Publications by authors named "Bushra Mirza"

100 Publications

Inducible expression of human papillomavirus-16 L1 capsomeres in the plastomes of Nicotiana tabacum: Transplastomic plants develop normal flowers and pollen.

Biotechnol Appl Biochem 2021 Mar 2. Epub 2021 Mar 2.

Department of Biochemistry, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.

Human papillomavirus type-16 (HPV-16) is the major HPV type involved in causing cervical cancer among women. The disease burden is high in developing and underdeveloped countries. Previously, the constitutive expression of HPV-16 L1 protein led to male sterility in transplastomic tobacco plants. Here, the HPV-16 L1 gene was expressed in chloroplasts of Nicotiana tabacum under the control of an ethanol-inducible promoter, trans-activated by nucleus-derived signal peptide. Plants containing nuclear component were transformed with transformation vector pEXP-T7-L1 by biolistic gun. The transformation and homoplasmic status of transformed plants was verified by polymerase chain reaction and Southern blotting, respectively. Protein was induced by spraying 5% ethanol for 7 consecutive days. The correct folding of L1 protein was confirmed by antigen-capture ELISA using a conformation-specific antibody. The L1 protein accumulated up to 3 μg/g of fresh plant material. The L1 protein was further purified using affinity chromatography. All transplastomic plants developed normal flowers and produced viable seeds upon self-pollination. Pollens also showed completely normal structure under light microscope and scanning electron microscopy. These data confirm the use of the inducible expression as plant-safe approach for expressing transgenes in plants, especially those genes that cause detrimental effects on plant growth and morphology.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1002/bab.2136DOI Listing
March 2021

Novel copper complexes of metronidazole and metronidazole benzoate: synthesis, characterization, biological and computational studies.

J Biomol Struct Dyn 2021 Jan 11:1-16. Epub 2021 Jan 11.

Department of Chemistry, School of Natural Sciences, National University of Sciences and Technology (NUST), Islamabad, Pakistan.

Synthesis and characterization of novel copper complexes of metronidazole benzoate (MTZ Benz), metronidazole (MTZ) in the presence of another ligand; dichloroacetic acid (DCA) were compared and reported in the present work. Different bacterial and fungus strains were ascertained to evaluate the biological potency of the synthesized complexes, that is, and yeast strain Agar diffusion method was employed to investigate antibacterial activities of the synthesized metal complexes and the tested parent ligands. α-Amylase and α-glucosidase inhibition studies of the synthesized complexes were also carried out. The antibacterial potential and α-amylase and α-glucosidase inhibition studies of complexes were further investigated by molecular docking studies, which supported the experimental results. Significant α-amylase and α-glucosidase inhibition activities were shown by the synthesized complexes. S-1 and S-5 were found to be most inhibitors of α-amylase and α-glucosidase having IC 42.50, 44.80 and 4.52 µg/mL, 4.80 µg/mL, respectively. The newly synthesized copper complexes showed overall better biological activities compared to each parent ligands used. Communicated by Ramaswamy H. Sarma.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1080/07391102.2020.1871072DOI Listing
January 2021

Assessing the biological potential of new symmetrical ferrocene based bisthiourea analogues.

Bioorg Chem 2021 Jan 27;106:104180. Epub 2020 Aug 27.

Coordination Chemistry Laboratory, Department of Chemistry, Quaid-i-Azam University, (45320) Islamabad, Pakistan. Electronic address:

In the present work synthesis and characterization of five new bisferrocenyl bisthiourea analogues (G, S, G, G and T) is reported. UV-Visible and electrochemical studies were performed in order to have optical (absorption maximum, Molar absorption coefficient and optical band gap) and electrochemical parameters (Oxidation/reduction potentials and nature of the electrochemical process) of the compounds. In vitro various biological studies such as antibacterial, antifungal, anti-oxidant and antidiabetic activities were carried out to have comparative overview of the phermacochemical strength of the newly synthesized compounds. Similarly, theoretical analysis was accomplished utilizing density functional theory calculations. DFT/B3LYP (6-31G d, p) technique was used. With a view to explore the structure activity relationship (SAR) of the compounds theoretical docking analysis (against α-amylase, α-glucosidase) was also performed to have pictorial view and understanding of the actual interactions responsible for the activity. S displayed best antibacterial activity. Similarly, Antifungal and antidiabetic activities showed G as a best candidate, whereas T proved to be the best antioxidant agent.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bioorg.2020.104180DOI Listing
January 2021

Potential Nutraceutical Benefits of In Vivo Grown Saffron (Crocus sativus L.) As Analgesic, Anti-inflammatory, Anticoagulant, and Antidepressant in Mice.

Plants (Basel) 2020 Oct 22;9(11). Epub 2020 Oct 22.

Department of Biology, University College Turabah, Taif University, Taif 21995, Saudi Arabia.

Crocus sativus, a medicinally important herbaceous plant, has been traditionally used to cure coughs, colds, insomnia, cramps, asthma, and pain. Moreover, the therapeutic applications of saffron include its immunomodulatory and anticancer properties. The current experimental analysis was performed to explore the potential nutraceutical efficacy of corm, leaf, petal, and stigma of saffron ethanolic extracts as analgesic, anti-inflammatory, anticoagulant, and antidepressant using hot plate, carrageenan-induced paw edema, capillary tube and forced swim test, respectively in mice. The results indicated that among all the extracts, stigma ethanolic extract (SEE) represented maximum latency activity (72.85%) and edema inhibition (77.33%) followed by petal ethanolic extract (PEE) with latency activity and edema inhibition of 64.06 and 70.50%, respectively. Corm ethanolic extract (CEE) and leaf ethanolic extract (LEE) displayed mild analgesic activity of 22.40% and 29.07%, respectively. Additionally, LEE (53.29%) and CEE (47.47%) exhibited mild to moderate response against inflammation. The coagulation time of SEE (101.66 s) was almost equivalent to the standard drug, aspirin (101.66 s), suggesting a strong anticoagulant effect followed by PEE (86.5 s). LEE (66.83 s) represented moderate inhibitory effect on coagulation activity while CEE (42.83 s) showed neutral effect. Additionally, PEE and SEE also expressed itself as potential antidepressants with immobility time ≤76.66 s, while CEE (96.50 s) and LEE (106.83 s) indicated moderate to mild antidepressant efficacy. Based on the in vivo activities, saffron extract, particularly SEE and PEE, can be used as a potential nutraceutical and therapeutic agent due to its significant pharmacological activities.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/plants9111414DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7690613PMC
October 2020

Evolutionary History of Alzheimer Disease-Causing Protein Family Presenilins with Pathological Implications.

