized enzyme has optimum temperature of 60°C, <i>K</i> <sub><i>M</i></sub> = 11.57 mg mL<sup>-1</sup> substrate, <i>V</i> <sub>max</sub>=3.37 <i>μ</i>molemL<sup>-1</sup>min<sup>-1</sup>, <i>k</i> <sub><i>i</i></sub> = 0.0045 min<sup>-1</sup>, <i>t</i> <sub>1/2</sub> = 154.00 min, and Δ<i>G</i> <sub><i>i</i></sub> = 108.17 kJ mole<sup>-1</sup>. After sixth cycle of reuse, the residual activity of the immobilized enzyme was 38%. The improvement in the stability of <i>α</i>-amylase immobilized on the CB hybrid based on the increase in half-life was four times of the free enzyme.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":" ","pages":"5692438"},"PeriodicalIF":3.0,"publicationDate":"2022-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8938080/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40317380","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Y. F. Djohan, M. Camara-Cissé, G. Fouret, B. Bonafos, B. Jover, J. Cristol, C. Coudray, C. Feillet-Coudray, É. Badia
{"title":"Diets Rich in Olive Oil, Palm Oil, or Lard Alter Mitochondrial Biogenesis and Mitochondrial Membrane Composition in Rat Liver","authors":"Y. F. Djohan, M. Camara-Cissé, G. Fouret, B. Bonafos, B. Jover, J. Cristol, C. Coudray, C. Feillet-Coudray, É. Badia","doi":"10.1155/2022/9394356","DOIUrl":"https://doi.org/10.1155/2022/9394356","url":null,"abstract":"Palm oil (crude or refined) and lard are rich in SFA, while olive oil is rich in polyunsaturated fatty acids. SFA are considered harmful to health, while polyunsaturated fatty acids are beneficial to health. The aim of this study was to determine the effect of diets rich in crude PO, refined PO, OO, or lard on the mitochondrial membrane, the activity of mitochondrial respiratory chain complexes, and mitochondrial biogenesis. This was an experimental study in male Wistar rats fed a diet containing 30% of each oil. Rats had free access to food and water. After being fed for 12 weeks, animals were sacrificed and liver mitochondria were collected. This collection was used to determine membrane potential and ROS production, membrane phospholipid and fatty acid composition, citrate synthase activity and respiratory chain complex, cardiolipin synthase protein expression, and expression of selected genes involved in mitochondrial biogenesis. We found that diets rich in olive oil, palm oil, or lard altered mitochondrial biogenesis by significantly decreasing Pgc1α gene expression and altered the fatty acid composition of rat liver mitochondrial membrane PL.","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2022-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48828082","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Antidiarrheal and Antisecretory Effect of 80% Hydromethanolic Leaf Extract of <i>Moringa stenopetala</i> Baker f. in Mice.","authors":"Menbere Getaneh Woldeyohannes, Gelila Tamyalew Eshete, Alfoalem Araba Abiye, Abebe Ejigu Hailu, Solomon Assefa Huluka, Wondmagegn Tamiru Tadesse","doi":"10.1155/2022/5768805","DOIUrl":"https://doi.org/10.1155/2022/5768805","url":null,"abstract":"<p><strong>Introduction: </strong>In Ethiopia, different medicinal plants have been claimed and used to treat diarrheal diseases. However, these claimed effects for most medicinal plants have not been scientifically verified. One of such plants in Ethiopian folkloric medicine is <i>Moringa stenopetala,</i> which is usually consumed as a vegetable in southern Ethiopia. Thus, this study aimed to evaluate the antidiarrheal and antisecretory effects of 80% methanolic leaf extract of <i>Moringa stenopetala</i> in different mice models.</p><p><strong>Method: </strong>Using Swiss albino mice, castor oil-induced diarrhea, charcoal meal-based gastrointestinal motility, and castor oil-induced secretion models were employed to assess antidiarrheal activity. In all of the test models, animals were randomly assigned into five groups consisting of six animals in each group. Group I received 0.5 ml of the vehicle (2% tween-80), while group II was treated with standard drug (3 mg/kg loperamide) in the respective models, whereas groups III to V received 150, 300, and 450 mg/kg of the methanolic leaf extracts of <i>Moringa stenopetala</i>. Onset, frequency, consistency, and weight of stool (diarrhea) were recorded, and different parameters and percentage proportions were calculated. Data were analyzed using one-way ANOVA followed by Tukey's test, and <i>p</i> < 0.05 was considered statistically significant at 95% confidence of interval.