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1.
J Tradit Chin Med ; 44(3): 496-504, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38767633

RESUMO

OBJECTIVE: To investigate the effects of Hippeastrum hybridum (HH) as a free radical scavenger, and an inhibitor of the two enzymes i-e Alpha-amylase (α-amylase) and acetylcholinesterase (AChE). METHODS: In this study, HH plant was preliminary analyzed for phytochemical screening and then tested for its antioxidant, anti-α-amylase, and anti-AChE efficiency via standard procedures. RESULTS: Phytochemical analysis shows the existence of different compounds; while Coumarins and quinones were absent. The total phenolic, flavonoid, and tannins content were found to be (78.52 ± 0.69) mg GAE/g, (2.01 ± 0.04) mg RUE/g, and (58.12 ± 0.23) mg TAE/g of plant extract respectively. 28.02% ± 0.02% alkaloid and 2.02% ± 0.05% saponins were present in the HH extract. The HH extract showed the anti-oxidant property with IC50 (50% inhibition) of (151.01 ± 0.13) (HH), (79.01 ± 0.04) (Ascorbic acid) for ferric reducing, (91.48 ± 0.13) (HH), (48.02 ± 0.11) (Ascorbic acid) against Ammonium molybdenum, (156.02 ± 0.31) (HH), (52.38 ± 0.21) (Ascorbic acid) against DPPH, 136.01 ± 0.21 (HH), 52.02± 0.31 (Ascorbic acid) against H2O2, and 154.12 ± 0.03 (HH), (40.05 ± 0.15) (Ascorbic acid) µg/mL against ABTS respectively. Statistical analysis indicated that HH caused a competitive type of inhibition of α-amylase (Vmax remained constant and Km increases from 10.65 to 84.37%) while Glucophage caused the un-competitive type of inhibition i-e both Km and Vmax decreased from 40.49 to 69.15% and 38.86 to 69.61% respectively. The Ki, (inhibition constant); KI, (dissociation constant), Km, (Michaelis-Menten constant), and IC50 were found to be 62, 364, 68.1, and 38.08 ± 0.22 for HH and 12, 101.05, 195, 34.01 ± 0.21 for Glucophage. Similarly, HH causes an anon-competitive type of inhibition of AChE i-e Km remains constant while Vmax decreases from 60.5% to 74.1%. The calculated Ki, KI, Km, and IC50 were found to be 32, 36.2, 0.05, and 18.117 ± 0.018. CONCLUSION: From the current results, it is concluded that HH extract contains bioactive compounds, and could be a good alternative to controlling oxidants, Alzheimer's and Type-II diabetic diseases.


Assuntos
Acetilcolinesterase , Antioxidantes , Inibidores da Colinesterase , Extratos Vegetais , alfa-Amilases , Antioxidantes/química , Antioxidantes/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Acetilcolinesterase/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia
2.
Artigo em Inglês | MEDLINE | ID: mdl-38619588

