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1.
Heliyon ; 10(1): e23183, 2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-38163140

RESUMO

Aim and objective: Due to the a lot of unexplored proteins in HIV-1, this research aimed to explore the functional roles of a hypothetical protein (AAB33144.1) that might play a key role in HIV-1 pathogenicity. Methods: The homologous protein was identified along with building and validating the 3D structure by searching several bioinformatics tools. Results: Retroviral aspartyl protease and retropepsin like functional domains and motifs, folding pattern (cupredoxins), and subcellular localization in cytoplasmic membrane were determined as biological activity. Besides, the functional annotation revealed that the chosen hypothetical protein possessed protease-like activity. To validate our generated protein 3D structure, molecular docking was performed with five compounds where nelfinavir showed (-8.2 kcal/mol) best binding affinity against HXB2 viral protease (PDB ID: 7SJX) and main protease (PDB ID: 4EYR) protein. Conclusions: This study suggests that the annotated hypothetical protein related to protease action, which may be useful in viral genetics and drug discovery.

2.
Chem Biodivers ; 20(12): e202300952, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37994297

RESUMO

The genus Melicope, which consists of 230 species, stands out as the largest genus within the Rutaceae family. Melicope species are characterized by their evergreen nature and can range from shrubs to predominantly dioecious trees. The Melicope species have been utilized in traditional medicine to address a wide range of ailments, including fever, colds, cramps, and inflammation. These plants have gained significant attention due to their noteworthy ethnopharmacological and ethnomedicinal significance. Researchers have isolated numerous biologically active secondary metabolites from different Melicope species, which include polymethoxylated flavonoids, furanocoumarins, acetophenones, benzenoids, and quinolone alkaloids. These compounds exhibit diverse biological activities, such as antibacterial, antidiabetic, antifungal, and antiproliferative properties against human cancer cell lines. This review provides an update on the chemical constituents of the selected species of Melicope. The study also highlights the anticancer and cytotoxicity properties of the plant extracts and phytochemical constituents from Melicope species. Furthermore, the molecular mechanisms underlying the anticancer effects are elucidated. Overall, this review contributes to understanding the significant pharmacological potential of Melicope species and unlocking their chemical composition, emphasizing their relevance in the development of therapeutic agents, particularly in the field of cancer research.


Assuntos
Rutaceae , Humanos , Rutaceae/química , Medicina Tradicional , Etnofarmacologia , Extratos Vegetais , Compostos Fitoquímicos/química , Fitoterapia
3.
J Biomol Struct Dyn ; : 1-16, 2023 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-37916669

RESUMO

Diabetes affects millions globally and poses treatment challenges. Targeting the enzyme fructose-1,6-bisphosphatase (FBPase) in gluconeogenesis and exploring plant-based therapies offer potential solutions for improving diabetes management while supporting sustainability and medicinal advancements. Utilizing pineapple (Ananas comosus L. Merr.) waste as a source of drug precursors could be valuable for health and environmental care due to its medicinal benefits and abundant yearly biomass production. Therefore, this study conducted a virtual screening to identify potential natural compounds from pineapple that could inhibit FBPase activity. A total of 112 compounds were screened for drug-likeness and ADMET properties, and molecular docking simulations were performed on 20 selected compounds using blind docking. The lead compound, butane-2,3-diyl diacetate, was subjected to 100 ns MD simulations, revealing a binding energy of -5.4 kcal/mol comparable to metformin (-5.6 kcal/mol). The MD simulation also confirmed stable complexes with crucial hydrogen bonds. Glu20, Ala24, Thr27, Gly28, Glu29, Leu30, Val160, Met177, Asp178, and Cys179 were identified as key amino acids that stabilized the human liver FBPase-butane-2,3-diyl diacetate complex, while Tyr215 and Asp218 played a crucial role in the human liver FBPase-Metformin complex. Our study indicates that the lead compound has high intestinal solubility. Therefore, it would show rapid bloodstream distribution and effective action on the target protein, making butane-2,3-diyl diacetate a potential antidiabetic drug candidate. However, further investigations in vitro, preclinical, and clinical trials are required to thoroughly assess its efficacy and safety.Communicated by Ramaswamy H. Sarma.

