Displaying publications 1 - 20 of 35 in total

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  1. Fulltext Docking Based 3D-QSAR Study of Tricyclic Guanidine Analogues of Batzelladine K As Anti-Malarial Agents
    Ahmed N, Anwar S, Thet Htar T
    Front Chem, 2017;5:36.
    PMID: 28664157 DOI: 10.3389/fchem.2017.00036
    The Plasmodium falciparum Lactate Dehydrogenase enzyme (PfLDH) catalyzes inter-conversion of pyruvate to lactate during glycolysis producing the energy required for parasitic growth. The PfLDH has been studied as a potential molecular target for development of anti-malarial agents. In an attempt to find the potent inhibitor of PfLDH, we have used Discovery studio to perform molecular docking in the active binding pocket of PfLDH by CDOCKER, followed by three-dimensional quantitative structure-activity relationship (3D-QSAR) studies of tricyclic guanidine batzelladine compounds, which were previously synthesized in our laboratory. Docking studies showed that there is a very strong correlation between in silico and in vitro results. Based on docking results, a highly predictive 3D-QSAR model was developed with q(2) of 0.516. The model has predicted r(2) of 0.91 showing that predicted IC50 values are in good agreement with experimental IC50 values. The results obtained from this study revealed the developed model can be used to design new anti-malarial compounds based on tricyclic guanidine derivatives and to predict activities of new inhibitors.
  2. Fulltext Editorial: Targeting tumor EMT-related signaling by natural products
    Anwar S, Ahmed N, Giampietro L
    Front Pharmacol, 2023;14:1152328.
    PMID: 36891267 DOI: 10.3389/fphar.2023.1152328
  3. Fulltext An evolutionary firefly algorithm for the estimation of nonlinear biological model parameters
    Abdullah A, Deris S, Anwar S, Arjunan SN
    PLoS One, 2013;8(3):e56310.
    PMID: 23469172 DOI: 10.1371/journal.pone.0056310
    The development of accurate computational models of biological processes is fundamental to computational systems biology. These models are usually represented by mathematical expressions that rely heavily on the system parameters. The measurement of these parameters is often difficult. Therefore, they are commonly estimated by fitting the predicted model to the experimental data using optimization methods. The complexity and nonlinearity of the biological processes pose a significant challenge, however, to the development of accurate and fast optimization methods. We introduce a new hybrid optimization method incorporating the Firefly Algorithm and the evolutionary operation of the Differential Evolution method. The proposed method improves solutions by neighbourhood search using evolutionary procedures. Testing our method on models for the arginine catabolism and the negative feedback loop of the p53 signalling pathway, we found that it estimated the parameters with high accuracy and within a reasonable computation time compared to well-known approaches, including Particle Swarm Optimization, Nelder-Mead, and Firefly Algorithm. We have also verified the reliability of the parameters estimated by the method using an a posteriori practical identifiability test.
  4. Fulltext A novel rules based approach for estimating software birthmark
    Nazir S, Shahzad S, Khan SA, Alias NB, Anwar S
    ScientificWorldJournal, 2015;2015:579390.
    PMID: 25945363 DOI: 10.1155/2015/579390
    Software birthmark is a unique quality of software to detect software theft. Comparing birthmarks of software can tell us whether a program or software is a copy of another. Software theft and piracy are rapidly increasing problems of copying, stealing, and misusing the software without proper permission, as mentioned in the desired license agreement. The estimation of birthmark can play a key role in understanding the effectiveness of a birthmark. In this paper, a new technique is presented to evaluate and estimate software birthmark based on the two most sought-after properties of birthmarks, that is, credibility and resilience. For this purpose, the concept of soft computing such as probabilistic and fuzzy computing has been taken into account and fuzzy logic is used to estimate properties of birthmark. The proposed fuzzy rule based technique is validated through a case study and the results show that the technique is successful in assessing the specified properties of the birthmark, its resilience and credibility. This, in turn, shows how much effort will be required to detect the originality of the software based on its birthmark.