J Mol Evol 2020 11 1;88(8-9):674-688. Epub 2020 Oct 1.

Department of Animal Sciences, Quaid-I-Azam University, Islamabad, 453 20, Pakistan.

Presenilin proteins make the catalytic component of γ-secretase, a multiprotein transmembrane protease, and are type II transmembrane proteins. Amyloid protein, Notch, and beta catenin are among more than 90 substrates of Presenilins. Mutations in Presenilins lead to defects in proteolytic cleavage of its substrate resulting in some of the most devastating pathological conditions including Alzheimer disease (AD), developmental disorders, and cancer. In addition to catalytic roles, Presenilin protein is also shown to be involved in many non-catalytic roles, i.e., calcium homeostasis, regulation of autophagy, and protein trafficking, etc. These proteolytic proteins are highly conserved and are present in almost all the major eukaryotic groups. Studies, performed on a wide variety of organisms ranging from human to unicellular dictyostelium, have shown the important catalytic and non-catalytic roles of Presenilins. In this study, we infer the evolutionary patterns and history of Presenilins as well as of other γ-secretase proteins. We show that Presenilins are the most ancient of the γ-secretase proteins and that Presenilins may have their origin in the last common ancestor (LCA) of Eukaryotes. We also demonstrate that Presenilin proteins generally lack diversifying selection during the course of their evolution. Through evolutionary trace analysis, we show that Presenilin protein sites that undergo mutations in Familial Alzheimer disease, are highly conserved in metazoans. Finally, we discuss the evolutionary, physiological, and pathological implications of our findings and propose that the evolutionary profile of Presenilins supports the loss of function hypothesis of AD pathogenesis.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1007/s00239-020-09966-wDOI Listing
November 2020

Assessment of antidiabetic potential and phytochemical profiling of Rhazya stricta root extracts.

BMC Complement Med Ther 2020 Sep 29;20(1):293. Epub 2020 Sep 29.

KTH Royal Institute of Technology, School of Chemical Science and Engineering, SE-100 44, Stockholm, Sweden.

Background: Diabetes mellitus is a chronic disease characterized by hyperglycemia that may occur due to genetic, environmental or lifestyle factors. Natural remedies have been used to treat diabetes since long and many antidiabetic compounds of varied efficacies have been isolated from medicinal plants. Rhazya stricta has been used for decades for the treatment of diabetes mellitus and associated ailments. Considering the folkloric use of R. stricta against diabetes, it was aimed to investigate the effectiveness of its root extracts against diabetes through in vitro assays and in vivo studies using animal model along with phytochemical profiling through GCMS.

Methods: Various fractions of Rhazya stricta obtained through column chromatography were evaluated for a variety of assays including α-glucosidase, Dipeptidyl peptidase-IV (DPP-IV), β-secretase and Glucagon-like peptide-1 (GLP-1) secretion studies. For the in vivo studies the alloxan-induced diabetic mice were treated with root extracts and blood glucose levels, HbA1C, and other biochemical markers along with the histological study of the liver were done. The phytochemical identification was performed using an Agilent 7890B GC coupled to a 7010 Triple Quadrupole (MS/MS) system. GraphPad Prism software version 5.01 was used for statistical analysis.

Results: Majority of the extract fractions showed excellent results against diabetes by inhibiting enzymes DPP-IV (Up to 61%) and β-secretase (Up to 83%) with IC 979 μg/ml and 169 μg/ml respectively with increase in the GLP1 secretion. The results of in vivo studies indicated a marked reduction in blood glucose and HbA1c levels along with positive effects on other parameters like lipid profile, liver functions and renal functions of extract-treated mice as compared to control. The histological examination of the liver demonstrated hepatoprotective effects against diabetes led changes and various classes of phytochemicals were also identified through GCMS in different fractions.

Conclusion: The results revealed strong antidiabetic activity of R. stricta root with the potential to protect body organs against diabetic changes. Moreover, a variety of phytochemicals has also been identified through GCMS that might be responsible for the antidiabetic potential of Rhazya stricta root.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1186/s12906-020-03035-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7523044PMC
September 2020

Plastid genomics of (Solanaceae): insights into molecular evolution, positive selection and the origin of the maternal genome of Aztec tobacco ().

PeerJ 2020 23;8:e9552. Epub 2020 Jul 23.

Department of Biochemistry, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.