4.
Biosensors (Basel) ; 13(7)2023 Jun 22.
Artigo em Inglês | MEDLINE | ID: mdl-37504070

RESUMO

An amperometric enzyme-free hydrogen peroxide (H2O2) sensor was developed by catalytically stabilizing active gold nanoparticles (Au NPs) of 4-5 nm on a porous titanium dioxide nanotube (TiO2 NTs) electrode. The Au NPs were homogeneously distributed on anatase TiO2 NTs with an outer diameter of ~102 nm, an inner diameter of ~60 nm, and a wall of thickness of ~40 nm. The cyclic voltammogram of the composite electrode showed a pair of redox peaks characterizing the electrocatalytic reduction of H2O2. The entrapping of Au NPs on TiO2 NTs prevented aggregation and facilitated good electrical conductivity and electron transfer rate, thus generating a wide linear range, a low detection limit of ~104 nM, and high sensitivity of ~519 µA/mM, as well as excellent selectivity, reproducibility, repeatability, and stability over 60 days. Furthermore, excellent recovery and relative standard deviation (RSD) were achieved in real samples, which were tap water, milk, and Lactobacillus plantarum bacteria, thereby verifying the accuracy and potentiality of the developed nonenzymatic sensor.


Assuntos
Nanopartículas Metálicas , Nanotubos , Ouro , Peróxido de Hidrogênio , Reprodutibilidade dos Testes , Técnicas Eletroquímicas , Titânio , Eletrodos , Limite de Detecção
5.
Cancers (Basel) ; 15(7)2023 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-37046789

RESUMO

Despite significant therapeutic advancements for cancer, an atrocious global burden (for example, health and economic) and radio- and chemo-resistance limit their effectiveness and result in unfavorable health consequences. Natural compounds are generally considered safer than synthetic drugs, and their use in cancer treatment alone, or in combination with conventional therapies, is increasingly becoming accepted. Interesting outcomes from pre-clinical trials using Baicalein in combination with conventional medicines have been reported, and some of them have also undergone clinical trials in later stages. As a result, we investigated the prospects of Baicalein, a naturally occurring substance extracted from the stems of Scutellaria baicalensis Georgi and Oroxylum indicum Kurz, which targets a wide range of molecular changes that are involved in cancer development. In other words, this review is primarily driven by the findings from studies of Baicalein therapy in several cancer cell populations based on promising pre-clinical research. The modifications of numerous signal transduction mechanisms and transcriptional agents have been highlighted as the major players for Baicalein's anti-malignant properties at the micro level. These include AKT serine/threonine protein kinase B (AKT) as well as PI3K/Akt/mTOR, matrix metalloproteinases-2 & 9 (MMP-2 & 9), Wnt/-catenin, Poly(ADP-ribose) polymerase (PARP), Mitogen-activated protein kinase (MAPK), NF-κB, Caspase-3/8/9, Smad4, Notch 1/Hes, Signal transducer and activator of transcription 3 (STAT3), Nuclear factor erythroid 2-related factor 2 (Nrf2)/Kelch-like ECH-associated protein-1 (Keap 1), Adenosine monophosphate-activated protein kinase (AMPK), Src/Id1, ROS signaling, miR 183/ezrin, and Sonic hedgehog (Shh) signaling cascades. The promise of Baicalein as an anti-inflammatory to anti-apoptotic/anti-angiogenic/anti-metastatic medicinal element for treating various malignancies and its capability to inhibit malignant stem cells, evidence of synergistic effects, and design of nanomedicine-based drugs are altogether well supported by the data presented in this review study.

