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1.
Cureus ; 16(6): e62794, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-39040717

RESUMO

INTRODUCTION: Diabetes mellitus (DM) poses a significant global health challenge, with its prevalence steadily increasing. Natural compounds derived from plants have garnered attention for their potential therapeutic effects in managing this metabolic disorder. Camellia sinensis, commonly known as tea, is rich in bioactive compounds exhibiting various pharmacological properties. This study investigates the potential anti-diabetic activity of C. sinensis leaf extract through in vitro analysis. MATERIALS AND METHODS: Camella sinensis leaf extract was prepared by grinding the plant's leaf into a powder, mixing it with distilled water, and heating. The antidiabetic activity was assessed through α-Amylase and α-Glucosidase inhibitory assays, employing varying concentrations of the plant extract. Molecular docking analysis utilized Autodock 1.5.6 software (The Scripps Research Institute, California, US) to predict ligand-receptor interactions, guiding subsequent experimental validation. RESULT: Camella sinensis leaf extract exhibited high phenolic content, suggesting potential in managing hyperglycemia. Tannins may aid glucose absorption and inhibit adipogenesis, making them promising for non-insulin-dependent DM (NIDDM). Terpenoids, with antioxidant activity, inhibit advanced glycation. Saponins and steroids were absent. Molecular docking revealed residues like IR, IRS1, and AS160 with significant impact on α-Amylase and α-Glucosidase, comparable to metformin. CONCLUSION: The findings of this study highlight the promising potential of C. sinensis leaf extract in managing hyperglycemia associated with DM. The high phenolic content aids in glucose regulation. Specifically, the presence of tannins suggests a potential role in modulating glucose absorption and inhibiting adipogenesis, which could be particularly beneficial for individuals with NIDDM. These findings provide valuable insights into the molecular mechanisms underlying the potential therapeutic efficacy of C. sinensis leaf extract against DM, paving the way for further research and development of novel therapeutic interventions in diabetes management.

2.
Ageing Res Rev ; 99: 102393, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38925479

RESUMO

Alzheimer's disease (AD) stands as a formidable challenge in modern medicine, characterized by progressive neurodegeneration, cognitive decline, and memory impairment. Despite extensive research, effective therapeutic strategies remain elusive. The antioxidant, anti-inflammatory, and neuroprotective properties of curcumin, found in turmeric, have demonstrated promise. The poor bioavailability and rapid systemic clearance of this drug limit its clinical application. This comprehensive review explores the potential of curcumin-loaded polymeric nanomaterials as an innovative therapeutic avenue for AD. It delves into the preparation and characteristics of diverse polymeric nanomaterial platforms, including liposomes, micelles, dendrimers, and polymeric nanoparticles. Emphasis is placed on how these platforms enhance curcumin's bioavailability and enable targeted delivery to the brain, addressing critical challenges in AD treatment. Mechanistic insights reveal how these nanomaterials modulate key AD pathological processes, including amyloid-beta aggregation, tau phosphorylation, oxidative stress, and neuroinflammation. The review also highlighted the preclinical studies demonstrate reduced amyloid-beta plaques and neuroinflammation, alongside improved cognitive function, while clinical trials show promise in enhancing curcumin's bioavailability and efficacy in AD. Additionally, it addresses the challenges of clinical translation, such as regulatory issues, large-scale production, and long-term stability. By synthesizing recent advancements, this review underscores the potential of curcumin-loaded polymeric nanomaterials to offer a novel and effective therapeutic approach for AD, aiming to guide future research and development in this field.