  5. Fulltext An improved swarm optimization for parameter estimation and biological model selection
    Abdullah A, Deris S, Mohamad MS, Anwar S
    PLoS One, 2013;8(4):e61258.
    PMID: 23593445 DOI: 10.1371/journal.pone.0061258
    One of the key aspects of computational systems biology is the investigation on the dynamic biological processes within cells. Computational models are often required to elucidate the mechanisms and principles driving the processes because of the nonlinearity and complexity. The models usually incorporate a set of parameters that signify the physical properties of the actual biological systems. In most cases, these parameters are estimated by fitting the model outputs with the corresponding experimental data. However, this is a challenging task because the available experimental data are frequently noisy and incomplete. In this paper, a new hybrid optimization method is proposed to estimate these parameters from the noisy and incomplete experimental data. The proposed method, called Swarm-based Chemical Reaction Optimization, integrates the evolutionary searching strategy employed by the Chemical Reaction Optimization, into the neighbouring searching strategy of the Firefly Algorithm method. The effectiveness of the method was evaluated using a simulated nonlinear model and two biological models: synthetic transcriptional oscillators, and extracellular protease production models. The results showed that the accuracy and computational speed of the proposed method were better than the existing Differential Evolution, Firefly Algorithm and Chemical Reaction Optimization methods. The reliability of the estimated parameters was statistically validated, which suggests that the model outputs produced by these parameters were valid even when noisy and incomplete experimental data were used. Additionally, Akaike Information Criterion was employed to evaluate the model selection, which highlighted the capability of the proposed method in choosing a plausible model based on the experimental data. In conclusion, this paper presents the effectiveness of the proposed method for parameter estimation and model selection problems using noisy and incomplete experimental data. This study is hoped to provide a new insight in developing more accurate and reliable biological models based on limited and low quality experimental data.
  6. Fulltext In vivo anticlastogenic effect of silymarin from milk thistle Silybum marianum L
    Anwar S, Madkor HR, Ahmed N, Wagih ME
    Indian J Pharmacol, 2018 9 1;50(3):108-115.
    PMID: 30166747 DOI: 10.4103/ijp.IJP_660_16
    OBJECTIVE: Silymarin, extracted from the seeds of Silybum marianum L. (Milk thistle), is traditionally used for treating various illnesses such as diabetes, cancer, inflammation, hepatitis, liver cirrhosis, and renal problems. Acute cytotoxicity and genotoxicity studies have been reported with ambiguous outcomes; however, its relevant anticlastogenic potential is not yet evaluated. This study was aimed to evaluate in vivo subacute anticlastogenic properties of silymarin to validate its use as a medicinal agent.

    MATERIALS AND METHODS: Silymarin was isolated from seeds of milk thistle. Various genotoxicity bioassays of silymarin were performed using mice. First, the bone marrow cell proliferation was estimated by calculating mitotic index. Second, the chromosomal abnormalities in mice bone marrow cells were studied. Third, micronucleated polychromatic erythrocytes (MPE) test and in vivo activation of sister chromatid exchanges (SCEs) were carried out in mice bone marrow cells. Finally, primary spermatocytes were analyzed to estimate genotoxic effect of silymarin on germ cells.

    RESULTS: We found that silymarin is capable of inducing a significant increase (P ≤ 0.05) in cell proliferation of bone marrow cells. There is no increase in chromosomal aberrations following silymarin treatments. Results clearly showed that it significantly (P ≤ 0.05) decreased the MPE. Likewise, it was found to be a negative inducer of SCEs. It decreased in total abnormal metaphase, SCEs, MPE, and aberrant diakinesis.

    CONCLUSION: The results demonstrated that silymarin has a strong anticlastogenic activity upon mice genome in somatic and germ cells, indicating its safe use as a medicinal substance. Furthermore, it is not only safe but also has protective effect from clastogens.