</p><p><strong>Result: </strong>In the castor oil-induced diarrheal model, the percentage inhibition of diarrhea was 48.5, 58.6, and 60% for the respective doses of 150, 300, and 450 mg/kg of the extract. And, the extract showed a 36.8, 54.4, and 55.9% reduction of peristalsis in charcoal meal-based gastrointestinal motility test compared to the negative control group. Moreover, in the antisecretory assay, the 150, 300, and 450 mg/kg doses of MEMS inhibited fluid contents of the stool by 11.5, 54.54, and 61.82%, respectively, relative to the vehicle-treated group.</p><p><strong>Conclusion: </strong>The findings revealed that the 80% methanolic leaf extract of <i>Moringa stenopetala</i> extract has shown antidiarrheal activity.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":" ","pages":"5768805"},"PeriodicalIF":3.0,"publicationDate":"2022-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8818423/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39609482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"The Stability Improvement of <i>α</i>-Amylase Enzyme from <i>Aspergillus fumigatus</i> by Immobilization on a Bentonite Matrix.","authors":"Yandri Yandri, Ezra Rheinsky Tiarsa, Tati Suhartati, Heri Satria, Bambang Irawan, Sutopo Hadi","doi":"10.1155/2022/3797629","DOIUrl":"https://doi.org/10.1155/2022/3797629","url":null,"abstract":"<p><p>The stability of the <i>α</i>-amylase enzyme has been improved from <i>Aspergillus fumigatus</i> using the immobilization method on a bentonite matrix. Therefore, this study aims to obtain the higher stability of <i>α</i>-amylase enzyme from <i>A. fumigatus</i>; hence, it is used repeatedly to reduce industrial costs. The procedures involved enzyme production, isolation, partial purification, immobilization, and characterization. Furthermore, the soluble enzyme was immobilized using 0.1 M phosphate buffer of pH 7.5 on a bentonite matrix, after which it was characterized with the following parameters such as optimum temperature, Michaelis constant (<i>K</i> <sub><i>M</i></sub> ), maximum velocity (<i>V</i> <sub>max</sub>), thermal inactivation rate constant (<i>k</i> <sub>i</sub>), half-life (<i>t</i> <sub>1/2</sub>), and the change of energy due to denaturation (Δ<i>G</i> <sub><i>i</i></sub> ). The results showed that the soluble enzyme has an optimum temperature of 55°C, <i>K</i> <sub><i>M</i></sub> of 3.04 mg mL<sup>-1</sup> substrate, <i>V</i> <sub>max</sub> of 10.90 <i>μ</i>mole mL<sup>-1</sup> min<sup>-1</sup>, <i>k</i> <sub>i</sub> of 0.0171 min<sup>-1</sup>, t<sub>1/2</sub> of 40.53 min, and Δ<i>G</i> <sub><i>i</i></sub> of 104.47 kJ mole<sup>-1</sup>, while the immobilized enzyme has an optimum temperature of 70°C, <i>K</i> <sub><i>M</i></sub> of 8.31 mg mL<sup>-1</sup> substrate, <i>V</i> <sub>max</sub> of 1.44 <i>μ</i>mole mL<sup>-1</sup> min<sup>-1</sup>, <i>k</i> <sub>i</sub> of 0.0060 min<sup>-1</sup>, <i>t</i> <sub>1/2</sub> of 115.50 min, and Δ<i>G</i> <sub><i>i</i></sub> of 107.37 kJ mole<sup>-1</sup>. Considering the results, the immobilized enzyme retained 42% of its residual activity after six reuse cycles. Additionally, the stability improvement of the <i>α</i>-amylase enzyme by immobilization on a bentonite matrix, based on the increase in half-life, was three times greater than the soluble enzyme.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":" ","pages":"3797629"},"PeriodicalIF":3.0,"publicationDate":"2022-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8763562/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39834057","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Denga Nthai, Vuyisile Samuel Thibane, Sechene Stanley Gololo
{"title":"Comparative Study of Abiotic Stress Factors on GC-MS-Detected Phytoconstituents of <i>Aloe greatheadii</i> var: davyana Using Heat Map and Hierarchical Clustering Dendrogram.","authors":"Denga Nthai, Vuyisile Samuel Thibane, Sechene Stanley Gololo","doi":"10.1155/2022/5365024","DOIUrl":"https://doi.org/10.1155/2022/5365024","url":null,"abstract":"<p><p><i>Aloe greatheadii</i> var. davyana or spotted aloe is indigenous to South Africa and widely distributed in the northern provinces. The plant has a vast ethnopharmacological application which is mostly attributed to its phytochemical content. The aim of the study was to examine the effect of abiotic stress factors on the plant's phytochemical content. The phytochemical content of <i>A. greatheadii</i> hexane extracts from four different provinces (Limpopo, Mpumalanga, Gauteng, and North West), harvested from the wild at varied altitudes, rainfall patterns, and