RESUMO

MiRNAs (microRNAs) constitute a group of diminutive molecules of non-coding RNA intricately involved in regulating gene expression. This regulation is primarily accomplished through the binding of miRNAs to complementary sequences situated in the 3'-UTR of the messenger RNA (mRNA) target; as a result, they are degraded or repressed. The multifaceted biogenesis of miRNAs is characterized by a meticulously orchestrated sequence of events encompassing transcription, processing, transportation, and decay. Colorectal cancer stands as a pervasive and formidable ailment, afflicting millions across the globe. Colorectal cancer is not well diagnosed early, and metastasis rates are high, which results in low survival rates in advanced stages. The genesis and progression of colorectal cancer are subject to the influence of genetic and epigenetic factors, among which miRNAs play a pivotal role. When it comes to colorectal cancer, miRNAs have a dual character, depending on the genes they target, functioning as either tumor suppressors or oncogenes and the prevailing cellular milieu. Their impact extends to modulating critical facets of colorectal cancer pathogenesis, including proliferation, angiogenesis, apoptosis, chemoresistance, and radiotherapy response. The discernible potential of miRNAs which are used as biomarkers to diagnose colorectal cancer, prognosis, and treatment response has come to the forefront. Notably, miRNAs are easily found and detected readily in a variety of biological fluids, including saliva, blood, urine, and feces. This prominence is attributed to the inherent advantages of miRNAs over conventional biomarkers, including heightened stability, specificity, sensitivity, and accessibility. Various investigations have pinpointed miRNA signatures or panels capable of differentiating colorectal cancer patients from their healthy counterparts, predicting colorectal cancer stage and survival, and monitoring colorectal cancer recurrence and therapy response. Although there has been research on miRNAs in various diseases, there has been less research on miRNAs in cancer. Moreover, updated results of preclinical and clinical studies on miRNA biomarkers and drugs are required. Nevertheless, the integration of miRNAs as biomarkers for colorectal cancer is not devoid of challenges and limitations. These encompass the heterogeneity prevalent among colorectal cancer subtypes and stages, the variability in miRNA expression across different tissues and individuals, the absence of standardized methodologies for miRNA detection and quantification, and the imperative for validation through extensive clinical trials. Consequently, further research is imperative to conclusively establish the clinical utility and reliability of miRNAs as colorectal cancer biomarkers. MiR-21 demonstrates carcinogenic characteristics by targeting several tumor suppressor genes, which encourages cell division, invasion, and metastasis. On the other hand, by controlling the Wnt/ß-catenin pathway, the tumor suppressor miRNA miR-34a prevents CRC cell proliferation, migration, and invasion. Furthermore, in colorectal cancer, the miR-200 family increases chemotherapy sensitivity while suppressing epithelial-mesenchymal transition (EMT). As an oncogene, the miR-17-92 cluster targets elements of the TGF-ß signaling pathway to encourage the growth of CRC cells. Finally, miR-143/145, which is downregulated in CRC, influences apoptosis and the progression of the cell cycle. These miRNAs affect pathways like Wnt, TGF-ß, PI3K-AKT, MAPK, and EMT, making them potential clinical biomarkers and therapeutic targets. This review summarizes recent research related to miRNAs, their role in tumor progression and metastasis, and their potential as biomarkers and therapeutic targets in colorectal cancer. In addition, we combined miRNAs' roles in tumorigenesis and development with the therapy of CRC patients, leading to novel perspectives on colorectal cancer diagnosis and treatment.

3.
ACS Omega ; 8(38): 35140-35151, 2023 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-37779996

RESUMO

In this study, we described the environmentally friendly biosynthesis of silver nanoparticles (AgNPs) utilizing ethanolic extract of Filago desertorum (F. desertorum) as a capping and reducing agent. We also looked at the antioxidant and antibacterial capacities of AgNPs. In order to determine the size, shape, and crystallinity of the created AgNPs, the current project was designed to produce AgNPs utilizing the crude extract of the F. desertorum. The effectiveness of the project was evaluated by UV-visible spectrophotometry, Fourier transform infrared spectroscopy, scanning electron microscopy, and X-ray diffraction. AgNPs are monodispersed and spherical and have 50 nm average particle diameters, as determined using Image J software calculations and SEM observation. Four significant peaks from an XRD study, located at 38.46, 44.63, 64.81, and 77.74 nm, were used to calculate the average crystalline size of AgNPs which was reported to be 15 nm. In the crude extract of F. desertorum, it is possible to see the functional group peaks of a number of substances that are essential for bioreduction and the stability of the AgNPs. Antibacterial and antioxidant properties of AgNPs in vitro (DPPH, ABTS, H2O2, phosphomolybdenum, and ferric reducing power) were examined using conventional methods. The AgNPs showed maximum DPPH (72.51% with IC50 = 144.61 µg/mL), ABTS (75.24% with IC50 = 131.21 µg/mL), hydrogen peroxide (73.33% with IC50 = 115.05 µg/mL), phosphomolybdenum activity (73.43% with IC50 = 75.25 µg/mL), and observing reducing power (0.25) at a concentration of 250 g/mL. Inhibition by the AgNPs against the bacterial strain Staphylococcus aureus was greatest (12 mm). According to the current findings, AgNPs produced by F. desertorum have the highest potential for free radical scavenging and antibacterial activity, which can result in antioxidant and antibiotic agents.