Assuntos
Doença de Alzheimer , Curcumina , Nanoestruturas , Curcumina/administração & dosagem , Curcumina/uso terapêutico , Doença de Alzheimer/tratamento farmacológico , Humanos , Animais , Polímeros , Nanopartículas/administração & dosagem , Sistemas de Liberação de Medicamentos/métodos , Fármacos Neuroprotetores/administração & dosagem , Fármacos Neuroprotetores/uso terapêutico , Fármacos Neuroprotetores/farmacologia
3.
J Pharm Bioallied Sci ; 16(Suppl 2): S1304-S1307, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38882735

RESUMO

Objectives: This study presents the antioxidant and anti-inflammatory activity of the ethanolic extract of Euphorbia hirta leaf extract. Materials and Methods: The antioxidant and anti-inflammatory activity of the extract was performed by in vitro assay. Our research employs a comprehensive approach combining experimental assays and computational simulations to assess the extract's potential bioactive components and their interactions with key biomolecules. Results: The study's results demonstrated a progressive rise in the percentage of inhibition, which was dependent on the dosage, in both antioxidant and anti-inflammatory activities. This trend was observed for both the extract and the standard, encompassing concentrations ranging from 100 to 500 µg/ml. Conclusion: The results showed that Euphorbia hirta's possesses antioxidant and anti-inflammatory activity, and this may contribute to a traditional medicinal. The discoveries of this study contribute to a deeper understanding of Euphorbia hirta's medicinal properties and its potential as a source of natural therapeutic agents.

4.
J Pharm Bioallied Sci ; 16(Suppl 2): S1317-S1320, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38882754

RESUMO

Tinospora cordifolia, commonly known as "Giloy" or "Guduchi," is a medicinal plant with a rich history in traditional medicine systems. The aqueous extract of Tinospora cordifolia stems has garnered attention due to its reported pharmacological activities. This study aimed to investigate the in vitro biological properties of the aqueous extract and complement the findings with in silico studies to gain insights into potential molecular interactions. The Tinospora cordifolia stem aqueous extract was subjected to a battery of in vitro assays to assess its biological properties. Anti-inflammatory activity was evaluated using invitro assay. To complement the in vitro findings, in silico studies involving molecular docking analyses were conducted to predict potential interactions between the extract's constituents and relevant biomolecular targets. The in vitro evaluation revealed significant anti-inflammatory activity of the Tinospora cordifolia stem aqueous extract, as evidenced by its ability to suppress the production of pro-inflammatory cytokines. In silico studies provided insights into the molecular interactions between the extract's bioactive constituents and key inflammatory and antioxidant targets, further supporting the observed biological properties. The combined in vitro biological assays and in silico studies offer a comprehensive assessment of the Tinospora cordifolia stem aqueous extract's potential therapeutic properties. The demonstrated anti-inflammatory activities align with the traditional use of Tinospora cordifolia and suggest its potential in managing inflammatory and oxidative stress-related disorders. The in silico insights provide a molecular understanding of the extract's mode of action, strengthening the rationale for further investigation and development of natural products derived from Tinospora cordifolia for pharmaceutical and medicinal applications.

5.
J Pharm Bioallied Sci ; 16(Suppl 2): S1308-S1311, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38882780

RESUMO

Background: Crataeva nurvala, a medicinal plant with potential therapeutic properties, offers a promising avenue for the development of novel anti-inflammatory drugs. This study adopted a combined in silico and in vitro approach to investigate the anti-inflammatory potential of compounds derived from Crataeva nurvala. Materials and Methods: In the in silico phase, virtual screening and molecular docking analyses were conducted to identify bioactive compounds from Crataeva nurvala that could interact with key inflammatory targets. Subsequently, selected compounds were synthesized and subjected to in vitro experimentation. Cellular models were employed to assess the anti-inflammatory effects of Crataeva nurvala-derived compounds, focusing on the modulation of pro-inflammatory cytokine levels and the underlying signaling pathways. Results: Virtual screening and molecular docking led to the identification of several bioactive compounds with favorable interactions with inflammatory targets. In the in vitro experiments, treatment with Crataeva nurvala-derived compounds resulted in a significant reduction in pro-inflammatory cytokine production. Moreover, the compounds exhibited the ability to modulate inflammatory signaling pathways, further substantiating their anti-inflammatory potential. Conclusions: This study not only contributes to the development of effective anti-inflammatory drugs but also underscores the value of harnessing natural sources such as Crataeva nurvala for therapeutic interventions in inflammatory disorders. The dual-phase strategy presented here provides a robust framework for anti-inflammatory drug discovery and validation.