6.
Saudi Pharm J ; 31(3): 410-416, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36744104

RESUMO

Introduction: Grit is proposed as an essential trait for academic achievement. Thus, evaluating its current status and the associated factors could aid academic support planning. Objective: The present study aimed to assess grit level and its related factors among undergraduate pharmacy students from 14 countries amid the COVID-19 pandemic. Methods: A cross-sectional survey-based study was conducted among pharmacy students from 14 countries in Asia and the Middle East. A 31-item questionnaire was developed, validated, and pilot-tested, including the validated short scale for grit assessment. The data was collected between 1 February and 15 April 2022. Descriptive and inferential statistics were employed as appropriate. Results: A total of 2665 responses were received, mainly from females (68.7 %), living in urban areas (69.2 %) and studying at private universities (59.1 %). The average grit score on a scale of 5 was 3.15 ± 0.54. The responses revealed higher favourable responses to items on the perseverance of efforts (34.9 % to 54 %) compared to items on the consistency of interests (26.5 % to 31.1 %). Students who did not exercise (AOR: 0.47, 95 %CI: 0.33-0.67) or exercised irregularly (AOR: 0.64, 95 %CI: 0.45-0.90) were less likely to have higher grit scores than those who exercised regularly. Additionally, students who did not receive COVID-19 vaccination (AOR: 0.50, 95 %CI: 0.36-0.71) or received only one dose (AOR: 0.67, 95 %CI: 0.46-0.99) were less likely to have higher grit scores than those who received their booster vaccination. Interestingly, students who chose the pharmacy program as their only available or reasonable choice (AOR: 0.33, 95 %CI: 0.17-0.62) and students from public universities (AOR: 0.82, 95 %CI: 0.68-0.98) were less likely to have higher grit scores. On the other hand, students who did not face educational challenges with online learning (AOR: 1.19, 95 %CI: 1.003-1.416) and students with excellent (AOR: 2.28, 95 %CI: 1.57-3.31) and very good (AOR: 2.16, 95 %CI: 1.53-3.04) academic performance were more likely to have higher grit scores. Conclusion: The findings revealed moderate grit levels. Higher grit levels were thought to be associated with several personal, lifestyle and academic factors. Further interventions to support students' grit attributes are required, particularly concerning the consistency of interests.

7.
J Biomol Struct Dyn ; 41(21): 12186-12203, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36645141

RESUMO

Dengue fever is a significant public health concern throughout the world, causing an estimated 500,000 hospitalizations and 20,000 deaths each year, despite the lack of effective therapies. The DENV-2 RdRp has been identified as a potential target for the development of new and effective dengue therapies. This research's primary objective was to discover an anti-DENV inhibitor using in silico ligand- and structure-based approaches. To begin, a ligand-based pharmacophore model was developed, and 130 distinct natural products (NPs) were screened. Docking of the pharmacophore-matched compounds were performed to the active site of DENV-2 RdRp protease . Eleven compounds were identified as potential DENV-2 RdRp inhibitors based on docking energy and binding interactions. ADMET and drug-likeness were done to predict their pharmacologic, pharmacokinetic, and drug-likeproperties . Compounds ranked highest in terms of pharmacokinetics and drug-like appearances were then subjected to additional toxicity testing to determine the leading compound. Additionally, MD simulation of the lead compound was performed to confirm the docked complex's stability and the binding site determined by docking. As a result, the lead compound (compound-108) demonstrated an excellent match to the pharmacophore, a strong binding contact and affinity for the RdRp enzyme, favourable pharmacokinetics, and drug-like characteristics. In summary, the lead compound identified in this study could be a possible DENV-2 RdRp inhibitor that may be further studied on in vitro and in vivo models to develop as a drug candidate.Communicated by Ramaswamy H. Sarma.


Assuntos
Produtos Biológicos , Farmacóforo , Simulação de Acoplamento Molecular , Produtos Biológicos/farmacologia , Ligantes , RNA Polimerase Dependente de RNA , Simulação de Dinâmica Molecular
8.
J Biomol Struct Dyn ; 41(19): 9756-9769, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-36399018

RESUMO

Antimicrobial drug resistance (AMR) is a severe global threat to public health. The increasing emergence of drug-resistant bacteria requires the discovery of novel antibacterial agents. Quinoline derivatives have previously been reported to exhibit antimalarial, antiviral, antitumor, antiulcer, antioxidant and, most interestingly, antibacterial properties. In this study, we evaluated the binding affinity of three newly designed hydroxyquinolines derived from sulfanilamide (1), 4-amino benzoic acid (2) and sulfanilic acid (3) towards five bacterial protein targets (PDB ID: 1JIJ, 3VOB, 1ZI0, 6F86, 4CJN). The three derivatives were designed considering the amino acid residues identified at the active site of each protein involved in the binding of each co-crystallized ligand and drug-likeness properties. The ligands displayed binding energy values with the target proteins ranging from -2.17 to -8.45 kcal/mol. Compounds (1) and (3) showed the best binding scores towards 1ZI0/3VOB and 1JIJ/4CJN, respectively, which may serve as new antibiotic scaffolds. Our in silico results suggest that sulfanilamide (1) or sulfanilic acid (3) hydroxyquinoline derivatives have the potential to be developed as bacterial inhibitors, particularly MRSA inhibitors. But before that, it must go through the proper preclinical and clinical trials for further scientific validation. Further experimental studies are warranted to explore the antibacterial potential of these compounds through preclinical and clinical studies.Communicated by Ramaswamy H. Sarma.


