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BACKGROUND: NSCLC is a lethal cancer that is highly prevalent and accounts for 85% of cases of lung cancer. Conventional cancer treatments, such as chemotherapy and radiation, frequently exhibit limited efficacy and notable adverse reactions. Therefore, a drug repurposing method is proposed for effective NSCLC treatment. AIMS: This study aims to evaluate candidate drugs that are effective for NSCLC at the clinical level using a systems biology and network analysis approach. METHODS: Differentially expressed genes in transcriptomics data were identified using the systems biology and network analysis approaches. A network of gene co-expression was developed with the aim of detecting two modules of gene co-expression. Following that, the Drug-Gene Interaction Database was used to find possible drugs that target important genes within two gene co-expression modules linked to non-small cell lung cancer (NSCLC). The use of Cytoscape facilitated the creation of a drug-gene interaction network. Finally, gene set enrichment analysis was done to validate candidate drugs. RESULTS: Unlike previous research on repositioning drugs for NSCLC, which uses a gene co-expression network, this project is the first to research both gene co-expression and co-occurrence networks. And the co-occurrence network also accounts for differentially expressed genes in cancer cells and their adjacent normal cells. For effective management of non-small cell lung cancer (NSCLC), drugs that show higher gene regulation and gene affinity within the drug-gene interaction network are thought to be important. According to the discourse, NSCLC genes have a lot of control over medicines like vincristine, fluorouracil, methotrexate, clotrimazole, etoposide, tamoxifen, sorafenib, doxorubicin, and pazopanib. CONCLUSION: Hence, there is a possibility of repurposing these drugs for the treatment of non-small-cell lung cancer.
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Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Humanos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Carcinoma Pulmonar de Células não Pequenas/genética , Carcinoma Pulmonar de Células não Pequenas/metabolismo , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/genética , Neoplasias Pulmonares/metabolismo , Reposicionamento de Medicamentos , Regulação Neoplásica da Expressão Gênica , Redes Reguladoras de GenesRESUMO
Objective Neurosurgical patients account for the majority of cases across all surgical specialties that are admitted to the surgical intensive care unit (ICU) at our institution. The goal of this study was to analyze factors leading to ICU admission, type of neurosurgical intervention, length of ICU/hospital stays, and outcomes in terms of complications and ICU and in-hospital mortality. Methods This retrospective study conducted at the surgical ICU, Aga Khan University Hospital, investigated clinical data of neurosurgical patients admitted between January 2020 and June 2022. Quantitative data were collected regarding patients' characteristics, such as age, gender, comorbidities, type of surgical intervention, mode of surgery, source of admission to ICU, and type of osmotherapy. The primary and secondary outcomes were in terms of ICU and hospital mortality and complications. Results Among 321 patients admitted to the SICU, 197 were included according to inclusion/exclusion criteria. A total of 168 patients (85.3%) required surgical intervention, of whom 101 (60%) underwent elective surgery and 67 (40%) required emergency surgery. Thirteen patients died during the ICU or hospital stay, representing a mortality rate of 6.6%. The average length of stay in the ICU had a median IQR of 4 (4,6) days while the average hospital stay median IQR was 11 (12,18) days. Tracheostomy was performed in 77 patients (39%), and the median IQR day for tracheostomy was 4 (3,5) days. APACHE-II (Acute Physiology and Chronic Health Evaluation) score, length of ICU, and length of hospital stay were significantly higher in the deceased patients with a p-value of 0.042, 0.019, and 0.043, respectively. Conclusion In conclusion, this study on neurosurgical patients from the surgical intensive care unit of a low-middle-income country provided valuable insights about factors and their influence on outcomes. The study implies that a high APACHE-II score is linked to poorer outcomes for neurosurgical patients in this particular setting. Undertaking a large multicenter prospective study is vital for tailoring interventions and improving patient care in regions with limited resources where healthcare challenges may be distinct.