6.
J Pharm Bioallied Sci ; 16(Suppl 2): S1270-S1273, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38882817

RESUMO

Sesuvium portulacastrum, a coastal medicinal plant with traditional uses has shown promising biological activities including anti-inflammatory, antioxidant and antimicrobial properties. However, the mechanisms of action active ingredients of this plant have not been studied. Aim of the current study is to investigate the anticancer activity of Sesuvium portulacastrum using in vitro and in silico analysis. The in vitro assays included NO radical scavenging activity, total phenolic and flavonoid content determination. The data were analysed by one-way-ANOVA and p<0.05 was considered as statistically significant. The phytochemical analysis showed the presence of tannins, steroids, terpenoids and phenols. Antioxidant activity of S. portulacastrum showed the dose dependent effect of nitric oxide radical scavenging activity. In silico analysis showed a better binding affinity with IR, IRS1 and Akt molecules which demonstrated the action of bioactive compound of S. portulacastrum against IRS-1/AKT signalling pathway.

7.
J Pharm Bioallied Sci ; 16(Suppl 2): S1312-S1316, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38882845

RESUMO

Background: Spermacoce hispida, a medicinal plant from the Rubiaceae family, has garnered attention for its traditional use and reported therapeutic properties. This study aimed to investigate the phytochemical composition and assess the anti-inflammatory and anti-oxidant activities of the ethanolic extract derived from Spermacoce hispida. Materials and Methods: Phytochemical screening of the ethanolic extract involved qualitative analysis to identify major phytoconstituents such as tannins, phenols, and acids. The anti-inflammatory activity was evaluated through in vitro assays, and anti-oxidant potential was assessed using established methods to measure scavenging activity against free radicals and reactive oxygen species. Results: Phytochemical screening revealed the presence of various bioactive constituents in the Spermacoce hispida ethanolic extract, including acid, tannin, protein, and phenolic compounds. Furthermore, the extract exhibited potent anti-oxidant activity, as evidenced by its ability to scavenge free radicals and attenuate ROS-induced oxidative stress. Conclusion: The findings of this study underscore the potential of Spermacoce hispida ethanolic extract as a source of bioactive compounds with anti-inflammatory and anti-oxidant properties. The presence of phytochemicals and the observed bioactivity support its traditional use and suggest potential therapeutic applications. These results contribute to the growing body of knowledge on natural products with health-promoting effects and provide a basis for further research aimed at developing pharmaceutical and medicinal interventions harnessing the benefits of Spermacoce hispida.

8.
J Pharm Bioallied Sci ; 16(Suppl 2): S1246-S1248, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38882856

RESUMO

Background: Nowadays, diabetes mellitus has become common worldwide due to changes in lifestyle, sedentary life, alterations in food habits, and other genetic and environmental factors. It is necessary to create awareness about the growing pandemic. Aim: To evaluate the antidiabetic potential of Evolvulus alsinoides. Methods: In vitro α-amylase inhibition and α-glucosidase inhibition activity. Molecular docking analysis. Results: The plant is rich in naturally occurring phytocompound. The results of the study showed that E. alsinoides has the potential to inhibit the activity of alpha-amylase and alpha-glucosidase. Moreover, this result was validated using in silico molecular docking studies that showed a good binding affinity of one of the major phytocompound, caffeic acid, with molecules in the insulin signaling cascade. Conclusion: E. alsinoides has a potent antidiabetic activity and can be further employed in animal and human studies.