4.
RSC Adv ; 13(42): 29632-29644, 2023 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-37822660

RESUMO

Iron-nickel bimetallic nanoparticles (Fe-Ni BMNPs) are prepared by combining two different metals by using the bottom-up approach. The resulting material has entirely different properties as compared to both the metals. The product is examined by using different analytical instruments such as.; scanning electron microscope (SEM), transmission electron microscope (TEM), X-ray diffraction (XRD), MDIJADE, ORIGIN pro to characterize their morphology, crystallinity and elemental composition and the final data has been statistically analyzed. SEM findings show that most nanoparticles are irregular in form and range in size from 10 nm to 100 nm. The findings of the TEM verified that the particles between 10 nm and 50 nm are irregular in size shape. The products acquired utilized as a fuel additive to monitor oil effectiveness by studying various parameters. The degradation of methylene blue dye depends directly on the concentration of the nanocatalyst. Different parameters also use the freshly prepared bimetallic nanocatalyst to investigate the efficacy of the kerosene fuel. By adding a tiny quantity of the nanocatalyst, the value of the flash point and fire point is significantly reduced. The nanocatalyst does not affect the cloud point and pour point to a large extent. The bimetallic nanocatalyst therefore has very excellent catalytic characteristics.

5.
Molecules ; 27(22)2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-36431998

RESUMO

Nanotechnology is one of the most recent technologies. It is uncertain whether the production of small-size nanoparticles (NPs) can be achieved through a simple, straightforward, and medicinally active phytochemical route. The present study aimed to develop an easy and justifiable method for the synthesis of Ag, Au, and their Ag/Au bimetallic NPs (BNPs) by using Hippeastrum hybridum (HH) extract, and then to investigate the effects of Ag, Au, and their Ag/Au BNPs as antimicrobial and phytotoxic agents. Ag, Au, and their Ag/Au BNPs were characterized by UV-visible spectroscopy, FT-IR spectroscopy, XRD, EDX, and SEM analysis. XRD analysis conferring to the face of face-centered cubic crystal structure with an average size of 13.3, 10.72, and 8.34 nm of Ag, Au, and Ag/Au BNPs, respectively. SEM showed that Ag, Au, and Ag/Au BNPs had spherical morphologies, with calculated nano measurements of 40, 30, and 20 nm, respectively. The EDX analysis confirmed the composition of elemental Ag signal of the HH-AgNPs with 22.75%, Au signal of the HH-AuNPs with 48.08%, Ag signal with 12%, and Au signal with 38.26% of the Ag/Au BNPs. The Ag/Au BNPs showed an excellent antimicrobial efficacy against Gram-positive Staphylococcus aureus, Actinomycetes meriye, Bacillus cereus, Streptococcus pyogenes, Methicillin-resistant Staphylococcus aureus, Micrococcus luteus, Streptococcus pneumonia, and Gram-negative Klebsiella pneumonia, Escherichia coli, and Serratia marcescens bacterial strains, as well as against three fungal strains (Aspergillus niger, Aspergillus fumigatus, and Aspergillus flavus) compared to HH extract, HH-AgNPs, and HH-AuNPs. However, further investigations are recommended to be able to minimize potential risks of application.