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BACKGROUND: To present the population-based cancer statistics for Khyber Pakhtunkhwa (KP), Pakistan, an incidence study was conducted at the Shaukat Khanum Memorial Cancer Hospital and Research Centre (SKMCH&RC) in Lahore, Pakistan, in 2023. METHODS: Records from various centres on new cancers diagnosed among residents of KP between January and December 2020 were gathered. Both active and passive methods of data collection were applied, and the information was saved in a central repository at SKMCH&RC. The incidence rates were computed by age group and sex and presented per 100,000 population. RESULTS: Among children (0-14 years), the Age-Standardised Incidence Rate (ASIR) was 4.0 in girls and 6.1 in boys, and haematologic malignancies were more prevalent; in adolescents (15-19 years), the ASIR was 7.7 in females, 9.4 in males, and bone tumours, haematologic malignancies, and neurological cancers were prominent; in adult females (> / = 20 years), the ASIR was 84.9, and cancers of the breast, digestive system, and reproductive organs were predominant; and adult males, the ASIR was 73.0, and cancers of the gastrointestinal tract, lip/oral cavity/pharynx, prostate, and Non-Hodgkin Lymphoma (NHL) were common. CONCLUSIONS: It is crucial to investigate the aetiology of these diseases at the community level because dietary elements, infectious diseases, and tobacco use all appear to be significant contributors. Prospective studies could play a key role in highlighting the factors linked to these diseases. Therefore, cancer registration must continue in conjunction with the exploration of risk factors.
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Neoplasias Hematológicas , Neoplasias , Adolescente , Adulto , Masculino , Criança , Feminino , Humanos , Incidência , Paquistão/epidemiologia , Estudos Prospectivos , Neoplasias/epidemiologiaRESUMO
This case report features unique anaesthetic management of a patient with implanted deep brain stimulation (DBS) device undergoing abdominal surgery. It features the intraoperative measures taken for this patient for the implanted DBS. After turning off the DBS preoperatively, the patient showed an exaggerated sympathetic response which was very much resistant to medicines. It was unique to this patient that restarting the device alleviated refractory hypertension. The report also includes review of literature for anaesthetic management of patients with implanted DBS.
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Estimulação Encefálica Profunda , Hipertensão , Humanos , Estimulação Encefálica Profunda/efeitos adversos , Hipertensão/complicações , Hipertensão/terapia , Próteses e ImplantesRESUMO
OBJECTIVE: To compile a comprehensive national cancer registry report of Pakistan by merging and analysing cancer registration data received from major functional cancer registries in various parts of Pakistan. STUDY DESIGN: Observational study. Place and Duration of the Study: Health Research Institute (HRI), National Institutes of Health (NIH), Islamabad, from 2015-2019. METHODOLOGY: Data from major cancer registries which included 'Punjab Cancer Registry (PCR), 'Karachi Cancer Registry (KCR)', 'Pakistan Atomic Energy Commission (PAEC) Cancer Registry', Armed Forces Institute of Pathology (AFIP) Cancer Registry, Nishtar Medical University Hospital Multan (NMH), and Shifa International Hospital, Islamabad (SIH) registries were pooled, cleared, and analysed at HRI. RESULTS: A total of 269,707 cancer cases were analysed. Gender-wise 46.7% were males and 53.61% were females. As per province-wise distribution, 45.13% of cases were from Punjab, 26.83% from Sindh, 16.46% from Khyber Pakhtunkhwa (KP), and 3.52% from Baluchistan. Both genders combined, 'breast cancer' 57633 (21.4%) was the most common cancer. In males, the top-5 cancers in order of frequency/percenatages were 'oral' 14477 (11.6%), 'liver' 8398 (6.73%), colorectal 8024 (6.43%), 'lung' 7547 (6.05%) and 'prostate' 7322 (5.87% cancers). In females, causes of the top-5-cancers included 'breast' 56250 (38.8%), 'ovary' 8823 (6.09%), 'oral' 7195 (4.97%), 'cervix' 6043 (4.17%), and 'colorectal' 4860 (3.36%) cancers. In children 'Leukemia' 1626 (14.50%) and in adolescents 'Bone' 880 (14%) were the leading malignancies. CONCLUSION: Breast cancer is the most common cancer in females touching epidemic proportions while 'oral cancer' which is the leading cancer in males ranks third in frequency in females. Like 'oral cancer' which shows a strong correlation with chewing, other common cancers in Pakistan including liver cancer, lung cancer, and cervical cancer are also largely preventable as showed a strong correlation with hepatitis B and C, smoking, and high-risk human papillomavirus. KEY WORDS: National Cancer Registry, Health Research Institute - NIH, Islamabad, Pakistan.