Species of the genus (Solanaceae), commonly referred to as tobacco plants, are often cultivated as non-food crops and garden ornamentals. In addition to the worldwide production of tobacco leaves, they are also used as evolutionary model systems due to their complex development history tangled by polyploidy and hybridization. Here, we assembled the plastid genomes of five tobacco species: and . De novo assembled tobacco plastid genomes had the typical quadripartite structure, consisting of a pair of inverted repeat (IR) regions (25,323-25,369 bp each) separated by a large single-copy (LSC) region (86,510-86,716 bp) and a small single-copy (SSC) region (18,441-18,555 bp). Comparative analyses of plastid genomes with currently available Solanaceae genome sequences showed similar GC and gene content, codon usage, simple sequence and oligonucleotide repeats, RNA editing sites, and substitutions. We identified 20 highly polymorphic regions, mostly belonging to intergenic spacer regions (IGS), which could be suitable for the development of robust and cost-effective markers for inferring the phylogeny of the genus and family Solanaceae. Our comparative plastid genome analysis revealed that the maternal parent of the tetraploid was the common ancestor of and , and the later species is more closely related to . Relaxed molecular clock analyses estimated the speciation event between and appeared 0.56 Ma (HPD 0.65-0.46). Biogeographical analysis supported a south-to-north range expansion and diversification for and related species, where and evolved in North/Central Peru, while developed in Southern Peru and separated from which adapted to the Southern coastal climatic regimes. We further inspected selective pressure on protein-coding genes among tobacco species to determine if this adaptation process affected the evolution of plastid genes. These analyses indicate that four genes involved in different plastid functions, including DNA replication (A) and photosynthesis (B, D and ), came under positive selective pressure as a result of specific environmental conditions. Genetic mutations in these genes might have contributed to better survival and superior adaptations during the evolutionary history of tobacco species.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.7717/peerj.9552DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7382938PMC
July 2020

Quinovic acid purified from medicinal plant Fagonia indica mediates anticancer effects via death receptor 5.

Mol Cell Biochem 2020 Nov 30;474(1-2):159-169. Epub 2020 Jul 30.

Department of Pharmacology, State University of New York (SUNY), Upstate Medical University, 750 E Adams St, Syracuse, NY, 13210, USA.

Plants are major source for discovery and development of anticancer drugs. Several plant-based anticancer drugs are currently in clinical use. Fagonia indica is a plant of medicinal value in the South Asian countries. Using mass spectrometry and NMR spectroscopy, several compounds were purified from the F. indica extract. We have used one of the purified compounds quinovic acid (QA) and found that QA strongly suppressed the growth and viability of human breast and lung cancer cells. QA did not inhibit growth and viability of non-tumorigenic breast cells. QA mediated its anticancer effects by inducing cell death. QA-induced cell death was associated with biochemical features of apoptosis such as activation of caspases 3 and 8 as well as PARP cleavage. QA also upregulated mRNA and protein levels of death receptor 5 (DR5). Further investigation revealed that QA did not alter DR5 gene promoter activity, but enhanced DR5 mRNA and protein stabilities. DR5 is one of the major components of the extrinsic pathway of apoptosis. Accordingly, Apo2L/TRAIL, the DR5 ligand, potentiated the anticancer effects of QA. Our results indicate that QA mediates its anticancer effects, at least in part, by engaging DR5-depentent pathway to induce apoptosis. Based on our results, we propose that QA in combination with Apo2L/TRAIL can be further investigated as a novel therapeutic approach for breast and lung cancers.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11010-020-03841-4DOI Listing
November 2020

Artemisinin and its derivatives: a promising cancer therapy.

Mol Biol Rep 2020 Aug 24;47(8):6321-6336. Epub 2020 Jul 24.

Department of Biochemistry, Faculty of Biological Sciences, Quaid-I-Azam University, Islamabad, 45320, Pakistan.

The world is experiencing a cancer epidemic and an increase in the prevalence of the disease. Cancer remains a major killer, accounting for more than half a million deaths annually. There is a wide range of natural products that have the potential to treat this disease. One of these products is artemisinin; a natural product from Artemisia plant. The Nobel Prize for Medicine was awarded in 2015 for the discovery of artemisinin in recognition of the drug's efficacy. Artemisinin produces highly reactive free radicals by the breakdown of two oxygen atoms that kill cancerous cells. These cells sequester iron and accumulate as much as 1000 times in comparison with normal cells. Generally, chemotherapy is toxic to both cancerous cells and normal cells, while no significant cytotoxicity from artemisinin to normal cells has been found in more than 4000 case studies, which makes it far different than conventional chemotherapy. The pleiotropic response of artemisinin in cancer cells is responsible for growth inhibition by multiple ways including inhibition of angiogenesis, apoptosis, cell cycle arrest, disruption of cell migration, and modulation of nuclear receptor responsiveness. It is very encouraging that artemisinin and its derivatives are anticipated to be a novel class of broad-spectrum antitumor agents based on efficacy and safety. This review aims to highlight these achievements and propose potential strategies to develop artemisinin and its derivatives as a new class of cancer therapeutic agents.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11033-020-05669-zDOI Listing
August 2020

Comparative Plastomics of Ashwagandha (, Solanaceae) and Identification of Mutational Hotspots for Barcoding Medicinal Plants.

Plants (Basel) 2020 Jun 15;9(6). Epub 2020 Jun 15.

Department of Biochemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan.

Within the family Solanaceae, is a small genus belonging to the Solanoideae subfamily. Here, we report the de novo assembled chloroplast genome sequences of , and The length of these genomes ranged from 154,162 to 154,364 base pairs (bp). These genomes contained a pair of inverted repeats (IRa and IRb) ranging from 25,029 to 25,071 bp that were separated by a large single-copy (LSC) region of 85,635-85,765 bp and a small single-copy (SSC) region of 18,457-18,469 bp. We analyzed the structural organization, gene content and order, guanine-cytosine content, codon usage, RNA-editing sites, microsatellites, oligonucleotide and tandem repeats, and substitutions of plastomes, which revealed high similarities among the species. Comparative analysis among the species also highlighted 10 divergent hotspots that could potentially be used for molecular marker development, phylogenetic analysis, and species identification. Furthermore, our analyses showed that even three mutational hotspots (4-T, M-E, and 15) were sufficient to discriminate the species included in current study.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/plants9060752DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7355740PMC
June 2020

Assessment of the Antitumor Potential of Umbelliprenin, a Naturally Occurring Sesquiterpene Coumarin.

Biomedicines 2020 May 18;8(5). Epub 2020 May 18.

Department of Science in Korean Medicine, College of Korean Medicine, Kyung Hee University, 24 Kyungheedae-ro, Dongdaemun-gu, Seoul 02447, Korea.