Assuntos
Anti-Infecciosos , Nanopartículas Metálicas , Staphylococcus aureus Resistente à Meticilina , Pneumonia , Humanos , Prata/farmacologia , Prata/química , Ouro/farmacologia , Ouro/química , Nanopartículas Metálicas/química , Espectroscopia de Infravermelho com Transformada de Fourier , Antibacterianos/química , Escherichia coli , Anti-Infecciosos/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química
6.
J Tradit Chin Med ; 42(3): 426-431, 2022 06.
Artigo em Inglês | MEDLINE | ID: mdl-35610012

RESUMO

OBJECTIVES: To estimate the existence of phyto-chemicals and then to determine the antidiabetic activity against α-amylase and ß-glucosidase inhibition . METHODS: The study was carried out by following standard procedures. RESULTS: Phytochemicals analysis indicated the presence of different phytochemicals. The total phenolic content was 6.055 mg GAE/g and the total flavonoid content was 5.706 mg RU/g in the plant extract. The total saponins, alkaloids, and tannins contents were (0.044%), (2.88%) and (2.862 nm) respectively. α-amylase inhibition activity of Calligonum polygonoides (CP) extract was 70% with IC50 of 610 µg/mL and that of ß-gluco-sidase inhibition activity was 65% with IC50 of 640 µg/mL. CONCLUSION: The findings reported for the first time the antidiabetes-promoting effects of an extract of CP, thus validating their promising anti-diabetes potential.


Assuntos
Inibidores de Glicosídeo Hidrolases , alfa-Amilases Pancreáticas , Antioxidantes/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Amilases , alfa-Glucosidases/química , beta-Glucosidase
7.
Front Vet Sci ; 9: 827407, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35425833

RESUMO

The immune system is most likely developed to reduce the harmful impact of infections on the host homeostasis. This defense approach is based on the coordinated activity of innate and adaptive immune system components, which detect and target infections for containment, killing, or expulsion by the body's defense mechanisms. These immunological processes are responsible for decreasing the pathogen burden of an infected host to maintain homeostasis that is considered to be infection resistance. Immune-driven resistance to infection is connected with a second, and probably more important, defensive mechanism: it helps to minimize the amount of dysfunction imposed on host parenchymal tissues during infection without having a direct adverse effect on pathogens. Disease tolerance is a defensive approach that relies on tissue damage control systems to prevent infections from causing harm to the host. It also uncouples immune-driven resistance mechanisms from immunopathology and disease, allowing the body to fight infection more effectively. This review discussed the cellular and molecular processes that build disease tolerance to infection and the implications of innate immunity on those systems. In addition, we discuss how symbiotic relationships with microbes and their control by particular components of innate and adaptive immunity alter disease tolerance to infection.

8.
Concurr Comput ; 34(28): e7386, 2022 Dec 25.
Artigo em Inglês | MEDLINE | ID: mdl-36714183

RESUMO

The virus of COVID-19 has affected humans physically, mentally, and economically all over the world. Each country's development level, resources, and immunization to have coping capacity against this covid19 differ country-wise. Thus, understanding socioeconomic vulnerability and coping capacity among countries under different health systems can be crucial. Contrasting most articles on COVID-19, this article focuses on evaluating and estimating the COVID-19 risk and lack of coping capacity in 190 countries. This present study suggests an exponential estimator using two auxiliary attributes. Theoretically, the mean square error expressions are derived and compared with some existing estimators. These findings were supported by using the real data of INFORM COVID-19 risk.