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Neoplasias da Mama , Neoplasias Pulmonares , Neoplasias Bucais , Neoplasias , Criança , Adolescente , Humanos , Masculino , Feminino , Paquistão/epidemiologia , Neoplasias/epidemiologia , Neoplasias/patologia , Neoplasias da Mama/epidemiologia , Sistema de Registros , IncidênciaRESUMO
We present a case that describes the airway management of a patient with recurrent head and neck cancer and confirmed COVID-19 infection. Securing airway of these patients with anticipated difficulty and at the same time limiting virus exposure to providers can be challenging. The risk of aerosolization during awake tracheal intubation is extreme as it carries a high risk of transmitting respiratory infections. A multidisciplinary team discussion before the procedure highlighted aspects of both airway management and the urgency of surgical procedure where particular care and modifications are required. Successful flexible bronchoscopy and intubation was done under inhalational anaesthetics with spontaneous breathing. Although fiberoptic intubation during sleep,in anticipated difficult airways, have led to enhanced intubation time, this technique was opted to minimize the risk of aerosol generation associated with topicalisation, coughing and hence reduced incidence of cross infection to health care workers.
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COVID-19 , Neoplasias de Cabeça e Pescoço , Humanos , Síndrome da Fibrose por Radiação , Recidiva Local de Neoplasia , Manuseio das Vias Aéreas/métodos , Intubação Intratraqueal/métodos , Neoplasias de Cabeça e Pescoço/radioterapia , BocaRESUMO
The chronic inflammatory conditions like psoriasis has an increased prevalence and is linked with various associated life threatening disease conditions. The main objective of this project was to developed a methotrexate-olive loaded nano emulsion. The formulation was assessed for various parameters including Thermodynamic Stability, physico-chemically characterization, drug release kinetics and entrapment efficiency and in vitro/ in vivo skin permeation analysis. Final optimized formulation had a particle size 18.27±5.78 nm with a PDI of 0.25±0.01, whereas the average entrapment efficiency of formulation was 74.68±2.1%. The release kinetics suggested 97.72% drug release at pH 5 after 20 hrs. The FTIR data confirmed that the chemical structure of drug is retained with efficient loading into the formulation. Permeation data showed that an average of 79.23±3.6µg/cm2 of methotrexate was permeated from the nano emulsion with an average flux of 2.326±0.45µg/cm2/h after 24 hrs. Finally in vivo studies on rabbit skin confirmed that the structural changes of intercellular lipid layers in the stratum corneum are not responsible for enhanced skin permeation of methotrexate loaded nano emulsion. It was concluded that olive oil based MTX-NE is suitable for topical application and can be used for management of psoriasis.