Cancer is one of the greatest causes of mortality worldwide. The prevalence rates of different types of cancer is increasing around the world as well. Limitations in chemotherapy and radiotherapy, owing to multiple side effects including cytotoxic effects of antitumor compounds on normal cells as well as the development of resistance to these treatment options in patients, create a serious threat to successful treatment of cancer. The use of natural compounds to prevent and treat cancers has been found to be quite effective, with fewer adverse effects found in patients. Umbelliprenin (UMB) is a naturally occurring sesquiterpene compound found in species and recently in . Many studies have highlighted the antitumor potential of UMB in different cancer cell lines as well as in animal models. UMB exerts its anticancer actions by regulating extrinsic and intrinsic apoptotic pathways; causing inhibition of the cell cycle at the G0/G1 phase; and attenuating migration and invasion by modulating the Wnt signaling, NF-ĸB, TGFβ, and Fox3 signaling pathways. UMB also affects the key hallmarks of tumor cells by attenuating tumor growth, angiogenesis, and metastasis. This review provides an insight into the role of UMB as a potential antitumor drug for different malignancies and highlights the signaling cascades affected by UMB treatment in diverse tumor cell lines and preclinical models.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/biomedicines8050126DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7277383PMC
May 2020

Engineering electroactive and biocompatible tetra(aniline)-based terpolymers with tunable intrinsic antioxidant properties in vivo.

Mater Sci Eng C Mater Biol Appl 2020 Mar 20;108:110456. Epub 2019 Nov 20.

Department of Women's and Children's Health, Karolinska Institutet and Pediatric Endocrinology Unit, Karolinska University Hospital, SE-171 74 Solna, Sweden. Electronic address:

Under different pathological conditions, high levels of reactive oxygen species (ROS) cause substantial damage to multiple organs. To counter these ROS levels in multiple organs, we have engineered highly potent novel terpolymers. We found that combination of FDA-approved polyethylene glycol, fumaric acid moieties and electroactive tetra(aniline) by varying the content of tetra(aniline) results into a novel drug composition with biologically active and tunable intrinsic antioxidant properties. To test the intrinsic antioxidative properties of these novel terpolymers, we used alloxan to induce diabetes in rats where ROS generation is known to be higher. The systemic administration of terpolymers to the diabetic rats showed strong electroactive antioxidant behavior which not only normalized ROS levels, but also improved the levels of enzymatic antioxidants including superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH). As a proof-of-principle, we here show TANI based novel drug composition of terpolymers with tunable intrinsic antioxidant properties in multiple organs.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.msec.2019.110456DOI Listing
March 2020

Expression of ESAT-6 antigen from Mycobacterium tuberculosis in broccoli: An edible plant.

Biotechnol Appl Biochem 2020 Jan 2;67(1):148-157. Epub 2020 Jan 2.

Department of Biochemistry, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.

Tuberculosis (TB) is one of the major infectious diseases caused by Mycobacterium tuberculosis. The development of an effective and economical vaccine for controlling TB is essential especially for developing countries. Edible plants can serve as biofactories to produce vaccine antigens. In this study, 6 kDa early secretory antigenic target (ESAT-6) of M. tuberculosis was expressed in Brassica oleracea var. italica via Agrobacterium-mediated transformation to facilitate oral delivery of antigen. ESAT-6 gene was cloned using Gateway® cloning strategy. Transformation and presence of transgene was confirmed through PCR. Expression level of transgene was calculated via quantitative real-time PCR (qRT-PCR) and the maximum integrated transgene number was two. Maximum amount of total soluble fraction of ESAT-6 was evaluated by immunoblotting, estimated to accumulate up to 0.5% of total soluble protein. The recombinant ESAT-6 protein was further purified and detected using silver staining and Western blotting. ESAT-6 protein induced humoral immune response in mice immunized orally and subcutaneously. The expression of M. tuberculosis antigen in edible plants could aid in the development of cost-effective and oral delivery of an antigen-based subunit vaccine against TB. To the best our knowledge, it is the first report of expression of a vaccine antigen in broccoli.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1002/bab.1867DOI Listing
January 2020

Inhibition of mouse embryonic stem cell proliferation and induction of differentiation by natural products isolated from Rhazya stricta Decne.

Pak J Pharm Sci 2019 Jul;32(4(Supplementary)):1885-1891

Department of Biochemistry, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.

Embryonic stem cells provide an ideal system to study various therapies for serious human diseases such as juvenile diabetes, neurodegenerative diseases, heart diseases and cancer. Synthetic or natural compounds that affect cell proliferation and/or differentiation of embryonic stem cells are of great value. Focus of the current project was upon the isolation and evaluation of natural components from a medicinal plant; Rhazya stricta on proliferation/ differentiation potential of embryonic stem cells. For this purpose, after a series of fractionation and purification steps, 7 compounds named as RS1-RS7 were isolated from aerial parts of the plant. The effects of these compounds were evaluated on the morphology and rate of cell proliferation of mouse naive embryonic stem cells. Only RS7 inhibited the proliferation of cell and reduced the induction of differentiation of cell. The qPCR analysis confirmed that the expression of the selected pluripotency markers (Oct4, Nanog and Sox2) was down regulated by RS7 treatment as compared to control. Furthermore, upon withdraw of Leukemia inhibitory factor (lif) from medium; effect of RS7 to promote differentiation was enhanced. Through structure elucidation studies, RS7 was found to be ursolic acid. This study first time shows the effect of natural compounds of Rhazya stricta Decne. on mouse embryonic stem cells.
View Article and Find Full Text PDF

Download full-text PDF

Source
July 2019

Optimization of cell suspension culture of transformed and untransformed lettuce for the enhanced production of secondary metabolites and their pharmaceutical evaluation.

3 Biotech 2019 Sep 22;9(9):339. Epub 2019 Aug 22.

2Department of Biochemistry, Quaid-I-Azam University, Islamabad, 45320 Pakistan.