  7. Quinolone Derivatives as Anticancer Agents: Importance in Medicinal Chemistry
    Azzman N, Anwar S, Syazani Mohamed WA, Ahemad N
    Curr Top Med Chem, 2024 Apr 08.
    PMID: 38591202 DOI: 10.2174/0115680266300736240403075307
    Quinolone is a heterocyclic compound containing carbonyl at the C-2 or C-4 positions with nitrogen at the C-1 position. The scaffold was first identified for its antibacterial properties, and the derivatives were known to possess many pharmacological activities, including anticancer. In this review, the quinolin-2(H)-one and quinolin-4(H)-one derivatives were identified to inhibit several various proteins and enzymes involved in cancer cell growth, such as topoisomerase, mi-crotubules, protein kinases, phosphoinositide 3-kinases (PI3K) and histone deacetylase (HDAC). Hybrids of quinolone with curcumin or chalcone, 2-phenylpyrroloquinolin-4-one and 4-quinolone derivatives have demonstrated strong potency against cancer cell lines. Additionally, quinolones have been explored as inhibitors of protein kinases, including EGFR and VEGFR. Therefore, this review aims to consolidate the medicinal chemistry of quinolone derivatives in the pipeline and discuss their similarities in terms of their pharmacokinetic profiles and potential target sites to provide an understanding of the structural requirements of anticancer quinolones.
  8. Fulltext Sweet's syndrome in Crohn's colitis
    Anwar S, Hishamuddin A, Khairul AJ, Shamsul AJ, Razlan H, Said MS
    BMJ Case Rep, 2009;2009.
    PMID: 21687021 DOI: 10.1136/bcr.01.2009.1438
    We would like to report a case involving a 38-year-old woman who presented with knee and ankle swellings 2 weeks prior to admission. There were also multiple painful oral ulcers and a few skin sores on the wrist. She also had associated diarrhoea for 2 weeks. There was also marked loss of weight (6 kg in 2 weeks). Colonoscopy examination showed macroscopic and histopathological findings of Crohn's disease; however, skin histology showed extensive neutrophilic infiltration in the dermis, predominantly in the perivascular region. Her final diagnosis was Sweet's syndrome with Crohn's disease.
  9. Fulltext Splenic tuberculosis presenting as pyrexia of unknown origin
    Hamizah R, Rohana AG, Anwar SA, Ong TZ, Hamzaini AH, Zulkarnaen AN
    Med J Malaysia, 2007 Mar;62(1):70-1.
    PMID: 17682577 MyJurnal
    We report a case of a previously healthy 38-year old lady who presented with prolonged fever and hepatosplenomegaly. Intensive investigations were performed for pyrexia of unknown origin which revealed negative. CT scan of the abdomen showed multiple hypodense lesions which did not respond to broad-spectrum antibiotics. Percutaneous biopsy of the splenic lesion revealed granuloma formation and Langhan's giant cells suggestive of TB. She responded well with anti- TB medication but required extended treatment duration of 24 months due to persistence of the splenic lesion on repeated CT scans. This case illustrates a very rare clinical entity of isolated splenic TB with a therapeutic dilemma following incomplete resolution, despite prolonged treatment.
  10. Fulltext HPLC-PDA Polyphenolic Quantification, UHPLC-MS Secondary Metabolite Composition, and In Vitro Enzyme Inhibition Potential of Bougainvillea glabra
    Saleem H, Htar TT, Naidu R, Anwar S, Zengin G, Locatelli M, et al.
    Plants (Basel), 2020 Mar 20;9(3).