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Fármacos Dermatológicos/administração & dosagem , Fármacos Dermatológicos/farmacologia , Metotrexato/administração & dosagem , Metotrexato/farmacologia , Azeite de Oliva , Psoríase/tratamento farmacológico , Pele/diagnóstico por imagem , Administração Cutânea , Animais , Portadores de Fármacos , Emulsões , Sistemas de Liberação de Fármacos por Nanopartículas , Coelhos , Pele/metabolismo , Absorção CutâneaRESUMO
Bioassays guided phytochemical investigations on the ethyl acetate-soluble fraction of the root material of Ballota pseudodictamnus (L.) Benth. led to the isolation of two new compounds, ballodiolic acid A (1) and ballodiolic acid B (2), along with three known compounds ballodiolic acid (3), ballotenic acid (4), and ß-amyrin (5), which were also isolated for the first time from this species by using multiple chromatographic techniques. The structures of the compounds (1-5) were determined by modern spectroscopic analysis including 1D and 2D NMR techniques and chemical studies. In three separate experiments, the isolated compounds (1-5) demonstrated potent antioxidant scavenging activity, with IC50 values ranging from 07.22-34.10 µM in the hydroxyl radical (â¢OH) inhibitory activity test, 58.10-148.55 µM in the total ROS (reactive oxygen species) inhibitory activity test, and 6.23-69.01 µM in the peroxynitrite (ONOO-) scavenging activity test. With IC50 values of (07.22 ± 0.03, 58.10 ± 0.07, 6.23 ± 0.04 µM) for â¢OH, total ROS, and scavenge ONOO-, respectively, ballodiolic acid B (2) showed the highest scavenging ability. Antibacterial and antifungal behaviors were also exposed to the pure compounds 1-5. In contrast to compounds 4 and 5, compounds 1-3 were active against all bacterial strains studied, with a good zone of inhibition proving these as a potent antibacterial agent. Similarly, compared to compounds 3-5, compounds 1 and 2 with a 47 percent and 45 percent respective inhibition zone were found to be more active against tested fungal strains.
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Coronavirus infection (COVID-19) has significantly increased the mortality and morbidity rates worldwide. The present study was conducted to assess the general public's awareness of COVID-19 and its association with mental health, dietary habits, and physical activity. A web-based survey was conducted to gather information about demographics, knowledge about COVID-19, dietary habits, mental health, and anthropometry among the general public of Pakistan. Descriptive statistics, chi-square test, and multiple logistic regression were used for data analysis. The majority of the participants were suffering from anxiety (71.0%) and depression (52.0%) during the COVID-19 pandemic; 32.4% of participants had poor COVID-19-related knowledge. COVID-19 lockdown reduced the physical activity of 66.9% of participants and increased weight of 38.8% of the survey participants. Demographic variables, including age, gender, ethnicity, education, employment, family type, and geographical location, were significantly associated with knowledge about COVID-19 (P < 0.05). Depression was inversely associated with COVID-19 knowledge (P < 0.05). Healthy changes in dietary habits including decreased consumption of fast foods, soft and cola drinks, fruit drinks, cooked meat (outside the home), sugar, and fats, and were associated with increased knowledge of COVID-19. Vitamin C and immunity-boosting supplement consumption were significantly associated with increased knowledge regarding COVID-19 (< 0.05). Inadequate knowledge about COVID-19 and the presence of anxiety and depression were found among most of the study participants. There is a need to conduct educational seminars to limit the health consequences resulting from COVID-19 lockdown.
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COVID-19/psicologia , Comportamento Alimentar , Conhecimentos, Atitudes e Prática em Saúde , Saúde Mental , SARS-CoV-2 , Adulto , COVID-19/epidemiologia , Estudos Transversais , Feminino , Humanos , Masculino , Paquistão/epidemiologia , Adulto JovemRESUMO
Hepatitis C is affecting millions of people around the globe annually, which leads to death in very high numbers. After many years of research, hepatitis C virus (HCV) remains a serious threat to the human population and needs proper management. The in silico approach in the drug discovery process is an efficient method in identifying inhibitors for various diseases. In our study, the interaction between Epigallocatechin-3-gallate, a component of green tea, and envelope glycoprotein E2 of HCV is evaluated. Epigallocatechin-3-gallate is the most promising polyphenol approved through cell culture analysis that can inhibit the entry of HCV. Therefore, various in silico techniques have been employed to find out other potential inhibitors that can behave as EGCG. Thus, the homology modelling of E2 protein was performed. The potential lead molecules were predicted using ligand-based as well as structure-based virtual screening methods. The compounds obtained were then screened through PyRx. The drugs obtained were ranked based on their binding affinities. Furthermore, the docking of the topmost drugs was performed by AutoDock Vina, while its 2D interactions were plotted in LigPlot+. The lead compound mms02387687 (2-[[5-[(4-ethylphenoxy) methyl]-4-prop-2-enyl-1,2,4-triazol-3-yl] sulfanyl]-N-[3(trifluoromethyl) phenyl] acetamide) was ranked on top, and we believe it can serve as a drug against HCV in the future, owing to experimental validation.