9.
Cureus ; 13(8): e17471, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34589364

RESUMO

Introduction Rectal cancer has become a major cause of mortality worldwide. Imaging has a primary role in staging and assessing the response to therapy. MRI is superior to all other modalities in local staging of the rectal tumor and in predicting tumor response. Pelvic MRI has an undeniable role in the therapeutic management of rectal cancer, particularly for the determination of the circumferential resection margin (CRM), evaluation of sphincter invasion, and assessment of the extramural vascular invasion. Post-chemoradiotherapy (CRT) staging aims at assessing treatment response and choosing methods for further treatment such as surgical resection or extended CRT. MRI with diffusion restriction is a non-invasive and useful tool for assessing the treatment response of locally advanced lower rectal cancer. It will reduce the burden of extensive abdominoperineal resection (APR) surgery in patients. Objective The purpose of this study was to determine the role of diffusion-weighted imaging (DWI) in the evaluation of post-treatment tumor response in rectal carcinoma. Materials and methods The study was approved by our institutional review board, which waived the requirement for informed consent. The clinical data of all the patients treated for rectal carcinoma at the Shaukat Khanum Memorial Cancer Hospital and Research Centre, Lahore between February 1, 2014, and February 28, 2019, were retrospectively evaluated. The inclusion criteria were as follows: (1) patients with histopathologically proven rectal adenocarcinoma, (2) those who underwent APR before February 2019 at our hospital, and (3) those who underwent MRI including DWI/apparent diffusion coefficient (ADC) imaging before and after CRT. Those patients who had upfront surgery without neoadjuvant CRT and those who did not have MRI imaging with DWI/ADC were excluded from the study. Results A total of 200 patients who fulfilled the inclusion criteria were included in this study. Among those, 141 were males and 59 were females. On histology, 110 had moderately differentiated adenocarcinoma, 25 had well-differentiated adenocarcinoma, and 65 had poorly differentiated adenocarcinomas. Overall diagnostic accuracy of DWI MRI sequence was calculated to be 91%, while the sensitivity was 98.09%, specificity was 65.12%, positive predictive value was 91.12%, and negative predictive value was 90.32%. Conclusion DWI was proven to be very useful in the post-treatment evaluation of tumor response with very high diagnostic accuracy.

10.
Pak J Pharm Sci ; 34(1): 151-156, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34248014

RESUMO

The present research study investigates the phytochemical and pharmacological importance of Bromus pectinatus. Qualitative phytochemical analysis of this plant was carried out to use standard method for the presence of various bioactive constituents. Results showed the ethanolic extract contain natural product such as steroids, alkaloids, tannins, coumarin, saponins, flavonoids and phenols. These compounds play a key role to reducing various disease and microbial inhibition. The ethanolic extract also showed the antimicrobial and antifugal activity against different pathogenic bacterial strains e.g Escherichia coli, Micrococus leutus, Protus vulgarus, and Kelebsela pneumona and three fungal strains Aspergillus fumigatus, Aspergillus flavous, Aspergillus niger. The antioxidant assay was performed as % inhibition of DPPH (1, 1-diphenyl-2-picryl-hydrazyl) free radicals. The plant extract has more antioxidant activity as compared to ascorbic acid. The maximum concentration (800µg/ml) is the most effective of all. The plant extract showed the high cytotoxicity activity against Brine shrimp. Moreover, the plant extract exhibited allelopathic effect on different growth parameters of wheat plant mostly at higher concentration. These results indicate that the BPEE have a potential broad-spectrum antimicrobial, cytotoxic, antioxidant and phytotoxic activity due to the presence of bioactive compounds.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Bromus , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Anti-Infecciosos/isolamento & purificação , Antioxidantes/isolamento & purificação , Artemia , Aspergillus niger/efeitos dos fármacos , Aspergillus niger/fisiologia , Avaliação Pré-Clínica de Medicamentos/métodos , Escherichia coli/efeitos dos fármacos , Escherichia coli/fisiologia , Testes de Sensibilidade Microbiana/métodos , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação
11.
J Tradit Chin Med ; 41(3): 349-354, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-34114390

RESUMO

OBJECTIVE: To examine the efficacy of Silene arenosa extract on acetylcholinesterase (AChE) of krait (Bungarus Sindanus) snake venom. METHODS: The present project designed to evaluate the inhibition of AChE by following standard procedures. RESULTS: Statistical analysis of the results showed that Silene arenosa exerted 73% inhibition against the krait venom acetylcholinesterase at fixed substrate acetylcholine (ACh) concentration (0.5 mM). Kinetic analysis using the Lineweaver Burk plot revealed that Silene arenosa caused a competitive type of inhibition i.e. Km values increased from 26.6 to 93.3 mM (26.6% to 93.3%) and Vmax remained constant in a concentration-dependent manner. Silene arenosa competes with the substrate to bind at the active site of the enzyme. The Kmapp of venom AChE for Silene arenosa increased from 60% to 81.6% and the Vmaxapp remains constant. Ki (inhibition constant was estimated to be 48 µg for snake venom; while the Km (Michaelis-Menten constant of AChE- substrate into AChE and product) was estimated to be 0.5 mM. The IC50 of AchE calculated for Silene arenosa was 67 µg. CONCLUSION: The present results suggest that Silene arenosa extract can be considered as an inhibitor of snake venom AChE.