soil types, was examined using gas chromatography-mass spectra (GC-MS). The phytochemical content of hexane extracts from the four South African provinces was analysed using heat map analysis and hierarchical clustering dendrogram. The phytochemical content of <i>A. greatheadii</i> hexane extracts was composed of fatty acids, alkanes, benzene, carboxylic acids, ketones, phytosterols, and vitamins. Eicosane, henicosane, and [(2S)-2-[(2R)-4-hexadecanoyloxy-3-hydroxy-5-oxo-2H-furan-2-yl]-2-hydroxyethyl] hexadecanoate were the only compounds detected in all samples from the four provinces. The concentration levels of 2-(((2-ethylhexyl)oxy)carbonyl) benzoic acid, beta-sitosterol, tritetracontane, and ethyl 13-methyltetradecanoate were closely related and expressed a low clustering distance amongst the samples. Variations in soil pH, soil type, and rainfall patterns were detected and differed in the four provinces. The different abiotic stress factors affected the biochemical pathways for the different compounds, with conditions in Gauteng being less favourable for many of the compounds detected. Abiotic stress factors have shown to influence phytochemical biochemical pathways and quantity. <i>Aloe greatheadii</i> plants can be selected based on location seemingly due to the variations that persist in their phytochemical content.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":" ","pages":"5365024"},"PeriodicalIF":3.0,"publicationDate":"2022-01-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8754611/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39939542","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"<i>In Vitro</i> Experimental Assessment of Ethanolic Extract of <i>Moringa oleifera</i> Leaves as an <i>α</i>-Amylase and <i>α</i>-Lipase Inhibitor.","authors":"Adebanke Ogundipe, Babatunde Adetuyi, Franklyn Iheagwam, Keleko Adefoyeke, Joseph Olugbuyiro, Oluseyi Ogunlana, Olubanke Ogunlana","doi":"10.1155/2022/4613109","DOIUrl":"https://doi.org/10.1155/2022/4613109","url":null,"abstract":"<p><strong>Methods: </strong>Phytochemical screening, antioxidant activity, <i>α</i>-amylase, and <i>α</i>-lipase inhibitory assessment were carried out on <i>Moringa oleifera</i> extract.</p><p><strong>Results: </strong>The result of the phytochemical screening revealed the presence of total phenolic, flavonoid, tannin, and alkaloid contents of values 0.070 ± 0.005 mg gallic acid equivalent/g, 0.180 ± 0.020 mg rutin equivalent/g, 0.042 ± 0.001 mg tannic equivalent/g, and 12.17 ± 0.001%, respectively, while the total protein analysis was 0.475 ± 0.001 mg bovine serum albumin equivalent/g. Ferric reducing antioxidant power (FRAP) and total antioxidant capacity (TAC) values were 0.534 ± 0.001 mg gallic acid equivalent/g and 0.022 ± 0.00008 mg rutin equivalent/g, respectively. Diphenyl-2-picrylhydrazyl (DPPH), ABTS (2,2'-azino-bis (ethylbenzothiazoline-6-sulfonic acid)), and nitric oxide (NO) assays showed the extract to have a strong free radical scavenging activity. The 50% inhibitory concentration (IC<sub>50</sub>) values of the lipase and amylase activities of the extract are 1.0877 mg/mL and 0.1802 mg/mL, respectively.</p><p><strong>Conclusion: </strong>However, <i>α</i>-lipase and <i>α</i>-amylase inhibiting activity of <i>M. oleifera</i> could be related to the phytochemicals in the extract. This research validates the ethnobotanical use of <i>M. oleifera</i> leaves as an effective plant-based therapeutic agent for diabetes and obesity.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":"2022 ","pages":"4613109"},"PeriodicalIF":3.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9815922/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10506897","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Physicochemical Characterization of Dembi Reservoir Water for Suitability of Fish Production, Southwest Ethiopia.","authors":"Ephrem Chekole, Henok Kassa, Abebe Aschalew, Lalit Ingale","doi":"10.1155/2022/1343044","DOIUrl":"https://doi.org/10.1155/2022/1343044","url":null,"abstract":"<p><p>Reservoir water physicochemical characteristics provide important information about water suitability for fish production. Accordingly, the study aimed to characterize the physicochemical characteristics of Dembi reservoir water for sustainable fish production. The study was conducted in Dembi reservoir during the dry season. Water samples were collected in triplicate from selected 10 sampling sites of the reservoir water using manually prepared water sampler made from polyvinyl chloride (PVC) tube. The depth integrated sampling technique was employed to take water samples for all physicochemical characteristics analysis. From the selected 14 physicochemical characteristics, four (temperature, electrical conductivity, pH, and dissolved oxygen) were tested onsite using a multisystem HQ4d electronic meter (probe), whereas the rest 10 water quality characteristics were tested in the laboratory. The result showed that the current average depth of the dam was 5.6 ± 1.61 m. The overall mean values of the water quality characteristics at different sites of the reservoir were as follows: turbidity (26.4 ± 0.44 FTU), total hardness (22.2 ± 0.51 mgL<sup>-1</sup>), NO<sub>3</sub> (5.4 ± 0.48 mgL<sup>-1</sup>), NO<sub>2</sub> (0.3 ± 0.11 mgL<sup>-1</sup>), NH<sub>4</sub> (2.1 ± 0.06 mgL<sup>-1</sup>), PO<sub>4</sub> <sup>-3</sup> (1.7 ± 0.27 mgL<sup>-1</sup>), total alkalinity (52.5 ± 0.91 mgL<sup>-1</sup>), and BOD<sub>5</sub> (2.7 ± 0.24 mgL<sup>-1</sup>). There was a significant difference (<i>p</i> < 0.05) in all physicochemical characteristics among 10 sampling sites of the reservoir water. The recorded values of all physicochemical characteristics, except NO<sub>2</sub>, NH<sub>4</sub>, and PO<sub>4</sub> <sup>-3</sup>, were found within the recommended standard limit for fish production. The change in reservoir water depth and increase in nutrients shows the presence of sediment siltation and nutrient enrichment. Therefore, proper watershed management practices and waste management should be carried out for sustainable water quality maintenance and fish production.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":"2022 ","pages":"1343044"},"PeriodicalIF":3.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9792236/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10453352","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Recent Progress in Nanobiosensors for Precise Detection of Blood Glucose Level.","authors":"Haniye Khosravi Ardakani, Mitra Gerami, Mostafa Chashmpoosh, Navid Omidifar, Ahmad Gholami","doi":"10.1155/2022/2964705","DOIUrl":"https://doi.org/10.1155/2022/2964705","url":null,"abstract":"<p><p>Diabetes mellitus (DM) follows a series of metabolic diseases categorized by high blood sugar levels. Owing to the increasing diabetes disease in the world, early diagnosis of this disease is critical. New methods such as nanotechnology have made significant progress in many areas of medical science and physiology. Nanobiosensors are very sensible and can identify single virus particles or even low concentrations of a material that can be inherently harmful. One of the main factors for developing glucose sensors in the body is the diagnosis of hypoglycemia in individuals with insulin-dependent diabetes. Therefore, this study aimed to evaluate the most up-to-date and fastest glucose detection method by nanosensors and, as a result, faster and better treatment in medical sciences. In this review, we try to explore new ways to control blood glucose levels and treat diabetes. We begin with a definition of biosensors and their classification and basis, and then we examine the latest biosensors in glucose detection and new biosensors applications, including the artificial pancreas and updating quantum graphene data.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":"2022 ","pages":"2964705"},"PeriodicalIF":3.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8786499/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10256366","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Synthesis, DFT Analysis, and Evaluation of Antibacterial and Antioxidant Activities of Sulfathiazole Derivatives Combined with <i>In Silico</i> Molecular Docking and ADMET Predictions.","authors":"Yoseph Samuel, Ankita Garg, Endale Mulugeta","doi":"10.1155/2021/7534561","DOIUrl":"https://doi.org/10.1155/2021/7534561","url":null,"abstract":"<p><p>Synthetic modifications of sulfathiazole derivatives become an interesting approach to enhance their biological properties in line with their applications. As a result, sulfathiazole derivatives become a good candidate and potential class of organic compounds to play an important role towards medicinal chemistry. In present study, one thiazole derivative and two new sulfathiazole derivatives are synthesized with 94% and 72-81% yields, respectively. Furthermore, the synthesized compounds were evaluated for their <i>in vitro</i> antibacterial activity against two Gram-negative (<i>E. coli</i> and <i>P. aeruginosa</i>) and two Gram-positive bacterial