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Catequina/análogos & derivados , Hepacivirus/efeitos dos fármacos , Hepatite C/tratamento farmacológico , Proteínas do Envelope Viral/genética , Antivirais/química , Antivirais/farmacologia , Catequina/química , Catequina/farmacologia , Hepacivirus/genética , Hepacivirus/patogenicidade , Hepatite C/virologia , Humanos , Ligantes , Simulação de Acoplamento Molecular , Polifenóis/química , Polifenóis/farmacologia , Chá/química , Envelope Viral/química , Proteínas do Envelope Viral/antagonistas & inibidores , Internalização do Vírus/efeitos dos fármacosRESUMO
The present study was aimed to evaluate the effects of wheat germ oil and wheat bran fiber as fat replacers on quality and stability of low-fat beef patties. Total five treatments were prepared by employing wheat germ oil (WGO) and wheat bran fiber (WBF). WBF was used at fixed amount of 3% in all treatments except control in conjunction with varying WGO concentrations as follows: 1.5%, 3%, and 4.5%. Prepared raw and cooked beef patties were stored at 4°C, and further analyses were carried out up to 21 days of storage period with intermittent evaluation interval of 7 days. Higher values of TBARS, peroxide, and cholesterol were observed in raw and cooked beef patties in control, whereas minimum values were found in treatment of beef patties prepared with WGO 4.5% + WBF 3%. The physicochemical parameters were observed by pH and hunter color values. pH was higher in cooked patties as compared to beef patties and showed increases with increase in WGO concentration and storage intervals. The sensorial attributes were observed which included different parameters, such as appearance, texture, taste, odor, and overall acceptability. Higher score was given by the panelists to control for both raw and cooked beef patties; however, minimum score for all sensory properties was found in group treated with WGO 4.5% + WBF 3% within acceptable limit. In nutshell, raw and cooked beef patties treated with WGO 4.5% plus WBF 3% showed better quality, stability, and reduced cholesterol content.
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The modern-day review article is an exquisite attempt to demonstrate the extreme therapeutic potential of tamarind fruit (Tamarindus indica), particularly its pulp, seed, and leaf extract, against lifestyle-related chronic disorders. The rapid transition in the diet patterns and also the varying lifestyle of the people has made its way forth, a momentous upsurge in a number of chronic as well as degenerative diseases. An excess of foods having functional and nutraceutical significance has come into view recently. These foods have emerged as effective therapeutical remedies against these disorders owing to their natural phytochemical constituents present in them, in abundance. Tamarindus indica serves as a proverbial herbal medicine in each and every part of the world that is known to mankind. Also, the tamarind kernel powder (TKP) is of immense commercial significance in some of the major, leading industries of the World. The derivation of an important gel-forming substance (polysaccharide), named as "jellose," from the decorticated seed kernels of tamarind fruit has led to the manufacture of pectin. It is used in industrial scale in the preparation of various products like jams, jellies, and most important in the preparation of cheese. It plays an evident role as a stabilizer of commercial significance, and it has also been greatly recommend by the scientists to be used as a potent ingredient in a range of pharmaceutical products. The leaves of tamarind plant are also used as part of the daily diet in several countries where they are readily consumed in fresh form and especially during drought season.