9.
J Pharm Bioallied Sci ; 16(Suppl 2): S1291-S1294, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38882866

RESUMO

Diabetes mellitus is a persistent metabolic condition marked by elevated blood glucose levels due to compromised insulin secretion or functionality. The search for natural antidiabetic agents has gained attention due to their potential effectiveness and safety profiles. Sessuvium portulacastrum, a coastal plant, has been traditionally used for various medicinal purposes. This study investigates the antidiabetic potential of Sessuvium portulacastrum aqueous extract by analyzing its inhibitory effects on key enzymes involved in carbohydrate metabolism and exploring its molecular interactions with critical target proteins. The aqueous extract of Sessuvium portulacastrum was prepared and used for in vitro analysis. The reduced activity of the extract against α-amylase and α-glucosidase enzymes, crucial in glucose absorption and postprandial hyperglycemia, was assessed. Molecular docking techniques were employed to explore the potential interactions between active compounds in the extract and diabetes-related proteins, including BAX, GSK3ß, and CADH. The study revealed significant inhibition of both alpha-amylase and alpha-glucosidase enzymes by Sessuvium portulacastrum aqueous extract, indicating its potential to reduce glucose absorption and postprandial hyperglycemia. Moreover, the molecular docking analysis demonstrated strong binding interactions between active compounds in the extract and key proteins involved in diabetes-related pathways, namely apoptotic pathways, glycogen synthesis, and cell adhesion. The findings of this study highlight the promising antidiabetic potential of Sessuvium portulacastrum aqueous extract. Upcoming research should get an attention on isolating and characterizing the active compounds responsible for these effects on antidiabetic therapies from natural sources.

10.
Mol Divers ; 2024 Jun 17.
Artigo em Inglês | MEDLINE | ID: mdl-38884873

RESUMO

Rheumatoid arthritis (RA) is a chronic systemic autoimmune disease that is now potentially lethal and has a significant detrimental influence on people's daily lives by affecting bone joints. Inflammation plays a vital role in this type of autoimmune disorder. In rheumatoid arthritis, long-term production of pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α) and interleukin-1 (IL-1) stimulates the immune system against cells in bone joints and helps to develop the pathogenesis of rheumatoid arthritis. So, while treating rheumatoid arthritis, we need to block these kinds of mechanisms. We employed soxhlet extraction, thin-layer chromatography (TLC), and gas chromatography-mass spectroscopy (GC-MS) to analyze the phytocompound information in E. hirta leaves. Furthermore, our research included in vitro investigations using Western blotting and mRNA expression analysis (TNF-α, IL-1ß, IL-6) to affirm the anti-inflammatory effectiveness of our extract. For identifying the lead-like molecules, virtual screening and molecular dynamics simulations were used. TLC results confirmed the presence of phytocompounds in E. hirta crude through spots. The structure elucidation of the phytocompounds was confirmed by the GC-MS chromatogram. The in vitro outcomes collectively underscore the inhibitory influence of E. hirta on cell proliferation and its capacity to attenuate the expression of TNF- α within THP-1 cells. The results of in silico methodologies confirmed six lead-like molecules. We could conclude that phytocompounds from ethanol leaf crude have effective lead-like molecules against the TNF-α.

11.
Ageing Res Rev ; 99: 102359, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38821418

RESUMO

The intricate origins and diverse symptoms of Alzheimer's disease (AD) pose significant challenges for both diagnosis and treatment. Exosomes and microvesicles, which carry disease-specific cargo from a variety of central nervous system cell types, have emerged as promising reservoirs of biomarkers for AD. Research on the screening of possible biomarkers in Alzheimer's disease using proteomic profiling of EVs is systematically reviewed in this comprehensive review. We highlight key methodologies employed in EV isolation, characterization, and proteomic analysis, elucidating their advantages and limitations. Furthermore, we summarize the evolving landscape of EV-associated biomarkers implicated in AD pathogenesis, including proteins involved in amyloid-beta metabolism, tau phosphorylation, neuroinflammation, synaptic dysfunction, and neuronal injury. The literature review highlights the necessity for robust validation strategies and standardized protocols to effectively transition EV-based biomarkers into clinical use. In the concluding section, this review delves into potential future avenues and technological advancements pivotal in crafting EV-derived biomarkers applicable to AD diagnostics and prognostics. This review contributes to our comprehension of AD pathology and the advancement of precision medicine in neurodegenerative diseases, hinting at a promising era in AD precision medicine.