In vitro suspension culture techniques are cost effective for large-scale production of secondary metabolites. In the present study, firstly, suspension cultures of untransformed were prepared using different hormonal combinations and were subjected to different pH, temperature and salt concentrations. Maximum biomass was obtained for suspensions supplemented with 1.5 mg/L BAP and 0.1 mg/L NAA, at pH 5.8, temperature 28 °C and 0 mM NaCl concentration. Using these parameters, suspensions were produced for and -transformed lines of . All the transgenic lines showed prominent increase in fresh weight (FW) and dry weight (DW) with maximum values for 2 line producing 169.8 mg/mL FW and 25.3 mg/mL DW. The exudates of transformed and untransformed plants were tested for the antioxidant activity and in vivo assays on rats. Maximum phenolic content (261 μg/mL) and flavonoid content (637.6 μg/mL) were obtained for 1 transgenic line. Total antioxidant capacity was found maximum (1451.7 μg/mL) for untransformed lettuce, whereas 1 showed maximum total reducing power activity (637.6 μg/mL). In DPPH assay, maximum activity (104.7 μg/mL) was shown by 3 line. In rats analgesic assay, maximum activity (74.9%) was shown by 2. Line 1 showed maximum anti-inflammatory activity (69.2%) and maximum antidepressant activity (minimum immobility time of 55 s). Maximum anticoagulant activity was observed for 2 with maximum clotting time of 130 s. The present study could help in using lettuce suspension culture as platform for the enhanced production of important metabolites.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1007/s13205-019-1870-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6704210PMC
September 2019

Characterization of Withania somnifera chloroplast genome and its comparison with other selected species of Solanaceae.

Genomics 2020 03 27;112(2):1522-1530. Epub 2019 Aug 27.

Department of Biochemistry, Quaid-I-Azam University, 45320 Islamabad, Pakistan. Electronic address:

Withania somnifera (L) Dunal, a wonder herb of family Solanaceae, has multiple medicinal properties. Here, we reported the chloroplast genome sequence of Withania somnifera (154,386 bp) which comprises of a large single copy region (85,688 bp), and a small single copy region (18,464 bp), separated by a pair of large inverted repeats (25,117 bp). The chloroplast genome has 132 genes including 86 protein-coding, 37 tRNAs and 8 rRNAs. Comparison of chloroplast genomes of Withania somnifera with four other Solanaceae species revealed similarities in genomic features, including structure, nucleotide content, codon usage, RNA editing sites, simple sequence repeats (SSRs), oligonucleotide repeats, and tandem repeats. We identified 147 simple sequence repeats in protein-coding, and 229 in non-protein-coding regions. We observed numerous post-transcriptional substitutions of Serine to Leucine, specifically at the second nucleotide position of the codon. Maximum likelihood and maximum parsimony tree reconstructed displayed Withania somnifera a sister taxon of Physalis peruviana.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ygeno.2019.08.024DOI Listing
March 2020

Chloroplast-based inducible expression of ESAT-6 antigen for development of a plant-based vaccine against tuberculosis.

J Biotechnol 2019 Nov 24;305:1-10. Epub 2019 Aug 24.

Department of Biochemistry, Faculty of Biological Sciences, Quaid-i-Azam University, 45320, Islamabad, Pakistan. Electronic address:

Mycobacterium tuberculosis causes tuberculosis in humans. The major disease burden of tuberculosis lies in developing countries. Lack of an effective vaccine for adults is one of the major hurdles for controlling this deadly disease. In the present study, 6 kDa early secretory antigenic target (ESAT-6) of M. tuberculosis was inducibly expressed in chloroplasts of Nicotiana tabacum. The expression of ESAT-6 in chloroplasts was controlled by T7 promoter that was activated by nuclear-generated signal peptide. Tobacco plants, containing nuclear component, were transformed via biolistic bombardment with pEXP-T7-ESAT-6 obtained by Gateway® cloning. Transformation and homoplasmic status of transplastomic plants was confirmed by polymerase chain reaction and Southern blotting. Plants were induced for protein expression by spraying with 5% ethanol for 1 day, 3 days, 7 days and 10 days. ESAT-6 protein was detected by immunoblot analysis and maximum protein was obtained for 10 days induced plants that was estimated to accumulate up to 1.2% of total soluble fraction of protein. Transplastomic plants showed completely normal morphology. Transplastomic and untransformed plants became slightly chlorotic upon prolonged exposure to ethanol until 10 days. Taken together, this data could help in the development of an antigen-based subunit vaccine against tuberculosis.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jbiotec.2019.08.016DOI Listing
November 2019

Chloroplast genome sequences of Artemisia maritima and Artemisia absinthium: Comparative analyses, mutational hotspots in genus Artemisia and phylogeny in family Asteraceae.

Genomics 2020 03 23;112(2):1454-1463. Epub 2019 Aug 23.

Department of Biochemistry, Quaid-i-Azam University, Islamabad, Pakistan. Electronic address:

Artemisia L. is a complex genus of medicinal importance. Publicly available chloroplast genomes of few Artemisia species are insufficient to resolve taxonomic discrepancies at species level. We report chloroplast genome sequences of two further Artemisia species: A. maritima (151,061 bp) and A. absinthium (151,193 bp). Both genomes possess typical quadripartite structure comprising of a large single copy, a small single copy and a pair of long inverted repeats. The two genomes exhibited high similarities in genome sizes, gene synteny, GC content, synonymous and non-synonymous substitutions, codon usage, amino acids frequencies, RNA editing sites, microsatellites, and oligonucleotide repeats. Transition to transversion ratio was <1. Maximum likelihood tree showed Artemisia a monophyletic genus, sister to genus Chrysanthemum. We also identified 20 highly polymorphic regions including rpoC2-rps2, trnR-UCU-trnG-UCC, rps18-rpl20, and trnL-UAG-rpl32 that could be used to develop authentic and cost-effective markers to resolve taxonomic discrepancies and infer phylogenetic relationships among Artemisia species.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ygeno.2019.08.016DOI Listing
March 2020

Disease Status of Afghan Refugees and Migrants in Pakistan.