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BACKGROUND: Fish meat and its products are usually accepted as good source of biological high value food components and especially for polyunsaturated fatty acids. The quality of fish meat products is considered to be decreased by the lipid peroxidation which leads to reduction in nutritional quality, financial loss and severe health problems. Many tactics are present to reserve their quality and safety. In the present investigation, the extraction and supplementation of optimal total polyphenol extracts (TPC) from vegetable and fruit by-products was explored for lipids oxidative stability and sensoric acceptability of functional fish product samples. METHODS: Vegetable and fruit by-products (cabbage leaves and banana peels) were collected from local fruits and vegetables processing industries. A 3-level five factor Box-Behnken design was used to study the effect of extraction/sonication temperature (°C), amplitude level, water/meal ratio, extraction/sonication time (minutes) and pH conditions for maximum yield of TPC from dried vegetable and fruit samples. The TPC samples were analyzed for chemical composition (total polyphenols, cyanogenic contents and tannins). Natural TPC extracts were supplemented at different concentration (0.5, 1 and 1.5%) to fish meat for preparation of different meat ball samples. The fish meat product samples without supplementation of TPC extract were kept as control. The partial/parfrying of the products was carried out to determine the lipid stability (peroxide value and free fatty acids) stored at refrigerator (for 9 days) and at - 18 °C in a freezer for a storage period of 60-days. The sensoric analysis (color, flavor and overall acceptability) was performed at different storage intervals for experimental treatments. RESULTS: The percent values of TPC yield from cabbage leave and banana peel samples ranged from a from minimum value of 9.8 ± 0.12% to a maximum value of 19.8 ± 0.15% for cabbage leaves and minimum value of 15.55 ± 0.13% to a maximum value of 24.4 ± 0.17% for banana peels, respectively. The results revealed that extraction conditions significantly affect the TPC yield from cabbage leaves and banana peels. The cabbage leaves and banana peels contain up to 4.8% total phenolics, cyanogenic compounds (1.44 - 1.47 ± 0.14) and tannins (6.55-7.90 ± 0.22). Peroxide values (meqO2 /kg) of meat balls treated with TPC extracts at 4 °C were in the range of 1.31 ± 0.12 to 3.10 ± 0.20 while at - 18 °C ranged was found 1.31 ± 0.12 to 1.55 ± 0.17, respectively. Peroxide values of all the treatments increased at the end of second interval then decreased at the end of last storage interval. Peroxide values of all treatments were higher and significantly different at the beginning and the end of the storage period (p < 0.05). In a similar way, free fatty acids and moisture content values trend was recorded for all experimental treatments. Sensory scores of fish product samples for color, flavor and overall acceptability showed a significant difference in sensory scores at refrigeration temperatures where sensory scores of fish product samples decreased significantly (p < 0.05) throughout refrigeration storage. Whereas, the sensory scores at the - 18 °C shows the good sensory characteristics, relatively. CONCLUSIONS: Phenolic extracts containing antioxidant status can interact with free lipidperoxy or lipidoxy free radicals (formed in result of lipid oxidation) and hence stopping their further self-breakdown. Plant-based phenolic extracts can be used to decrease oxidation process and increase the shelf life of fish meat products. Additional studies should be undertaken to determine the maximal shelf life of food products supplemented with different plant-based polyphenol extracts and treatment of nutritional disorders through their absorption, metabolism and distribution pattern into biological tissues.