Assuntos
Doença de Alzheimer , Biomarcadores , Vesículas Extracelulares , Proteômica , Doença de Alzheimer/metabolismo , Doença de Alzheimer/diagnóstico , Humanos , Biomarcadores/metabolismo , Proteômica/métodos , Vesículas Extracelulares/metabolismo , Animais
12.
Cureus ; 16(4): e58091, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38738026

RESUMO

Introduction Osteosarcoma, a malignant bone tumor, poses significant treatment challenges, necessitating the development of alternative therapeutic strategies. Aerva lanata (A. lanata), a medicinal plant with traditional use in various healthcare systems, has anti-cancer properties. This study looks at the oncolytic effect of A. lanata extract on osteosarcoma cell lines (sarcoma osteogenic-Saos2). Aim The aim of this study was to investigate the oncolytic effect of Aerva lanata on Saos2 cell lines through the apoptotic signaling pathway. Materials and methods A. lanata extract was prepared using Soxhlet extraction, and its cytotoxic effects on Saos2 cells were assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Real-time polymerase chain reaction (RT-PCR) analysis of gene activity was used to assess the extract's effect on apoptotic signaling pathways. Results The MTT assay demonstrated a dose-dependent decrease in Saos2 proliferation following treatment with A. lanata extract at concentrations ranging from 50 µg to 200 µg. The standard deviations observed ranged from 1.414 to 7.071. Gene expression analysis revealed that the extract led to a reduction in the messenger ribonucleic acid (mRNA) levels of the anti-apoptotic marker B-cell lymphoma 2 (Bcl2), with standard deviations ranging from 1 to 0.535. Conversely, it induced an increase in the mRNA levels of the tumor suppressor protein p53, with standard deviations ranging from 1 to 1.835. These findings suggest that the extract modulates the apoptotic pathways of the Bcl2 and p53 genes.  Conclusion A. lanata extract exhibits promising anti-cancer activity against Saos2 osteosarcoma cell lines, inducing apoptosis by downregulating Bcl2 and increasing p53. The study's findings suggest that A. lanata may be useful as a natural treatment for osteosarcoma.

13.
Cell Biochem Funct ; 42(4): e4027, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38715184

RESUMO

Bioactive phytocompounds are crucial components in all plants. Since the time of traditional medicine, the utilization of plants has been grounded in the potential of these bioactive compounds to treat or manage specific illnesses. These natural bioactive compounds have sparked growing interest in employing medicinal plants for addressing various conditions, such as inflammatory diseases, diabetes, and cancer. This study focuses on assessing the qualitative phytochemical composition, antioxidant potential, and cytotoxic effects of blueberry (Vaccinium sect. Cyanococcus) extract using three different solvents, namely water, ethanol, and methanol. The extract exhibited notable antioxidant activities, as evidenced by DPPH and H2O2 free radical scavenging assays. The cell viability assay also demonstrated cell growth inhibition in A549 cells. Furthermore, nine specific phytocompounds sourced from existing literature were selected for molecular docking studies against CDK6 and, AMPK key protein kinases which enhance the cancer progression. The molecular docking results also revealed favorable binding scores, with a high score of -9.5 kcal/mol in CDK6 protein and a maximum score of AMPK with targets of -8.8 kcal/mol. The selected phytocompounds' pharmacodynamic properties such as ADMET also supported the study. Furthermore, rutin stated that pre-dominantly present in blueberry plants shows a potent cytotoxicity effect in A549 cells. Functional annotations by bioinformatic analysis for rutin also revealed the strong enrichment in the involvement of PI3K/AKT1/STAT, and p53 signaling pathways. Based on this analysis, the identified rutin and other compounds hold a promising anticancer activity. Overall, the comprehensive evaluation of both in vitro and in silico data suggests that the Vaccinium sect. Cyanococcus extract could serve as a valuable source of pharmaceutical agents and may prove effective in future therapeutic applications.