Front Public Health 2019 3;7:185. Epub 2019 Jul 3.

Department of Biochemistry, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.

World is facing the largest refugee crisis of its time due to continuously outgoing wars, conflicts and natural disasters. One of the important aspects of refugees and migrants is health. Till date, no comprehensive data was available related to health status of Afghan refugees and internally displaced persons (IDPs) in Pakistan. Here, we present health status for Afghan refugees for last seven years and for IDPs for 2-4 years. For Afghan refugees the data was provided by Commissionerate Afghan Refugee (CAR), Pakistan, whereas data for IDPs was collected from hospitals and Basic health units (BHUs) of different districts of Khyber Pakhtunkhwa namely Peshawar, Dera Ismail Khan and Bannu. Highest number of Afghan refugee's deaths occurred due to cardiovascular problems. Most prevalent reported infections were respiratory tract infections (48.05%). Skin diseases and Diarrhea collectively affected 21.08% of Afghan refugees. Overall, disease burden was more in females than males in Afghan refugee's population. To the best of our knowledge, this is the first comprehensive report on health and disease status of Afghan refugees and IDPs in Pakistan.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3389/fpubh.2019.00185DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6616124PMC
July 2019

Corrigendum: A Multi-Mode Bioactive Agent Isolated From L. Fill. With Therapeutic Potential for Type 2 Diabetes Mellitus.

Front Pharmacol 2019 13;10:643. Epub 2019 Jun 13.

Department of Biochemistry, Quaid-i-Azam University, Islamabad, Pakistan.

[This corrects the article DOI: 10.3389/fphar.2018.01376.].
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3389/fphar.2019.00643DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6585834PMC
June 2019

Identification of new spectral signatures from hepatitis C virus infected human sera.

Spectrochim Acta A Mol Biomol Spectrosc 2019 Nov 28;222:117181. Epub 2019 May 28.

Faculty of Biological Sciences, Qauid-i-Azam University, Islamabad, Pakistan. Electronic address:

Hepatitis C virus (HCV) infection is one of the leading causes of morbidity and mortality worldwide. Mortality linked with HCV infection can be lowered with effective and prompt diagnosis in early stages of infection. In this study potential of Raman spectroscopy to differentiate between healthy and HCV infected serum samples was investigated. Clear differences were observed in the Raman spectra of HCV infected and healthy sera samples. Using the analysis of variance (ANOVA) and t-test (p < 0.001) on Raman spectra of diseased and healthy samples, we observed eleven unique Raman bands at 676, 825, 853, 936, 1029, 1105, 1155, 1305, 1620, 1654 and 1757 cm associated with only HCV infected sera and have not been reported in earlier studies. In addition, six Raman bands at 556, 585, 716, 815, 1273 and 1142 cmwere observed in healthy sera only. Three Raman bands at 1330, 1526 and 1572 cm were observed in both type of samples but their intensity was drastically reduced in diseased samples. Various multivariate analysis techniques were employed to demonstrate the robustness of the results. We employed multivariate and unsupervised principal component analysis (PCA) in conjunction with supervised classification linear discriminant analysis (LDA), using ten-fold jackknife cross-validation, in order to develop effective diagnostic algorithm technique (PCA-LDA). Our PCA-LDA model yielded sufficient sensitivity and specificity i.e. correctly identified all infected samples included in this study. Ours results indicate that these unique Raman bands have the potential to be used as biomarkers for optical diagnosis of HCV infection.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.saa.2019.117181DOI Listing
November 2019

The Health Promoting Bioactivities of can be Enhanced by Genetic Modulation of Plant Secondary Metabolites.

Metabolites 2019 May 12;9(5). Epub 2019 May 12.

Institute for Global Food Security, School of Biological Sciences, Queen's University Belfast, Biological Sciences Building, Chlorine Gardens, Belfast BT9 5DL, UK.

Plant secondary metabolites are protective dietary constituents and genes evidently increase the synthesis of these versatile phytochemicals. This study subjected a globally important vegetable, lettuce () to a combination of untargeted metabolomics (LC-QTof-MS) and in vitro bioactivity assays. Specifically, we examined the differences between untransformed cultured lettuce (UnT), lettuce transformed with either (RA) or (RC) and commercially grown (COM) lettuce. Of the 5333 metabolite features aligned, deconvoluted and quantified 3637, 1792 and 3737 significantly differed in RA, RC and COM, respectively, compared with UnT. In all cases the number of downregulated metabolites exceeded the number increased. In vitro bioactivity assays showed that RA and RC (but not COM) significantly improved the ability of to inhibit α-glucosidase, inhibit dipeptidyl peptidase-4 (DPP-4) and stimulate GLP-1 secretion. We putatively identified 76 lettuce metabolites (sesquiterpene lactones, non-phenolic and phenolic compounds) some of which were altered by several thousand percent in RA and RC. Ferulic acid levels increased 3033-9777%, aminooxononanoic acid increased 1141-1803% and 2,3,5,4'tetrahydroxystilbene-2-O-β-d-glucoside increased 40,272-48,008%. Compound activities were confirmed using commercially obtained standards. In conclusion, gene transformation significantly alters the metabolome of and enhances its antidiabetic properties. There is considerable potential to exploit genes to modulate secondary metabolite production for the development of novel functional foods. This investigation serves as a new paradigm whereby genetic manipulation, metabolomic analysis and bioactivity techniques can be combined to enable the discovery of novel natural bioactives and determine the functional significance of plant metabolites.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/metabo9050097DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6572300PMC
May 2019

Synthesis, characterization and biological evaluation of novel benzimidazole derivatives.

J Biomol Struct Dyn 2020 Apr 22;38(6):1670-1682. Epub 2019 May 22.