    PMID: 32245104 DOI: 10.3390/plants9030388
    The plants of the Bougainvillea genus are widely explored regarding nutritive and medicinal purposes. In this study, dichloromethane (DCM) and methanol (MeOH) extracts of Bougainvillea glabra (Choisy.) aerial and flower parts were analyzed for high-performance liquid chromatography with photodiode array detection (HPLC-PDA), ultra-high-performance liquid chromatography-mass spectrometry (UHPLC-MS) phytochemical composition, and enzyme inhibition potential against key enzymes involved in diabetes (α-amylase), skin problems (tyrosinase), and inflammatory disorders (lipoxygenase (LOX)). HPLC-PDA quantification revealed the identification of nine different polyphenolics, amongst which both flower extracts were richest. The flower MeOH extract contained the highest amount of catechin (6.31 μg/g), gallic acid (2.39 μg/g), and rutin (1.26 μg/g). However, none of the quantified compounds were detected in the aerial DCM extract. UHPLC-MS analysis of DCM extracts revealed the tentative identification of 27 secondary metabolites, where the most common belonged to terpenoid, alkaloid, and phenolic derivatives. Similarly, for enzyme inhibition, all the extracts presented moderate activity against tyrosinase and α-amylases, whereas, for LOX, both methanolic extracts showed higher percentage inhibition compared with DCM extracts. Based on our findings, B. glabra could be regarded as a perspective starting material for designing novel pharmaceuticals.
  11. Antiviral activities of Cholistani plants against common poultry viruses
    Shahzad MI, Anwar S, Ashraf H, Manzoor A, Naseer M, Rani U, et al.
    Trop Biomed, 2020 Dec 01;37(4):1129-1140.
    PMID: 33612765 DOI: 10.47665/tb.37.4.1129
    Herbal medicines are becoming more popular and acceptable day by day due to their effectiveness, limited side effects, and cost-effectiveness. Cholistani plants are reported as a rich source of antibacterial, antifungal, antiprotozoal, antioxidant, and anticancer agents. The current study has evaluated antiviral potential of selected Cholistani plants. The whole plants were collected, ground and used in extract formation with n-hexane, ethyl acetate and n-butanol. All the extracts were concentrated by using a rotary evaporator and concentrate was finally dissolved in an appropriate vol of the same solvent. All of the extracts were tested for their antiviral potential by using 9-11 days old chick embryonated eggs. Each extract was tested against the Avian Influenza virus H9N2 strain (AIV), New Castle Disease virus Lasoota strain (NDV), Infectious bronchitis virus (IBV) and an Infectious bursal disease virus (IBDV). Hemagglutination test (HA) and Indirect Hemagglutination (IHA) tests were performed for different viruses. The overall order of the antiviral potential of Cholistani plants against viruses was NDV>IBV>IBDV>AIV. In terms of antiviral activity from extracts, the order of activity was n-butanol>ethyl acetate>n-hexane. The medicinal plants Achyranthes aspera, Neuroda procumbens, Panicum antidotale, Ochthochloa compressa and Suaeda fruticose were very effective against all four poultry viruses through their extracts. The low IC50 values of these extracts confirm the high antiviral potential against these viruses. It is worth to mention that Achyranthes aspera was found positive against IBDV through all its extracts which overcome the problem of unavailability of any known drug against IBDV. In short, the study proved that Cholistani plants are rich source of antiviral agent and their extracts can be used as good source of antiviral drugs both in crude and in purified form.
  12. Fulltext Can Natural Products Targeting EMT Serve as the Future Anticancer Therapeutics?
    Anwar S, Malik JA, Ahmed S, Kameshwar VA, Alanazi J, Alamri A, et al.
    Molecules, 2022 Nov 08;27(22).
    PMID: 36431766 DOI: 10.3390/molecules27227668
    Cancer is the leading cause of death and has remained a big challenge for the scientific community. Because of the growing concerns, new therapeutic regimens are highly demanded to decrease the global burden. Despite advancements in chemotherapy, drug resistance is still a major hurdle to successful treatment. The primary challenge should be identifying and developing appropriate therapeutics for cancer patients to improve their survival. Multiple pathways are dysregulated in cancers, including disturbance in cellular metabolism, cell cycle, apoptosis, or epigenetic alterations. Over the last two decades, natural products have been a major research interest due to their therapeutic potential in various ailments. Natural compounds seem to be an alternative option for cancer management. Natural substances derived from plants and marine sources have been shown to have anti-cancer activity in preclinical settings. They might be proved as a sword to kill cancerous cells. The present review attempted to consolidate the available information on natural compounds derived from plants and marine sources and their anti-cancer potential underlying EMT mechanisms.