Assuntos
Hidroxiquinolinas , Simulação de Dinâmica Molecular , Proteínas de Bactérias , Oxiquinolina/farmacologia , Antibacterianos/farmacologia , Sulfanilamida , Hidroxiquinolinas/farmacologia , Inibidores de Proteases , Simulação de Acoplamento Molecular
9.
Front Public Health ; 10: 1011376, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36388263

RESUMO

Background: Pharmacy students will assume future roles as frontline healthcare providers. Therefore, evaluating their current state of mental wellbeing and its associated factors is essential for better planning students' support initiatives. This study aimed to assess mental wellbeing and its associated factors among undergraduate pharmacy students from 14 countries during the pandemic. Methods: A cross-sectional study was conducted among undergraduate pharmacy students in 14 countries in Asia and the Middle East. The validated Warwick-Edinburgh Mental Wellbeing Scale (the 14-item WEMWBS) was adopted to assess mental wellbeing. Data collection was performed online between February and April 2022. Descriptive and inferential statistics were used as appropriate. Results: A total of 2,665 responses were received, mainly from females (68.7%) with a higher presence of private universities (59.1%). About 34.9% had low mental wellbeing levels, while 57 and 8.1% had medium, and high levels, respectively. Binary logistic regression showed that males (AOR: 1.34; CI 95%: 1.11-1.61; p < 0.01) and students with no chronic illnesses (AOR: 2.01; CI 95%: 1.45-2.80; p < 0.001) were more likely to have higher mental wellbeing. Also, participants who did not engage in any exercise (AOR: 0.71; CI 95%: 0.52-0.98; p = 0.04) and those in public universities (AOR: 0.82; CI 95%: 0.69-0.97; p = 0.02) were less likely to have higher mental wellbeing. Additionally, students who had interest/passion for pharmacy (AOR: 1.69; CI 95%: 1.07-2.68; p = 0.02), and those who known pharmacists inspired (AOR: 1.81; CI 95%: 1.06-3.12; p = 0.03), were more likely to have higher mental wellbeing compared with those who had no specific reason for their choice to study pharmacy. The participants with excellent (AOR: 1.87; CI 95%: 1.29-2.70; p = 0.001) or very good self-reported academic performance (AOR: 1.57; CI 95%: 1.12-2.22; p = 0.01) were more likely to have higher mental wellbeing compared to those with fair academic performance. Conclusion: More than a third of the participants had low mental wellbeing. Various demographic, lifestyle, medical and academic factors appeared to affect students' mental wellbeing. Careful consideration of these factors and their integration into the pharmacy schools' plans for student support services and academic advising would be essential to improve students' mental wellbeing.


Assuntos
Estudantes de Farmácia , Masculino , Feminino , Humanos , Estudos Transversais , Universidades , Saúde Mental , Estilo de Vida
10.
Artigo em Inglês | MEDLINE | ID: mdl-36231312

RESUMO

The COVID-19 pandemic globally impacted physical, spiritual, and mental health (MH). The consequences significantly affected students' quality of life (QoL) too. This cross-sectional study assessed MH status and its relationship to the QoL of college students in Indonesia. This study collected data (September 2021-April 2022) online using the depression, anxiety, and stress scale-21 (DASS-21) to measure MH and the world health organization quality-of-life scale (WHOQoL-BREF) to measure the QoL. The data were analysed using SPSS with a bivariate and multivariate linear regression test. A total of 606 respondents participated in this study, with the majority being women (81.0%), aged 21-27 years (44.3%), and unmarried (98.5%) respondents. We observed 24.4% (n = 148) moderate depression, 18.3% (n = 111) very severe anxiety, and 21.1% (n = 128) moderate stress status. The QoL measurement determined that a moderate QoL in the physical and environmental health domains (>70%) and poor QoL in the psychological health domain (58.3%) were found. Gender, age, family support, history of COVID-19 diagnosis, family with COVID-19 diagnosis, vaccination status, and physical symptoms are significantly associated with MH status and QoL (p-value < 0.05). This study demonstrated that COVID-19 was negatively related to college students' MH and QoL. Targeted interventions may be needed to ameliorate both MH and QoL.