Assuntos
Mirtilos Azuis (Planta) , Proliferação de Células , Receptores ErbB , Estresse Oxidativo , Extratos Vegetais , Fator de Transcrição STAT3 , Transdução de Sinais , Proteína Supressora de Tumor p53 , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Mirtilos Azuis (Planta)/química , Estresse Oxidativo/efeitos dos fármacos , Fator de Transcrição STAT3/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Células A549 , Transdução de Sinais/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Receptores ErbB/metabolismo , Interleucina-6/metabolismo , Simulação de Acoplamento Molecular , Neoplasias Pulmonares/metabolismo , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/patologia , Sobrevivência Celular/efeitos dos fármacos , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/metabolismo , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais
14.
Curr Med Chem ; 2024 May 16.
Artigo em Inglês | MEDLINE | ID: mdl-38757322

RESUMO

Globally, cardiovascular diseases (CVDs) are the main cause of mortality every year worldwide. CVD health is influenced by various health factors, such as blood pressure, cholesterol levels, and glucose control. The main risk factors include smoking, physical activity, food intake, and body mass index. Around 90% of CVDs could be prevented by controlling these risk factors. Heavy metals are indigenous to the environment of the earth. However, modern lifestyles have led to the exploitation of our environment by unconstrained use of heavy metals. Though heavy metals are essential components, they are hazardous to humans and living systems due to their persistent and non-degradable nature. The mainpurpose of this study is to provide a literature review on the mechanisms of heavy metals, particularly arsenic, lead, and cadmium, that cause cardiovascular diseases. The major mechanism by which heavy metals result in various modalities of cardiovascular disease is the generation of reactive species and the depletionof the antioxidant reserves inside the biological system. The generation of reactive species gradually leads to the activation of various signaling pathways, resulting in either apoptosis or unrestricted cell growth. These unfavorable conditions result in a state when there is an imbalance between reactive species generation and antioxidant activity. Both endogenously present antioxidants and dietary antioxidants are very much essential in regulating the redox potential of the body. They help in the detoxification and excretion of heavy metals and their metabolites in the biological system. Therefore, recognizing the role of heavy metals in cardiovascular health is crucial for developing preventive strategies and interventions aimed at mitigating their adverse effects on human health.

15.
Cureus ; 16(4): e58939, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38800305

RESUMO

Background Heliotropium bacciferum, often known as wild heliotrope or wild quailplant, is a flowering plant from the borage family. This study examines the anti-metastatic impact of H. bacciferum on Michigan Cancer Foundation-7 (MCF-7) breast cancer cells and its ability to disrupt signaling pathways. Aim To explore the anti-metastatic effect of H. bacciferum on the MCF-7 breast cancer cell line. Materials and methods For this research, MCF-7 breast cancer cells were used. Cells were cultured and subjected to 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, as well as gene expression analysis for glycogen synthase kinase 3 beta (GSK3ß), wingless-related integration site 2 (Wnt2), and ß-catenin. The plant extract was tested to determine if it successfully blocked the signalling pathway or not.  Results The MTT test was performed to study the cytotoxic impact of H. bacciferum. At an increasing concentration of 100 µg/mL, the extract inhibited growth by 55%, whereas at 150 µg/mL, it inhibited growth by 52.5%. Maximum inhibition was seen at 150 µg/mL. H. bacciferum suppressed the GSK3ß and Wnt2 signaling pathways in MCF-7 breast cancer cell lines, acting as an anti-metastatic and anticancer agent. The heliotrine compound in H. bacciferum showed high binding energy to metastatic targets such as GSK3ß, Wnt2, and ß-catenin. Moreover, chemical absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties also support the study. Conclusion In this study, we can infer that H. bacciferum has a favourable anticancer impact on MCF-7 breast cancer cell lines and may be utilised as an anticancer drug against breast cancer cells. It can also be further evaluated for different breast cancers and cell lines.