Assuntos
Acetilcolinesterase , Silene , Acetilcolinesterase/metabolismo , Animais , Bungarus/metabolismo , Inibidores da Colinesterase/farmacologia , Humanos , Cinética , Extratos Vegetais , Silene/metabolismo
12.
Mol Biotechnol ; 63(9): 757-767, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34041717

RESUMO

The sophistication and revolution in genome editing and manipulation have revolutionized livestock by harvesting essential biotechnological products such as drugs, proteins, and serum. It laid down areas for the large production of transgenic food, resistance against certain diseases such as mastitis, and large production of milk and leaner meat. Nowadays, the increasing demand for animal food and protein is fulfilled using genome-editing technologies. The recent genome-editing techniques have overcome the earlier methods of animal reproduction, such as cloning and artificial embryo transfer. The genome of animals now is modified using the recent alteration techniques such as ZFNs, TALENS technique, and clustered regularly interspaced short palindromic repeats/Cas9 (CRISPR-Cas9) system. The literature was illustrated for identifying the researchers to address the advances and perspectives in the application of Cas9 in Livestock. Cas9 is considered better than the previously identified techniques in livestock because of the production of resilience against diseases, improvement of reproductive traits, and animal production to act as a model biomedical research.


Assuntos
Animais Geneticamente Modificados , Sistemas CRISPR-Cas , Edição de Genes/métodos , Gado/genética , Carne/provisão & distribuição , Nucleases dos Efetores Semelhantes a Ativadores de Transcrição/genética , Animais , Bovinos , Feminino , Genoma , Cabras/genética , Cabras/metabolismo , Gado/metabolismo , Mastite/genética , Mastite/prevenção & controle , Carne/análise , Leite/química , Leite/provisão & distribuição , Transplante de Órgãos/métodos , Reação em Cadeia da Polimerase/métodos , Carneiro Doméstico/genética , Carneiro Doméstico/metabolismo , Suínos/genética , Suínos/metabolismo , Nucleases dos Efetores Semelhantes a Ativadores de Transcrição/metabolismo , Transplante Heterólogo
13.
Artigo em Inglês | MEDLINE | ID: mdl-33889183

RESUMO

BACKGROUND: The venom of the krait (Bungarus sindanus), an Elapidae snake, is highly toxic to humans and contains a great amount of acetylcholinesterase (AChE). The enzyme AChE provokes the hydrolysis of substrate acetylcholine (ACh) in the nervous system and terminates nerve impulse. Different inhibitors inactivate AChE and lead to ACh accumulation and disrupted neurotransmission. METHODS: The present study was designed to evaluate the effect of palladium(II) complex as antivenom against krait venom AChE using kinetics methods. RESULTS: Statistical analysis showed that krait venom AChE inhibition decreases with the increase of Pd(II) complex (0.025-0.05 µM) and exerted 61% inhibition against the AChE at a fixed concentration (0.5 mM) of ACh. Kinetic analysis using the Lineweaver Burk plot showed that Pd(II) caused a competitive inhibition. The compound Pd(II) complex binds at the active site of the enzyme. It was observed that K m (Michaelis-Menten constant of AChE-ACh into AChE and product) increased from 0.108 to 0.310 mM (45.74 to 318.35%) and V max remained constant with an increase of Pd(II) complex concentrations. In AChE K Iapp was found to increase from 0.0912 to 0.025 µM (29.82-72.58%) and did not affect the V maxapp with an increase of ACh from (0.05-1 mM). K i (inhibitory constant) was estimated to be 0.029 µM for snake venom; while the K m was estimated to be 0.4 mM. The calculated IC50 for Pd(II) complex was found to be 0.043 µM at constant ACh concentration (0.5 mM). CONCLUSIONS: The results show that the Pd(II) complex can be deliberated as an inhibitor of AChE.