School of Chemical Sciences, Dublin City University, Glasnevin, Ireland.

In search of achieving less toxic and more potent chemotherapeutics, three novel heterocyclic benzimidazole derivatives: 2-(1H-benzo[d]imidazol-2-yl)-4-chlorophenol (BM1), 4-chloro-2-(6-methyl-1H-benzo[d]imidazol-2-yl)phenol (BM2) and 4-chloro-2-(6-nitro-1H-benzo[d]imidazol-2-yl)phenol (BM3) with DNA-targeting properties, were synthesized and fully characterized by important physicochemical techniques. The DNA binding properties of the compounds were investigated by UV-Visible absorption titrations and thermal denaturation experiments. These molecules exhibited a good binding propensity to fish sperm DNA (FS-DNA), as evident from the high binding constants () values: 1.9 × 10, 1.39 × 10 and 1.8 × 10 M for BM1, BM2 and BM3, respectively. Thermal melting studies of DNA further validated the absorption titration results and best interaction was manifested by with Δ = 4.96 °C. The experimental DNA binding results were further validated theoretically by molecular docking study. It was confirmed that the molecules (BM1-BM3) bind to DNA an intercalative and groove binding mode. The investigations showed a correlation between binding constants and energies obtained experimentally and through molecular docking, indicating a binding preference of benzimidazole derivatives with the minor groove of DNA. BM1 was the preferential candidate for DNA binding because of its flat structure, π-π interactions and less steric hindrance. To complement the DNA interaction, antimicrobial assays (antibacterial & antifungal) were performed. It was observed that compound showed promising activity against all bacterial strains (, , and ) and fungi ( and ), while rest of the compounds were active against selective strains. The MIC values of were found to be in the range of 12.5 ± 2.2-25 ± 1.5 µg/mL. Thus, the compound was found to be the effective DNA binding antimicrobial agent. Furthermore, the preliminary cytotoxic properties of synthesized compounds were evaluated by brine shrimps lethality assay to check their nontoxic nature towards healthy normal cells.Communicated by Ramaswamy H. Sarma.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1080/07391102.2019.1617783DOI Listing
April 2020

Chloroplast genome of Hibiscus rosa-sinensis (Malvaceae): Comparative analyses and identification of mutational hotspots.

Genomics 2020 01 15;112(1):581-591. Epub 2019 Apr 15.

Department of Biochemistry, Quaid-i-Azam University, Islamabad, Pakistan. Electronic address:

Previous studies to resolve phylogenetic and taxonomic discrepancies of Hibiscus remained inconclusive. Here, we report chloroplast genome sequence of Hibiscus rosa-sinensis. Hibiscus rosa-sinensis chloroplast genome was 160,951 bp, comprising of large single copy (89,509 bp) and small single copy (20,246 bp) regions, separated by IRa and IRb (25,598 bp each). The genome contained 130 genes including 85 protein-coding genes, 37 transfer RNAs and 8 ribosomal RNAs. Comparative analyses of chloroplast genomes revealed similar structure among 12 species within family Malvaceae. Evolutionary rates of 77 protein-coding genes showed 95% similarities. Analyses of codon usage, amino acid frequency, putative RNA editing sites, and repeats showed a great extent of similarities between Hibiscus rosa-sinensis and Hibiscus syriacus. We identified 30 mutational hotpots including psbZ-trnG, trnK-rps16, trnD-trnY, trnW-trnP, rpl33-rps18, petG-trnW, trnS-trnG, trnH-psbA, atpB-rbcL, and rpl32-trnL that might be used as polymorphic and robust markers to resolve phylogenetic discrepancies in genus Hibiscus.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ygeno.2019.04.010DOI Listing
January 2020

Author Correction: Drier Climatic Conditions Increase Withanolide Content of Withania coagulans Enhancing its Inhibitory Potential against Human Prostate Cancer Cells.

Appl Biochem Biotechnol 2019 07;188(3):893-895

Department of Biochemistry, Quaid-i-Azam University, Islamabad, Pakistan.

The original version of this article unfortunately contained a mistake in the image of Figure 1 and in Table 4. The corrected version of the figure and table is shown here.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1007/s12010-018-02941-8DOI Listing
July 2019

A Multi-Mode Bioactive Agent Isolated From L. Fill. With Therapeutic Potential for Type 2 Diabetes Mellitus.

Front Pharmacol 2018 27;9:1376. Epub 2018 Nov 27.

Department of Biochemistry, Quaid-i-Azam University, Islamabad, Pakistan.

Type 2 diabetes is a metabolic disorder, characterized by hyperglycemia and glucose intolerance. Natural products and its derived active compounds may be achievable alternatives for the treatment of type 2 diabetes. In present study we investigated the antidiabetic potential of and isolated bioactive compounds i.e., Plectranthoic acid A (PA-A) and 3,4,5,7-Flavantetrol (FL). Anti-hyperglycemic potential was evaluated α-glucosidase, α-amylase and dipeptidyl peptidase 4 (DPP-4) assays. 5'AMP-activated kinase (AMPK) activation potential was assessed by using primary hepatocytes. Distribution of PA-A in different parts of was evaluated by using rapid high-performance liquid chromatography (HPLC). Ethyl acetate fraction (FME) exhibited significant inhibition of α-glucosidase, α-amylase, and DPP-4, therefore, was selected for isolation of bioactive compounds. Among isolated compounds PA-A was more potent and possessed pleotropic inhibitory activity with IC values of 39.5, 55.5, and 51.4 μM against α-glucosidase, α-amylase, and DPP-4, respectively. Our results showed that PA-A is also a potent activator of AMPK which is a central hub of metabolic regulation. Molecular docking studies confirmed the activity of PA-A against α-glucosidase, α-amylase, and DPP-4. Rapid HPLC method revealed that maximum concentration of PA-A is present in the stem (2.25 μg/mg dry weight) of . Both and studies proposed that and its isolated compound PA-A could be an important natural source for alleviating the symptoms of type 2 diabetes mellitus and we suggest that PA-A should be explored further for its ultimate use for the treatment of type 2 diabetes.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3389/fphar.2018.01376DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6277780PMC
November 2018

Drier Climatic Conditions Increase Withanolide Content of Withania coagulans Enhancing Its Inhibitory Potential Against Human Prostate Cancer Cells.