  13. Fulltext Malware detection using static analysis in Android: a review of FeCO (features, classification, and obfuscation)
    Jusoh R, Firdaus A, Anwar S, Osman MZ, Darmawan MF, Ab Razak MF
    PeerJ Comput Sci, 2021;7:e522.
    PMID: 34825052 DOI: 10.7717/peerj-cs.522
    Android is a free open-source operating system (OS), which allows an in-depth understanding of its architecture. Therefore, many manufacturers are utilizing this OS to produce mobile devices (smartphones, smartwatch, and smart glasses) in different brands, including Google Pixel, Motorola, Samsung, and Sony. Notably, the employment of OS leads to a rapid increase in the number of Android users. However, unethical authors tend to develop malware in the devices for wealth, fame, or private purposes. Although practitioners conduct intrusion detection analyses, such as static analysis, there is an inadequate number of review articles discussing the research efforts on this type of analysis. Therefore, this study discusses the articles published from 2009 until 2019 and analyses the steps in the static analysis (reverse engineer, features, and classification) with taxonomy. Following that, the research issue in static analysis is also highlighted. Overall, this study serves as the guidance for novice security practitioners and expert researchers in the proposal of novel research to detect malware through static analysis.
  14. Correction to: Understanding translational research in schizophrenia: A novel insight into animal models
    Malik JA, Yaseen Z, Lahari T, Ahmed S, Shaikh MF, Anwar S
    Mol Biol Rep, 2023 Apr 06.
    PMID: 37024749 DOI: 10.1007/s11033-023-08352-1
  15. Nano-drug delivery system: a promising approach against breast cancer
    Malik JA, Ansari JA, Ahmed S, Khan A, Ahemad N, Anwar S
    Ther Deliv, 2023 May;14(5):357-381.
    PMID: 37431741 DOI: 10.4155/tde-2023-0020
    Breast cancer (BC) is among the most frequent malignancies women face around the globe. Nanotherapeutics are constantly evolving to overcome the limitations of conventional diagnostic and therapeutic approaches. Nanotechnology-based nanocarriers have a higher entrapment efficiency, low cytotoxicity, greater stability and improved half-life than conventional therapy. Nano-drug delivery systems have improved pharmacokinetics and pharmacodynamics parameters because of nanomeric size. Currently, various nano-formulations are in preclinical and clinical settings for breast cancer, like polymeric nanoparticles, micelles, nanobodies, magnetic nanoparticles, liposomes, niosomes, gold-nanoparticles, dendrimers and carbon-nanotubes. This review highlights the recent advancement in developing nano-drug delivery systems for BC treatment. This review will open the gateway to researchers to understand the current approaches to developing nano-formulation and improving problems associated with conventional therapy.
  16. Fulltext Understanding translational research in schizophrenia: A novel insight into animal models
    Malik JA, Yaseen Z, Thotapalli L, Ahmed S, Shaikh MF, Anwar S
    Mol Biol Rep, 2023 Apr;50(4):3767-3785.