Assuntos
COVID-19 , Qualidade de Vida , COVID-19/epidemiologia , Teste para COVID-19 , Estudos Transversais , Surtos de Doenças , Feminino , Humanos , Indonésia/epidemiologia , Masculino , Saúde Mental , Pandemias , Qualidade de Vida/psicologia , Estudantes/psicologia , Inquéritos e Questionários
11.
Molecules ; 27(20)2022 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-36296655

RESUMO

Chalcones have been well examined in the extant literature and demonstrated antibacterial, antifungal, anti-inflammatory, and anticancer properties. A detailed evaluation of the purported health benefits of chalcone and its derivatives, including molecular mechanisms of pharmacological activities, can be further explored. Therefore, this review aimed to describe the main characteristics of chalcone and its derivatives, including their method synthesis and pharmacotherapeutics applications with molecular mechanisms. The presence of the reactive α,ß-unsaturated system in the chalcone's rings showed different potential pharmacological properties, including inhibitory activity on enzymes, anticancer, anti-inflammatory, antibacterial, antifungal, antimalarial, antiprotozoal, and anti-filarial activity. Changing the structure by adding substituent groups to the aromatic ring can increase potency, reduce toxicity, and broaden pharmacological action. This report also summarized the potential health benefits of chalcone derivatives, particularly antimicrobial activity. We found that several chalcone compounds can inhibit diverse targets of antibiotic-resistance development pathways; therefore, they overcome resistance, and bacteria become susceptible to antibacterial compounds. A few chalcone compounds were more active than conventional antibiotics, like vancomycin and tetracycline. On another note, a series of pyran-fused chalcones and trichalcones can block the NF-B signaling complement system implicated in inflammation, and several compounds demonstrated more potent lipoxygenase inhibition than NSAIDs, such as indomethacin. This report integrated discussion from the domains of medicinal chemistry, organic synthesis, and diverse pharmacological applications, particularly for the development of new anti-infective agents that could be a useful reference for pharmaceutical scientists.


Assuntos
Anti-Infecciosos , Antimaláricos , Chalcona , Chalconas , Chalcona/farmacologia , Chalconas/farmacologia , Chalconas/química , Antifúngicos/farmacologia , Vancomicina , Antimaláricos/farmacologia , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Antibacterianos/farmacologia , Antibacterianos/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios não Esteroides/farmacologia , Indometacina , Preparações Farmacêuticas , Lipoxigenases , Tetraciclinas , Relação Estrutura-Atividade
12.
Curr Issues Mol Biol ; 44(9): 3905-3922, 2022 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-36135180

RESUMO

Chondroitin sulphate (CS) is one of the most predominant glycosaminoglycans (GAGs) available in the extracellular matrix of tissues. It has many health benefits, including relief from osteoarthritis, antiviral properties, tissue engineering applications, and use in skin care, which have increased its commercial demand in recent years. The quest for CS sources exponentially increased due to several shortcomings of porcine, bovine, and other animal sources. Fish and fish wastes (i.e., fins, scales, skeleton, bone, and cartilage) are suitable sources of CS as they are low cost, easy to handle, and readily available. However, the lack of a standard isolation and characterization technique makes CS production challenging, particularly concerning the yield of pure GAGs. Many studies imply that enzyme-based extraction is more effective than chemical extraction. Critical evaluation of the existing extraction, isolation, and characterization techniques is crucial for establishing an optimized protocol of CS production from fish sources. The current techniques depend on tissue hydrolysis, protein removal, and purification. Therefore, this study critically evaluated and discussed the extraction, isolation, and characterization methods of CS from fish or fish wastes. Biosynthesis and pharmacological applications of CS were also critically reviewed and discussed. Our assessment suggests that CS could be a potential drug candidate; however, clinical studies should be conducted to warrant its effectiveness.