14.
J. venom. anim. toxins incl. trop. dis ; 27: e20200047, 2021. tab, graf
Artigo em Inglês | VETINDEX, LILACS | ID: biblio-1287090

RESUMO

The venom of the krait (Bungarus sindanus), an Elapidae snake, is highly toxic to humans and contains a great amount of acetylcholinesterase (AChE). The enzyme AChE provokes the hydrolysis of substrate acetylcholine (ACh) in the nervous system and terminates nerve impulse. Different inhibitors inactivate AChE and lead to ACh accumulation and disrupted neurotransmission. Methods: The present study was designed to evaluate the effect of palladium(II) complex as antivenom against krait venom AChE using kinetics methods. Results: Statistical analysis showed that krait venom AChE inhibition decreases with the increase of Pd(II) complex (0.025-0.05 µM) and exerted 61% inhibition against the AChE at a fixed concentration (0.5 mM) of ACh. Kinetic analysis using the Lineweaver Burk plot showed that Pd(II) caused a competitive inhibition. The compound Pd(II) complex binds at the active site of the enzyme. It was observed that K m (Michaelis-Menten constant of AChE-ACh into AChE and product) increased from 0.108 to 0.310 mM (45.74 to 318.35%) and V max remained constant with an increase of Pd(II) complex concentrations. In AChE K Iapp was found to increase from 0.0912 to 0.025 µM (29.82-72.58%) and did not affect the V maxapp with an increase of ACh from (0.05-1 mM). K i (inhibitory constant) was estimated to be 0.029µM for snake venom; while the K m was estimated to be 0.4 mM. The calculated IC50 for Pd(II) complex was found to be 0.043 µM at constant ACh concentration (0.5 mM). Conclusions: The results show that the Pd(II) complex can be deliberated as an inhibitor of AChE.(AU)


Assuntos
Animais , Bungarus , Venenos Elapídicos/toxicidade , Biologia Sintética , Paládio , Acetilcolinesterase
15.
Iran J Basic Med Sci ; 21(8): 869-872, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30186576

RESUMO

OBJECTIVES: The objective of this study was to evaluate pharmacological effect of Calligonum polygonoides against Krait snake's venom acetylcholinesterase (AChE) and to extent it for the treatment of Alzheimer's disease. MATERIALS AND METHODS: Acetylcholinesterase activity was measured using Ellman method with some modification. The kinetic studies of methanolic extract of C. polygonoides against krait (Bungarus Sindanus) snake venom AChE was measured with the help of the Lineweaver Burk double reciprocal plot. RESULTS: Statistical data of the results showed that C. polygonoides extract inhibited the krait venom AChE in concentration dependent manner. Kinetic analysis using Line weaver Burk plot revealed that C. polygonoides caused mixed type of inhibition i.e. km value increased (25-106.6%) while Vmax decreased from 15 to 50% with an increase of C. polygonoides extract concentrations (100-300 µg/ml). The calculated IC50 value of C. polygonoides was found to be 250 µg/ml. CONCLUSION: C. polygonoides extract can be considered as a therapeutic agent to cure Alzheimer's disease via inhibition of AChE activity to increase the level of acetylcholine in the body system.

16.
J Pak Med Assoc ; 65(11): 1161-3, 2015 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-26564284

RESUMO

OBJECTIVE: To assess the frequency of consanguinity in b-thalassemia major patients and its association with age, gender and hepatitis C virus antibody positivity. METHODS: The cross-sectional study was conducted from June 2013 to July 2014 at various hospitals of district Bannu in the North Western Khyber Pakhtunkhwa province of Pakistan. Data was recorded on a predesigned questionnaire. RESULTS: Out of 180 subjects, 133(74%) parents were cousins, while 47(26%) were unrelated. The frequency of anti-hepatitis C virus antibody positivity was 14(7.77%). CONCLUSIONS: High prevalence of the disease in the study region was due to consanguineous marriages.