    PMID: 36692676 DOI: 10.1007/s11033-023-08241-7
    Schizophrenia affects millions of people worldwide and is a major challenge for the scientific community. Like most psychotic diseases, it is also considered a complicated mental disorder caused by an imbalance in neurotransmitters. Due to the complexity of neuropathology, it is always a complicated disorder. The lack of proper understanding of the pathophysiology makes the disorder unmanageable in clinical settings. However, due to recent advances in animal models, we hope we can have better therapeutic approaches with more success in clinical settings. Dopamine, glutamate, GABA, and serotonin are the neurotransmitters involved in the pathophysiology of schizophrenia. Various animal models have been put forward based on these neurotransmitters, including pharmacological, neurodevelopmental, and genetic models. Polymorphism of genes such as dysbindin, DICS1, and NRG1 has also been reported in schizophrenia. Hypothesis based on dopamine, glutamate, and serotonin are considered successful models of schizophrenia on which drug therapies have been designed to date. New targets like the orexin system, muscarinic and nicotinic receptors, and cannabinoid receptors have been approached to alleviate the negative and cognitive symptoms. The non-pharmacological models like the post-weaning social isolation model (maternal deprivation), the isolation rearing model etc. have been also developed to mimic the symptoms of schizophrenia and to create and test new approaches of drug therapy which is a breakthrough at present in psychiatric disorders. Different behavioral tests have been evaluated in these specific models. This review will highlight the currently available animal models and behavioral tests in psychic disorders concerning schizophrenia.
  17. Fulltext The evidence for repurposing anti-epileptic drugs to target cancer
    Aroosa M, Malik JA, Ahmed S, Bender O, Ahemad N, Anwar S
    Mol Biol Rep, 2023 Sep;50(9):7667-7680.
    PMID: 37418080 DOI: 10.1007/s11033-023-08568-1
    Antiepileptic drugs are versatile drugs with the potential to be used in functional drug formulations with drug repurposing approaches. In the present review, we investigated the anticancer properties of antiepileptic drugs and interlinked cancer and epileptic pathways. Our focus was primarily on those drugs that have entered clinical trials with positive results and those that provided good results in preclinical studies. Many contributing factors make cancer therapy fail, like drug resistance, tumor heterogeneity, and cost; exploring all alternatives for efficient treatment is important. It is crucial to find new drug targets to find out new antitumor molecules from the already clinically validated and approved drugs utilizing drug repurposing methods. The advancements in genomics, proteomics, and other computational approaches speed up drug repurposing. This review summarizes the potential of antiepileptic drugs in different cancers and tumor progression in the brain. Valproic acid, oxcarbazepine, lacosamide, lamotrigine, and levetiracetam are the drugs that showed potential beneficial outcomes against different cancers. Antiepileptic drugs might be a good option for adjuvant cancer therapy, but there is a need to investigate further their efficacy in cancer therapy clinical trials.
  18. Fulltext Knowledge and awareness of hepatitis B among households in Malaysia: a community-based cross-sectional survey
    Rajamoorthy Y, Taib NM, Munusamy S, Anwar S, Wagner AL, Mudatsir M, et al.
    BMC Public Health, 2019 Jan 10;19(1):47.
    PMID: 30630464 DOI: 10.1186/s12889-018-6375-8
    BACKGROUND: Hepatitis B (HepB) is a major public health concern in Malaysia yet little is known about knowledge and awareness of this infection in the country. Such information is essential for designing effective intervention strategies for HepB prevention and control. The aim of this study was to characterize knowledge and awareness regarding HepB in Malaysia and to identify their associated sociodemographic determinants.

    METHODS: A community-based cross-sectional survey was conducted between January and May 2016 in Selangor state of Malaysia. A two-stage cluster random sampling design was used and one adult member of selected households was interviewed face-to-face. Logistic regression was used to estimate the differences in knowledge and awareness between groups.

    RESULTS: A total of 764 households completed the interviews and were included in the final analysis. Only 36.9 and 38.8% of the participants had good knowledge and awareness, respectively. The factors associated with good knowledge were being in the 35-44 year age group, Malay ethnicity, high educational attainment and high family income. Being Chinese, being older and having high educational attainment were determinants of having good awareness towards HepB. Participants who had good knowledge were 2.5 times more likely to also have good awareness (OR: 2.41, 95% CI: 1.78-3.26, p 

  19. A comprehensive phytochemical, biological, toxicological and molecular docking evaluation of Suaeda fruticosa (L.) Forssk.: An edible halophyte medicinal plant
    Saleem H, Khurshid U, Sarfraz M, Tousif MI, Alamri A, Anwar S, et al.