13.
PLoS One ; 17(8): e0273209, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36006935

RESUMO

BACKGROUND: Proper disaster preparedness by community pharmacists has the potential to counter many of the factors that cause threats and high-risk outcomes. Their preparedness and awareness may also help health practitioners and governments to improve disaster response planning. OBJECTIVES: This aims to explore the knowledge, attitude, and practice (KAP) towards disaster medicine preparedness and readiness among community pharmacists in the United Arab Emirates (UAE). METHOD: A cross-sectional study was conducted over the ten months among licensed community pharmacists who had three months' professional experience or more. Face-to-face interviews were carried out and a structured questionnaire was used for data collection. Logistic regression models were used to determine the factors influencing aboucine preparedness and readiness. SPSS Version 24 was used to analyze the data collected. RESULTS: A total of 500 community pharmacists participated in the study. The average knowledge score was 25.6% with a 95% confidence interval (CI) of [21.7%, 29.4%]. Better knowledge scores were observed in the male gender (OR 2.43; 95% CI 1.05-3.72), participants aged ≥ 31 years old (OR 2.97; 95% CI 1.16-7.6), postgraduates (OR 4.36; 95% CI 2.6-7.3), participants from independent Pharmacies (OR 6.5; 95% CI 4.04-10.4 3), chief pharmacists (OR 3.1; 95% CI 1.86-5.07), participants with 16 years and more experience years (OR 2.42; 95% CI 1.063-5.522) and participants who graduated from regional/international universities (OR 5.92; 95% CI 2.65-13.2). Better attitude and practice about disaster medicine preparedness were observed in postgraduates (OR 2.54; 95% CI 1.26-pharmacists from independent pharmacies (OR 1.35; 95% CI 2.43-2,.66), and chief pharmacists (OR 1.26; 95% CI 1.17-1.35). CONCLUSIONS: It's essential to provide a continuing education program using different educational strategies urgently needed to improve community pharmacy competencies (e.g. knowledge attitudes, and perceptions) to improve the skills and practices regarding disaster medicine preparedness and readiness.


Assuntos
Serviços Comunitários de Farmácia , Medicina de Desastres , Adulto , Atitude do Pessoal de Saúde , Estudos Transversais , Conhecimentos, Atitudes e Prática em Saúde , Humanos , Masculino , Farmacêuticos , Inquéritos e Questionários , Emirados Árabes Unidos
14.
Front Pharmacol ; 13: 865801, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35846992

RESUMO

Colorectal cancer (CRC) is the second most deadly cancer worldwide. CRC management is challenging due to late detection, high recurrence rate, and multi-drug resistance. Herbs and spices used in cooking, practised for generations, have been shown to contain CRC protective effect or even be useful as an anti-CRC adjuvant therapy when used in high doses. Herbs and spices contain many bioactive compounds and possess many beneficial health effects. The chemopreventive properties of these herbs and spices are mainly mediated by the BCL-2, K-ras, and MMP pathways, caspase activation, the extrinsic apoptotic pathway, and the regulation of ER-stress-induced apoptosis. As a safer natural alternative, these herbs and spices could be good candidates for chemopreventive or chemotherapeutic agents for CRC management because of their antiproliferative action on colorectal carcinoma cells and inhibitory activity on angiogenesis. Therefore, in this narrative review, six different spices and herbs: ginger (Zingiber officinale Roscoe), turmeric (Curcuma longa L.), garlic (Allium sativum L.), fenugreek (Trigonella foenum-graecum L.), sesame (Sesamum indicum L.), and flaxseed (Linum usitatissimum L.) used in daily cuisine were selected for this study and analyzed for their chemoprotective or chemotherapeutic roles in CRC management with underlying molecular mechanisms of actions. Initially, this study comprehensively discussed the molecular basis of CRC development, followed by culinary and traditional uses, current scientific research, and publications of selected herbs and spices on cancers. Lead compounds have been discussed comprehensively for each herb and spice, including anti-CRC phytoconstituents, antioxidant activities, anti-inflammatory properties, and finally, anti-CRC effects with treatment mechanisms. Future possible works have been suggested where applicable.

15.
Cancers (Basel) ; 14(7)2022 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-35406504

RESUMO

Colorectal cancer (CRC) is the second most deadly cancer. Global incidence and mortality are likely to be increased in the coming decades. Although the deaths associated with CRC are very high in high-income countries, the incidence and fatalities related to CRC are growing in developing countries too. CRC detected early is entirely curable by surgery and subsequent medications. However, the recurrence rate is high, and cancer drug resistance increases the treatment failure rate. Access to early diagnosis and treatment of CRC for survival is somewhat possible in developed countries. However, these facilities are rarely available in developing countries. Highlighting the current status of CRC, its development, risk factors, and management is crucial in creating public awareness. Therefore, in this review, we have comprehensively discussed the current global epidemiology, drug resistance, challenges, risk factors, and preventive and treatment strategies of CRC. Additionally, there is a brief discussion on the CRC development pathways and recommendations for preventing and treating CRC.