16.
Acta Trop ; 255: 107216, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38636584

RESUMO

According to the World Health Organization, infectious diseases, particularly those caused by multidrug-resistant bacteria (MDR), are projected to claim the lives of 15 million people by 2050. Septicemia carries a higher morbidity and mortality rate than infections caused by susceptible Pseudomonas aeruginosa, and MDR-mediated ocular infections can lead to impaired vision and blindness. To identify and develop a potential drug against MDR P. aeruginosa, we employed in silico reverse genetics-based target mining, drug prioritization, and evaluation. Rare Lipoprotein A (RlpA) was selected as the target protein, and its crystal structure was geometrically optimized. Molecular docking and virtual screening analyses revealed that RlpA exhibits strong binding affinity with 11 compounds. Among these, 3-chlorophthalic acid was evaluated, and subsequent in vitro assays demonstrated significant anti-Pseudomonas activity with negligible cytotoxicity. The compound was further evaluated against both drug-susceptible and MDR P. aeruginosa strains in vitro, with cytotoxicity assessed using an MTT assay. The study demonstrated that 3-chlorophthalic acid exhibits potent anti-Pseudomonas activity with minimal toxicity to host cells. Consequently, this compound emerges as a promising candidate against MDR P. aeruginosa, warranting further investigation.


Assuntos
Antibacterianos , Farmacorresistência Bacteriana Múltipla , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Pseudomonas aeruginosa , Pseudomonas aeruginosa/efeitos dos fármacos , Antibacterianos/farmacologia , Antibacterianos/química , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Humanos , Lipoproteínas/farmacologia , Lipoproteínas/genética , Lipoproteínas/química , Infecções por Pseudomonas/tratamento farmacológico , Infecções por Pseudomonas/microbiologia
17.
Odontology ; 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38619695

RESUMO

Oral premalignant disorders (OPMDs) are a group of potentially malignant conditions that pose a significant health burden globally. MicroRNAs (miRNAs), small non-coding RNA molecules, have emerged as crucial regulators of gene expression and have been implicated in various biological processes, including carcinogenesis. This review synthesizes existing knowledge to provide a comprehensive understanding of the molecular mechanisms underlying OPMDs and to highlight the potential of miRNAs as promising biomarkers and therapeutic targets. Additionally, this review seeks to explore the potential of miRNA-based diagnostic biomarkers for early detection of OPMDs in the current literature on miRNAs in OPMDs, examining their involvement in disease pathogenesis, diagnostic potential, and therapeutic implications. Dysregulated miRNAs can target genes involved in critical cellular processes, such as cell cycle regulation, apoptosis, and DNA repair, leading to disease progression. Notably, miR-21, miR-31, miR-135b, and miR-486-5p have shown promise as potential biomarkers for early detection of oral premalignant lesions. Furthermore, the paper discusses the therapeutic implications of miRNAs in OPMDs. Preclinical studies have demonstrated the efficacy of miRNA-targeted therapies, such as miRNA mimics and inhibitors, in suppressing the growth of oral premalignant lesions. Early-phase clinical trials have shown promising results, indicating the potential for personalized treatment approaches. The findings underscore the importance of understanding the molecular mechanisms underlying these disorders and provide insights for the development of improved diagnostic and therapeutic strategies. However, they pose certain limitations given their intrinsic variability in expression profiles, the need for optimized isolation and detection methods, and potential hurdles in transitioning from preclinical success to clinical applications. Thus, future clinical studies are warranted to fully exploit the potential of miRNAs in the management of OPMDs.

18.
Cureus ; 16(3): e56300, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38629020

RESUMO

Background This study investigates Merremia emarginata's curative effectiveness against colon cancer cells. M. emarginata, often known as Elika jemudu, is a Convolvulaceae family plant. The inhibitory ability of anticancer herbal extracts against cancer cell growth and mediators is tested.  Aim This study aims to evaluate the potent anticancer activity of M. emarginata against colon cancer cell line (HT-29). Materials and methods M. emarginata leaves were gathered and processed using solvent extraction. Anticancer activity on colon cancer cells was measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) test and cysteine aspartic acid protease-3 (caspase 3), B-cell lymphoma 2 (Bcl-2), and B-cell lymphoma-extra large (Bcl-xL) mRNA expressions. The data was reported as the mean ± SD of three separate experiments done in triplicate. The statistical analysis was carried out using one-way analysis of variance (ANOVA), with a p-value less than 0.05 indicating statistical significance. Results The cell viability test showed a gradual decrease in cell growth and proliferation as the concentration increased. The ethanolic extract of M. emarginata was found to be cytotoxic against colon caller cell lines. The extract was able to induce apoptosis of cancer as revealed by Bcl-2, Bcl-xL, and caspase-3 (p<0.05 and p<0.001) signaling pathways. Conclusion M. emarginata extracts showed good anticancer activity against colon cancer cell lines. Further work is required to establish and identify the chemical constituent responsible for its anticancer activity.