    Food Chem Toxicol, 2021 Aug;154:112348.
    PMID: 34144099 DOI: 10.1016/j.fct.2021.112348
    Suaeda fruticosa is an edible medicinal halophyte known for its traditional uses. In this study, methanol and dichloromethane extracts of S. fruticosa were explored for phytochemical, biological and toxicological parameters. Total phenolic and flavonoid constituents were determined by using standard aluminum chloride and Folin-Ciocalteu methods, and UHPLC-MS analysis of methanol extract was performed for tentative identification of secondary metabolites. Different standard methods like DPPH, ABTS, FRAP, CUPRAC, total antioxidant capacity (TAC), and metal chelation assays were utilized to find out the antioxidant potential of extracts. Enzyme inhibition studies of extracts against acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase and, α-glucosidase enzymes were also studied. Likewise, the cytotoxicity was also assessed against MCF-7, MDA-MB-231, and DU-145 cell lines. The higher phenolic and flavonoids contents were observed in methanol extracts which can be correlated to its higher radical scavenging potential. Similarly, 11 different secondary metabolites were tentatively identified by UHPLC profiling. Both the extract showed significant inhibition against all the enzymes except for α-glucosidase. Moreover, docking studies were also performed against the tested enzymes. In the case of cytotoxicity, both the samples were found moderately toxic against the tested cell lines. This plant can be explored further for its potential therapeutic and edible uses.
  20. Fulltext Evaluation of the Phytochemical, Antioxidant, Enzyme Inhibition, and Wound Healing Potential of Calotropis gigantea (L.) Dryand: A Source of a Bioactive Medicinal Product
    Alafnan A, Sridharagatta S, Saleem H, Khurshid U, Alamri A, Ansari SY, et al.
    Front Pharmacol, 2021;12:701369.
    PMID: 34483902 DOI: 10.3389/fphar.2021.701369
    Traditionally, plants of the genus Calotropis have been used to cure various common diseases. The present research work explores the chemical and biological characterization of one of the most common species of this genus, i.e., Calotropis gigantea (L.) Dryand (syn. Calotropis gigantea (L.) Dryand.), having multiple folklore applications. The ethanolic extract of leaves of Calotropis gigantea (L.) Dryand was analyzed for the phytochemical composition by determining the total bioactive (total phenolic and total flavonoid) contents and UHPLC-MS secondary metabolites analysis. For phytopharmacological evaluation, in vitro antioxidant (including DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelation antioxidant assays) activities, enzyme inhibition potential (against AChE, BChE, α-amylase, and tyrosinase enzymes), and in vivo wound healing potential were determined. The tested extract has been shown to contain considerable flavonoid (46.75 mg RE/g extract) and phenolic (33.71 mg GAE/g extract) contents. The plant extract presented considerable antioxidant potential, being the most active for CUPRAC assays. Secondary metabolite UHPLC-MS characterization, in both the positive and negative ionization modes, indicated the tentative presence of 17 different phytocompounds, mostly derivatives of sesquiterpene, alkaloids, and flavonoids. Similarly, the tested extract exhibited considerable inhibitory effects on tyrosinase (81.72 mg KAE/g extract), whereas it showed weak inhibition ability against other tested enzymes. Moreover, in the case of in vivo wound healing assays, significant improvement in wound healing was observed in both the tested models at the doses of 0.5 percent w/w (p < 0.001) and 2.0 percent w/w (p < 0.01) on the 16th day. The outcomes of the present research work suggested that C. gigantea (L.) Dryand plant extract could be appraised as a potential origin of bioactive molecules having multifunctional medicinal uses.
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