16.
Cell Mol Biol (Noisy-le-grand) ; 68(9): 1-13, 2022 09 30.
Artigo em Inglês | MEDLINE | ID: mdl-36905282

RESUMO

Piper betle L. leaves are very popular and traditionally used to chew with betel nut in many Asian countries. In this study, P. betle leaves juice (PBJ) was subjected to evaluation for its antihyperlipidemic activity in the high-fat-diet-induced hyperlipidemic rats model. Swiss albino rats were allowed to high-fat- diet for one month, followed by concurrent administration of PBJ for another month. The rats were then sacrificed and collected blood, tissues and organs. Pharmacokinetic, toxicological studies and molecular docking studies were performed using SwissADME, admetSAR and schrodinger suit-2017. Our investigation showed a promising effect of PBJ on body weight, lipid profile, oxidative and antioxidative enzymes, and the principle enzyme responsible for the synthesis of cholesterol. PBJ at 0.5 - 3.0 mL/rat significantly reduced body weight of hyperlipidemic rats compared to control. PBJ at the doses of 1.0, 1.5, 2.0, and 3.0 mL/rat significantly (p<0.05, p<0.01, p<0.001) improved the levels of TC, LDL-c, TG, HDL-c and VLDL-c. Similarly, PBJ doses starting from 1.0 mL/rat to 3.0 mL/rat reduced the oxidative biomarkers AST, ALT, ALP, and creatinine. The level of HMG-CoA was significantly reduced by PBJ doses 1.5, 2, and 3 ml/rat. A number of compounds have been found to have good pharmacokinetic profile and safety and 4-coumaroylquinic acid exerted the best docking score among them. Thus our findings clearly demonstrated the potential lipid-lowering activities of PBJ both in vivo and in silico studies. PBJ can be a good candidate for the development of antihyperlipidemic medication or as an alternative medicine.


Assuntos
Hipolipemiantes , Estresse Oxidativo , Piper betle , Ratos , Peso Corporal , Colesterol , Dieta Hiperlipídica , Hipolipemiantes/farmacologia , Fígado/metabolismo , Simulação de Acoplamento Molecular
17.
Biomed Pharmacother ; 143: 112182, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34649338

RESUMO

Nigella sativa L. is one of the most extensively used traditional medicinal plants. This widely studied plant is known to display diverse pharmacological actions, including antimicrobial activities. Current literature has documented its multi-target mode of antimicrobial actions. N. sativa or its bioactive compounds, such as thymoquinone, can induce oxidative stress, cell apoptosis (by producing reactive oxygen species), increase membrane permeability, inhibit efflux pumps, and impose strong biocidal actions. Despite its well-documented antimicrobial efficacy in the experimental model, to the best of our knowledge its antimicrobial mechanisms highlighting the multi-targeting properties have yet to be well discussed. Is N. sativa or thymoquinone a valuable lead compound for therapeutic development for infectious diseases? Are N. sativa's bioactive compounds potential antimicrobial agents or able to overcome antimicrobial resistance? This review aims to discuss the antimicrobial pharmacology of N. sativa-based treatments. Additionally, it provides a holistic overview of the ethnobotany, ethnopharmacology, and phytochemistry of N. sativa.


Assuntos
Anti-Infecciosos/farmacologia , Etnobotânica , Nigella sativa , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/toxicidade , Resistência Microbiana a Medicamentos , Humanos , Nigella sativa/química , Segurança do Paciente , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/toxicidade , Fitoterapia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Medição de Risco , Sementes
18.
Life (Basel) ; 11(8)2021 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-34440569