Assuntos
Consanguinidade , Casamento , Talassemia beta/epidemiologia , Estudos Transversais , Feminino , Anticorpos Anti-Hepatite C/sangue , Humanos , Incidência , Masculino , Paquistão , Talassemia beta/sangue
17.
J Physiol Biochem ; 71(4): 743-51, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26452500

RESUMO

In the present study, we investigated the efficiency of rosmarinic acid (RA) in preventing the alteration of oxidative parameters in the liver and kidney of diabetic rats induced by streptozotocin (STZ). The animals were divided into six groups (n = 8): control, ethanol, RA 10 mg/kg, diabetic, diabetic/ethanol, and diabetic/RA 10 mg/kg. After 3 weeks of treatment, we found that TBARS levels in liver and kidney were significantly increased in the diabetic/saline group and the administration of RA prevented this increase in the liver and kidney (P < 0.05). Diabetes caused a significant decrease in the activity of superoxide dismutase (SOD) and catalase (CAT) in the diabetes/saline group (P < 0.05). However, the treatment with 10 mg/kg RA (antioxidant) prevented this alteration in SOD and CAT activity in the diabetic RA group (P < 0.05). In addition, RA reverses the decrease in ascorbic acid and non-protein-thiol (NPSH) levels in diabetic rats. The treatment with RA also prevented the decrease in the Delta-aminolevulinic acid dehydratase (ALA-D) activity in the liver and kidney of diabetic rats. Furthermore, RA did not have any effect on glycemic levels. These results indicate that RA effectively reduced the oxidative stress induced by STZ, suggesting that RA is a potential candidate for the prevention and treatment of pathological conditions in diabetic models.


Assuntos
Antioxidantes/farmacologia , Cinamatos/farmacologia , Depsídeos/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Rim/metabolismo , Fígado/metabolismo , Animais , Antioxidantes/uso terapêutico , Ácido Ascórbico/metabolismo , Biomarcadores/metabolismo , Glicemia , Cinamatos/uso terapêutico , Depsídeos/uso terapêutico , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/metabolismo , Avaliação Pré-Clínica de Medicamentos , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Masculino , Malondialdeído/metabolismo , Estresse Oxidativo , Ratos Wistar , Estreptozocina , Superóxido Dismutase/metabolismo , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Ácido Rosmarínico
18.
Cell Biochem Funct ; 32(3): 287-93, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24301255

RESUMO

We investigated the efficacy of rosmarinic acid (RA) in preventing lipid peroxidation and increased activity of acetylcholinesterase (AChE) in the brain of streptozotocin-induced diabetic rats. The animals were divided into six groups (n = 8): control, ethanol, RA 10 mg/kg, diabetic, diabetic/ethanol and diabetic/RA 10 mg/kg. After 21 days of treatment with RA, the cerebral structures (striatum, cortex and hippocampus) were removed for experimental assays. The results demonstrated that the treatment with RA (10 mg/kg) significantly reduced the level of lipid peroxidation in hippocampus (28%), cortex (38%) and striatum (47%) of diabetic rats when compared with the control. In addition, it was found that hyperglycaemia caused significant increased in the activity of AChE in hippocampus (58%), cortex (46%) and striatum (30%) in comparison with the control. On the other hand, the treatment with RA reversed this effect to the level of control after 3 weeks. In conclusion, the present findings showed that treatment with RA prevents the lipid peroxidation and consequently the increase in AChE activity in diabetic rats, demonstrating that this compound can modulate cholinergic neurotransmission and prevent damage oxidative in brain in the diabetic state. Thus, we can suggest that RA could be a promising compound in the complementary therapy in diabetes.


Assuntos
Acetilcolinesterase/metabolismo , Antioxidantes/farmacologia , Encéfalo/metabolismo , Cinamatos/farmacologia , Depsídeos/farmacologia , Diabetes Mellitus Experimental/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Animais , Diabetes Mellitus Experimental/induzido quimicamente , Masculino , Ratos , Ratos Wistar , Estreptozocina , Ácido Rosmarínico
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