strains (<i>S. pyogenes</i> and <i>S. aureus</i>) by disk diffusion method. Among synthesized compounds, compound <b>11a</b> showed potent inhibitory activity against Gram-negative, <i>E. coli</i> with 11.6 ± 0.283 mm zone of inhibition compared to standard drug sulfamethoxazole (15.7 ± 0.707 mm) at 50 mg/mL. The radical scavenging activities of these compounds were evaluated using DPPH radical assay, and compound <b>11a</b> showed the strongest activity with IC<sub>50</sub> values of 1.655 <i>μ</i>g/mL. The synthesized compounds were evaluated for their <i>in silico</i> molecular docking analysis using <i>S. aureus</i> gyrase (PDB ID: 2XCT) and human myeloperoxidase (PDB ID: 1DNU) and were found to have minimum binding energy ranging from -7.8 to -10.0 kcal/mol with 2XCT and -7.5 to -9.7 with 1DNU. Compound <b>11a</b> showed very good binding score -9.7 kcal/mol with both of the proteins and had promising alignment with <i>in vitro</i> results. Compound 11b also showed high binding scores with both proteins. Drug likeness and ADMET of synthesized compounds were predicted. The DFT analysis of synthesized compounds was performed using Gaussian 09 and visualized through Gauss view 6.0. The structural coordinates of the lead compounds were optimized using B3LYP/6-31 G (d,p) level basis set without any symmetrical constraints. Studies revealed that all the synthesized compounds might be candidates for further antibacterial and antioxidant studies.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":"2021 ","pages":"7534561"},"PeriodicalIF":3.0,"publicationDate":"2021-12-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8692053/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39872166","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sara Haida, Kaltoum Bakkouche, Abdelaziz Ramadane Kribii, Abderahim Kribii
{"title":"Chemical Composition of Essential Oil, Phenolic Compounds Content, and Antioxidant Activity of <i>Cistus monspeliensis</i> from Northern Morocco.","authors":"Sara Haida, Kaltoum Bakkouche, Abdelaziz Ramadane Kribii, Abderahim Kribii","doi":"10.1155/2021/6669877","DOIUrl":"https://doi.org/10.1155/2021/6669877","url":null,"abstract":"<p><p>Currently, oxidative stress is one of the major problems that threatens human health. It is at the root of many diseases such as cancer. Despite the enormous efforts provided to combat this scourge, oxidative stress is still relevant and hence comes the need for research of new remedies especially from natural origin. For this purpose, the study of the antioxidant activity of extracts of <i>Cistus monspeliensis</i> from Morocco is a principal research objective. The phenolic extracts were obtained by maceration of the plant in a water/acetone mixture and then separated by liquid/liquid extraction with solvents of increasing polarity. The first phytochemical tests carried out on these extracts showed the existence of different families of phenolic compounds, such as flavonoids, tannins, and others. Assays for total polyphenols, flavonoids, hydrolysable, and condensed tannins were carried out by known colorimetric methods. The results of these assays have shown that the studied extracts are rich in phenolic compounds present in the plant in the form of flavonoids (69.81 ± 0.22 mg EQ/g DM), hydrolysable tannins (61.86 ± 0.89 mg ETA/g DM), and condensed tannins (70.05 ± 1.61 mg EC/g DM). The evaluation of the antioxidant activity is carried out by two different methods: the DPPH test (2,2-DiPhenyl-1-Picryl-Hydrazyl) and the FRAP test (Ferric Reducing Antioxidant Power). The results obtained show that the extracts of <i>Cistus monspeliensis</i> are active and have interesting antioxidant powers. In particular, the water/acetone (WAE) (IC<sub>50</sub> = 0.079 mg/mL) and butanolic (BUE) (IC<sub>0.5</sub> = 0.099 mg/mL) extracts are the most active with values comparable to that of ascorbic acid. The interesting results obtained in this study clearly show that <i>Cistus monspeliensis</i> originating from Morocco can be considered as a source of natural antioxidants. Therefore, the extracts of this plant deserve to be tested in the medicinal field, against cancer and cardiovascular diseases, and in food field as an additive and preservative.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":"2021 ","pages":"6669877"},"PeriodicalIF":3.0,"publicationDate":"2021-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8670979/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39733048","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}