RESUMO

Neurodegenerative diseases (NDs) extend the global health burden. Consumption of alcohol as well as maternal exposure to ethanol can damage several neuronal functions and cause cognition and behavioral abnormalities. Ethanol induces oxidative stress that is linked to the development of NDs. Treatment options for NDs are yet scarce, and natural product-based treatments could facilitate ND management since plants possess plenty of bioactive metabolites, including flavonoids, which typically demonstrate antioxidant and anti-inflammatory properties. Hypericum oblongifolium is an important traditional medicinal plant used for hepatitis, gastric ulcer, external wounds, and other gastrointestinal disorders. However, it also possesses multiple bioactive compounds and antioxidant properties, but the evaluation of isolated pure compounds for neuroprotective efficacy has not been done yet. Therefore, in the current study, we aim to isolate and characterize the bioactive flavonoid folecitin and evaluate its neuroprotective activity against ethanol-induced oxidative-stress-mediated neurodegeneration in the hippocampus of postnatal day 7 (PND-7) rat pups. A single dose of ethanol (5 g/kg body weight) was intraperitoneally administered after the birth of rat pups on PND-7. This caused oxidative stress accompanied by the activation of phosphorylated-c-Jun N-terminal kinase (p-JNK), nod-like receptor family pyrin domain containing 3 (NLRP3), apoptosis-associated speck-like protein (ASC), and cysteine-aspartic acid protease-1 (caspase-1) proteins to form a complex called the NLRP3-inflammasome, which converts pro-interleukin 1 beta (IL-1B) to activate IL-1B and induce widespread neuroinflammation and neurodegeneration. In contrast, co-administration of folecitin (30 mg/kg body weight) reduced ethanol-induced oxidative stress, inhibited p-JNK, and deactivated the NLRP3-inflammasome complex. Furthermore, folecitin administration reduced neuroinflammatory and neurodegenerative protein markers, including decreased caspase-3, BCL-2-associated X protein (BAX), B cell CLL/lymphoma 2 (BCL-2), and poly (ADP-ribose) polymerase-1 (PARP-1) expression in the immature rat brain. These findings conclude that folecitin is a flavone compound, and it might be a novel, natural and safe agent to curb oxidative stress and its downstream harmful effects, including inflammasome activation, neuroinflammation, and neurodegeneration. Further evaluation in a dose-dependent manner would be worth it in order to find a suitable dose regimen for NDs.

19.
Artigo em Inglês | MEDLINE | ID: mdl-34444015

RESUMO

Misuse and overuse of antibiotics are potential causes of the increasing prevalence of antibiotic resistance (ABR). Having information about the knowledge, attitude, and practices concerning antibiotics use by the public might help control ABR growth. Therefore, this cross-sectional study aimed to investigate the levels and associated factors of knowledge, attitude, and practice (KAP) of antibiotics use among the public. A questionnaire was designed and validated, which consisted of a total of 51 questions with four sections: demographics (6), knowledge (20), attitude (12), and practice (13) to measure KAP. Univariate analysis (using Mann-Whitney U and Kruskal-Wallis analysis) was applied to assess the differences in the mean scores of KAP. Linear regression analysis was performed to identify factors associated with KAP. Finally, using Spearman analysis we have examined the correlation between responses to the KAP. The sample size of this study was 575, with a 99.96% response rate. Regarding knowledge, 73.12% of respondents stated that antibiotics could be used to treat viral infections, and 63.35% of respondents answered that antibiotics could reduce fever. Concerning attitude, 50% of respondents had considered stopping taking antibiotics as soon as symptoms had disappeared. In analyzing practice, we found 40% of respondents obtained antibiotics from a pharmacy without a prescription from a physician, a nurse, or a midwife. Statistical analysis revealed that KAP about antibiotic use was significantly associated with gender, area of residence, level of education, and monthly income (p < 0.05). Our findings concluded that men, respondents with low income, those with low-level education, and those living in rural areas are more prone to excessive use of antibiotics without knowing the adverse effects of improper use and how it can contribute to high ABR. So it is urgently necessary to strengthen policies on antibiotics use, including drug provision, distribution, and sales. In addition, people with low KAP should be a priority consideration in education outreach initiatives.


Assuntos
Antibacterianos , Conhecimentos, Atitudes e Prática em Saúde , Antibacterianos/uso terapêutico , Estudos Transversais , Humanos , Indonésia , Masculino , Inquéritos e Questionários
20.
Front Physiol ; 7: 540, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27899897

RESUMO

The increased use of tissue expander in the past decades and its potential market values in near future give enough reasons to sum up the consequences of tissue expansion. Furthermore, the patients have the right to know underlying mechanisms of adaptation of inserted biomimetic, its bioinspired materials and probable complications. The mechanical strains during tissue expansion are related to several biological phenomena. Tissue remodeling during the expansion is highly regulated and depends on the signal transduction. Any alteration may lead to tumor formation, necrosis and/or apoptosis. In this review, stretch induced cell proliferation, apoptosis, the roles of growth factors, stretch induced ion channels, and roles of second messengers are organized. It is expected that readers from any background can understand and make a decision about tissue expansion.

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