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Suplementos Nutricionais , Produtos Pesqueiros , Extratos Vegetais , Antioxidantes , Manipulação de Alimentos/métodos , Qualidade dos Alimentos , Metabolismo dos Lipídeos , Oxirredução , Polifenóis , Verduras/químicaRESUMO
BACKGROUND: Recently oxidative stress induced maladies have amplified owing to sedentary lifestyle and monotonous diet. Introduction of plant based biomolecules may be a suitable strategy to cope with the lipid peroxidation. In this context, black tea polyphenols (theaflavin & thearubigins) are in fame among the scientific community as cost effective therapeutic agents owing to their safety, economics, structural diversity and ability to modulate various lipid peroxidation responses by halting the expression of different metabolic targets. METHODS: The mandate of present investigation was to first time check the synergism among the isolated theaflavins & thearubigins against lipid peroxidative indicators both in vitro and in vivo. Purposely, theaflavins and thearubigins were isolated from black tea through solvent partition methods by using different solvents (Aqueous ethanol, Aqueous methanol & Water) and time intervals (30, 60 & 90 min) and subjected to in vitro characterization through different antioxidant indices to access the in vitro lipid peroxidation shooting effect of these bioactive moieties. Moreover, individual theaflavins contents also estimate through HPLC. For evaluation of in vivo antioxidant effect, renal malfunction was induced through arginine and forty rats were divided in four groups (10 each after power analysis) and 04 types of diets were given i.e. T0 (control diet without supplementation), T1 (Basic experimental Diet+ theaflavins supplementation @ 1 g), T2 (Basic experimental Diet+ Thearubigins supplementation @ 1 g) & T3 (Basic experimental Diet+ Supplementation of theaflavins+ thearubigins @ 0.5 + 0.5 g, respectively) for the period of 56 days. Alongside, a control study was also carried out for comparison by involving normal rats fed on arginine free diet. The body weight, lipid profile, glycemic responses, Renal function test, liver function test, antioxidant indices and hematological parameters were estimated at the termination of study. RESULTS: The results indicated that theaflavins and thearubigins isolation was significantly affected by time of extraction and solvent. In this context, aqueous ethanol at 60 min extraction interval caused maximum extraction. Likewise, theaflavins isolate exhibited more antioxidant activity as compared to thearubigins. Moreover, the theaflavins and thearubigins based experimental diets imparted significant reduction in Lipid profile, glucose content, renal function tests and TBARS with enhancement in insulin, HDL and hematological parameters. In this context, theaflavin based diet caused maximum reduction in lipid profile and TBARS better as compared to thearubigins and theaflavins + thearubigins based. However, theaflavin+ thearubigins based diet caused highest glucose, urea & creatinine decline and maximum insulin increase & antioxidant indices as compared to other nutraceuticals. CONCLUSIONS: It was deduced that theaflavins & thearubigins have strong antioxidative potential both in in vitro as well as in vivo to tackle the menace associated with lipid peroxidation.
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Antioxidantes/farmacologia , Biflavonoides/farmacologia , Catequina/análogos & derivados , Polifenóis/farmacologia , Insuficiência Renal/dietoterapia , Chá/química , Administração Oral , Animais , Antioxidantes/isolamento & purificação , Arginina/administração & dosagem , Biflavonoides/isolamento & purificação , Biomarcadores/sangue , Compostos de Bifenilo/antagonistas & inibidores , Glicemia/metabolismo , Catequina/isolamento & purificação , Catequina/farmacologia , Creatinina/sangue , Testes de Função Renal , Peroxidação de Lipídeos/efeitos dos fármacos , Lipoproteínas HDL/sangue , Lipoproteínas LDL/sangue , Masculino , Estresse Oxidativo/efeitos dos fármacos , Picratos/antagonistas & inibidores , Polifenóis/isolamento & purificação , Ratos , Insuficiência Renal/sangue , Insuficiência Renal/induzido quimicamente , Insuficiência Renal/fisiopatologia , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Triglicerídeos/sangue , Ureia/sangueRESUMO
Epirubicin is an antineoplastic agent of anthracycline antibiotic, used for treating a variety of tumor types such as lymphoma, cancer of the breast, lung, ovary and stomach. The objective of this work was to demonstrate direct radiolabeling of epirubicin with 99mTc, quality control, biological characterization and scientigraphic evaluation in tumor bearing mice. The 99mTc-epirubicin labeling was optimized by varying the amounts of ligand 100-350µg, stannous chloride dihydride 20-50µg and pH range 2-10 by using NaOH or HCl. The radiochemical purity of 99mTc-epirubicin was evaluated by chromatographic techniques (Whatman No. 3 paper and ITLC-SG). HPLC analyses were performed to check purity of epirubicin and radiochemical purity of labeled 99mTc- epirubicin. Biodistribution and scintigraphic imaging of 99mTc-epirubicin was performed in normal and tumor bearing mice at various time intervals. The optimum conditions ensuring 99mTc-epirubicin labeling yield as high as 99% by adding 35µg SnCl2.2H2O, 200µg of ligand at pH 6 for 30 min at room temperature (25°C±2°C). HPLC of 99mTc-epirubicin shows about 99% binding of the compound with technetium-99m. Electrophoresis study indicated the neutral nature of 99mTc-epirubicin. Biodistribution data and scintigraphic results showed that 99mTc-epirubicin accumulated in the liver as well as in tumor with significant uptake and excellent retention. 99mTc-epirubicin shows good stability in human serum. In vitro and in vivo studies revealed the significantly uptake of 99mTc-epirubicin in the tumor, and also indicating the efficiency of 99mTc-epirubicin as a tumor diagnostic agent.