19.
Cureus ; 16(2): e54031, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38481883

RESUMO

Background The value and use of medicinal plants, including the widespread cultivation of Rosmarinus officinalis, have increased rapidly. R. officinalis, a medicinal plant native to the Mediterranean, has received attention for its potential therapeutic benefits. This study evaluates R. officinalis anticancer activity using human epithelial carcinoma (KB) cell lines derived from nasopharyngeal epidermoid carcinoma. The KB cell line is known for its increased sensitivity to specific chemotherapeutic agents (CA), making it a useful model in cancer research. The impact of R. officinalis is assessed using comprehensive analyses of cell viability and gene expression. Aim This study aims to evaluate the anti-cancer effects of R. officinalis on KB cell lines. Materials and methods The R. officinalis leaf extract was separated and used to treat KB cell lines. The cell viability of treated KB cells was determined using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Real-time polymerase chain reaction (RT-PCR) was used to analyze the expressions of matrix metalloproteinase (MMP-9) and tumor-inducing metalloproteins (TIMP-1) messenger ribonucleic acid (mRNA) genes. The statistical analysis was performed. Results This study analyzes the anticancer properties of R. officinalis on KB cell lines. The results show that increasing the concentration of rosemary extract reduces cell viability in malignant cells. Furthermore, the R. officinalis effect on the apoptotic signaling system is demonstrated by a decrease in MMP-9 and TIMP-1 mRNA expressions, as observed by RT-PCR analysis. Conclusion Patients looking for natural anticancer treatments may benefit from biogenically prepared anticancer drugs. The current research focuses on R. officinalis as a potential alternative to chemically synthesized anticancer drugs.

20.
Cureus ; 16(2): e54061, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38481895

RESUMO

BACKGROUND: Piperine, a naturally occurring compound in black pepper (Piper nigrum), is known for its potential health benefits, including its reported enhancement of insulin sensitivity. However, the precise impact of piperine on hepatocyte nuclear factor 1 alpha (HNF-1α) and sterol regulatory element-binding protein 1c (SREBP-1c), transcription factors for insulin signaling and glucose metabolism in hepatocytes, remains unclear. OBJECTIVE: This study aims to investigate the effect of piperine, compared to metformin, on blood glucose and insulin levels by modifying the expression of hepatic HNF-1α and SREBP-1c in high-fat-diet (HFD) and sucrose-induced type 2 diabetes mellitus (T2DM) rats and in human Chang liver cells. METHODS: Adult male albino rats were categorized into four groups: group 1 as the control, group 2 as T2DM, group 3 as T2DM rats treated with piperine (40 mg), and group 4 as T2DM rats treated with metformin (50 mg). Fasting blood glucose (FBG) and serum insulin levels were measured using enzyme-linked immunosorbent assay (ELISA), while real-time polymerase chain reaction (RT-PCR) analysis was conducted to assess the mRNA expression of HNF-1α and SREBP-1c. Further, piperine was treated with normal and high glucose-induced Chang liver cells, and gene expression was analysed. Data analysis was performed using one-way analysis of variance (ANOVA), with a significance set at p<0.05. RESULTS: Treatment with piperine led to a notable decrease in blood glucose levels and circulating insulin when compared with T2DM rats (group 2). Additionally, piperine administration resulted in the upregulation of HNF-1α mRNA expression and downregulation of SREBP-1c mRNA levels whose effects were found to be near that of the control and standard drug metformin's effects. In vitro study also confirmed that piperine improved the HNF-1α expression and reduced the expression of SREBP-1c in Chang liver cells. CONCLUSION: Our findings suggest that piperine treatment effectively regulates hyperglycemic and hyperinsulinemic insulin resistance in the liver by modulating the expression of HNF-1α and SREBP-1c. Consequently, piperine emerges as a promising candidate for therapeutic intervention in managing T2DM.

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