Appl Biochem Biotechnol 2019 Jun 10;188(2):460-480. Epub 2018 Dec 10.

Department of Biochemistry, Quaid-i-Azam University, Islamabad, Pakistan.

Prostate cancer is one of the major causes of cancer-related deaths in men and there is a growing interest in identifying natural compounds for its management. We analyzed bioactive withanolides in Withania coagulans from 11 different sites in Pakistan and evaluated the antiprostate cancer activities of leaf extracts from two sites with the greatest amounts. Total withanolide concentration differed by ~ 17-fold between sites, ranging from 1.01 ± 0.01 mg/g dry weight (mean ± SE) at Jand to 16.83 ± 0.02 mg/g at Mohmand Agency. Different tissues varied in their total withanolide content with roots having the least (0.42 ± 0.07 mg/g dry weight) and leaves the most (2.45 ± 0.45 mg/g). We found strong inverse correlations between site annual precipitation versus withanolide amounts in fruits (r = - 0.84, P = 0.001), leaves (r = - 0.88, P < 0.001), roots (r = - 0.91, P < 0.001), and total (r = - 0.89, P < 0.001), but not stems (r = - 0.20, P = 0.556). Extracts made from Mianwali and Mohmand Agency leaves possessed high anticancer activity in terms of increased induction of apoptosis and decreased cell viability, cell proliferation, invasion, and migration of different prostate cancer cell lines. These results are useful for the selection of withanolide-rich germplasm with potent anticancer properties.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1007/s12010-018-02933-8DOI Listing
June 2019

MTHFR polymorphisms as risk for male infertility in Pakistan and its comparison with socioeconomic status in the world.

Per Med 2019 01 23;16(1):35-49. Epub 2018 Nov 23.

Institute of Biomedical & Genetic Engineering (IB & GE), 24 Mauve Area, G9/1, Islamabad 44000, Pakistan.

Aim: 5,10-MTHFR-single nucleotide polymorphisms are important for normal functioning of the enzyme that plays a key role in DNA synthesis, folate metabolism and methylation reactions. Methodology & results: Male infertility association of C665T and A1298C polymorphisms was explored, this topic is still debatable. Infertile men (232) and controls (114) were genotyped and statistically analyzed. Comparison of patients (6180) and controls (5744) of Caucasian populations was performed by meta-analysis. Pooled results showed A1298C minor allele and homozygous genotype to be of a significantly higher frequency in the low-income group. Increase in per capita income has shown an increasing trend in the minor allele frequency in various world populations, potentially due to dietry-folate compensation.

Conclusion: A1298C seems more relevant marker than C665T for infertility association in Caucasian populations and may be addressed by improving dietary folate.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.2217/pme-2018-0045DOI Listing
January 2019

Neuroprotective, antidiabetic and antioxidant effect of Hedera nepalensis and lupeol against STZ + AlCl induced rats model.

Daru 2018 Dec 23;26(2):179-190. Epub 2018 Oct 23.

Department of Biochemistry, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan.

Purpose: This study was aimed to evaluate the effect of Hedera nepalensis crude extract (HNC) and its isolated compound lupeol on antioxidant defence system, biochemical parameters and behavioural indices of Alzheimer disease generated in diabetic rats.

Methods: To evaluate the effect of the plant extract and lupeol, symptoms of Alzheimer and diabetes were induced in rats by STZ + AlCl treatment. Glucose level was measured with glucometer followed by antioxidant and biochemical assessment of the treated and untreated animals. Behavioural response of the rats was determined by Elevated Plus Maze (EPM) test and Morris Water Maze (MWM) test followed by determination of brain neurotransmitters by HPLC.

Results: HNC significantly reduced blood glucose level in a time dependent manner and elevated liver function markers were significantly (P < 0.05) reinstated to normal levels. HNC showed increase in level of catalase (CAT), superoxide dismutase (SOD) and reduced glutathione (GSH). HPLC quantification revealed that HNC treatment led to significant (p < 0.001) elevation in the level of neurotransmitters (dopamine and serotonin) in the midbrain region as compared to Alzheimer control (AC) group. EPM and MWM test showed decrease in cognitive and memory impairment in a rat group treated with HNC as compared to AC group.

Conclusion: Overall, results showed that H. nepalensis has therapeutic potential for the treatment of diseases like Alzheimer and diabetes. Graphical abstract Therapeutic effect of Hedera nepalensis K. Koch and lupeol against STZ + AICI induced diabetic rats model.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-018-0223-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6279670PMC
December 2018

Synthesis, molecular docking and comparative efficacy of various alkyl/aryl thioureas as antibacterial, antifungal and α-amylase inhibitors.

Comput Biol Chem 2018 Dec 10;77:193-198. Epub 2018 Oct 10.

Department of Biochemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan.

Thioureas are exquisite building blocks for the construction of five and six membered heterocyclic units, and also display an extensive range of biological activities. 4-Nitro-2-cyano aniline was reacted with the various acid chlorides which were freshly prepared from carboxylic acids to afford the desired products in good yield. All the newly synthesized compounds were evaluated antibacterial, antifungal, antioxidant and α-amylase activity. The compounds showed significant activity against bacteria and fungi. The compound 4e and 4b were found to be most inhibitors of α-amylase having IC 9.7 μg/ml and 9.1 μg/ml. Further molecular docking studies were carried out to find out the binding mode of the inhibitors with the enzyme.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.compbiolchem.2018.10.007DOI Listing
December 2018