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Epirubicina/química , Marcação por Isótopo/métodos , Neoplasias Mamárias Experimentais/diagnóstico por imagem , Compostos Radiofarmacêuticos/farmacocinética , Tecnécio/farmacocinética , Animais , Estabilidade de Medicamentos , Epirubicina/farmacocinética , Feminino , Camundongos , Cintilografia/métodos , Compostos Radiofarmacêuticos/química , Tecnécio/química , Distribuição TecidualRESUMO
BACKGROUND: In recent decade, Hyperlipidemia related disorders like obesity, hypercholesterolemia and diabetes are considered as the leading killers for mankind. Fundamental nexus between nutrition and health diverting the consumers focus towards plant based natural products as a remedy against various metabolic syndrome. Considering this, present study was conducted to explicate the role of black tea polyphenols such as Theaflavins and thearubigins therapeutic potential to tackle targeted maladies especially oxidative stress related disorders like hypercholesterolemia and diabetes. METHODS: The mandate of current investigation was to explore the hypoglycemic and hypocholestrolemic perspective of isolated theaflavin and thearubigins through a model feeding trial. For the purpose, theaflavin & thearubigins were isolated from black tea through solvent partition method and utilize to form three types of nutraceutical drinks (theaflavin, thearubigins & theaflavin + thearubigins based) alongside control to be further utilized in bioefficacy trial. In bioefficacy trial, three types of independent studies were design on the bases of diet by involving 20 male wistar rats in each study (5 for each group). In study I, normal diet was administrated while, in study II & III high cholesterol and high sucrose diet was given, respectively along with prepared nutraceutical drinks to synchronize their therapeutic effect for a period of 56 days. At the termination of trial, Feed & drink intakes, body weight, total cholesterol, LDL, HDL, triglycerides, glucose and insulin levels were measured. RESULTS: The results indicated reduction in cholesterol, LDL and triglycerides levels of experimental rats in all studies with significant increase in HDL. In this context, theaflavin based drink imparted maximum reduction in cholesterol (3.75, 11.03 & 10.39%), LDL (3.84, 14.25& 10.84%) & triglycerides (2.99, 8.54 & 6.65%) in respective studies compared to thearubigins and theaflavin + thearubigins based drinks. However, theaflavin+ thearubigins based drink caused highest glucose decline and maximum insulin increase in all studies as compared to other nutraceutical drinks. The reported value for the insulin increase were 13.02 ± 1.02 & 14.55 ± 1.13, 10.09 ± 0.15 & 11.59 ± 0.86 for Hyperglycemic and Hypocholestrolemic rats respectively compared to control (7.84 ± 0.45 & 9.10 ± 0.41) for study I and II. CONCLUSIONS: In the nutshell, theaflavin and thearubigins based dietary interventions are helpful to alleviate the hypercholestrolemia and hyperglycemia and should be promoted as parallel therapy to combat these disorders.