RESUMEN
OBJECTIVES: Thyroid Cancer is one of the rarest cancers but its prevalence has been increasing worldwide for the last couple of decades. METHODS: The data collection tool was designed to assess knowledge, awareness, perception, and attitude towards preventive practices of thyroid cancer in Pakistani university students. The data were collected over a duration of six months and a total number of 3722 students participated. RESULTS: The knowledge of risk factors of thyroid cancer was an important parameter of this study. The students who knew all the early signs of thyroid cancer were 28.7%. In this study, the independent variables such as age, gender, demographic location, and financial status were found to be highly significant with knowledge, attitude towards warning signs of cancer, and the perception of students about developing thyroid cancer. CONCLUSIONS: The participants were found to have poor knowledge about early signs of thyroid cancer. The study participants perception, behavior, and attitude towards preventive practices of thyroid cancer were found inadequate and appropriate measures on a National level should be taken to enhance the knowledge about preventive practices of thyroid cancer. Increasing knowledge and awareness shall help decrease the overall morbidity and mortality linked with thyroid carcinomas and thyroid diseases.
Asunto(s)
Estudiantes de Medicina , Estudiantes , Neoplasias de la Tiroides/prevención & control , Adolescente , Adulto , Factores de Edad , Actitud , Estudios Transversales , Femenino , Conocimientos, Actitudes y Práctica en Salud , Humanos , Masculino , Pakistán , Factores de Riesgo , Factores Sexuales , Factores Socioeconómicos , Encuestas y Cuestionarios , Neoplasias de la Tiroides/epidemiología , Universidades , Adulto JovenRESUMEN
The descriptive cross-sectional study was planned to evaluate drug-related problems, including drug-drug interactions, dose error, use of nephrotoxic drugs and polypharmacy, with special emphasis on kidney disease patients. The study was conducted from January to June 2019 in the Nephrology Ward of Ayub Teaching Hospital, Abbottabad, Pakistan. Doses of medicine and drug-drug interactions were evaluated by comparing it with standard protocols in British National Formulary and Lexicomp. Prescriptions were also evaluated for polypharmacy and use of nephrotoxic drugs. Out of 131 patients, 72 (55%) were males. Drug-drug interactions were found in 69 (52.7%) patients among whom the highest percentage was of moderate drug-drug interaction 63 (48.1%), followed by major 39 (29.8%) and minor 29 (22%) drug-drug interactions. Incidence of polypharmacy 68 (51.9%) and use of nephrotoxic drug 101 (77%) was high, while dose error was low 14 (10.7%). All drug-related problems were present with a high percentage in patients with chronic kidney diseases 29 (78.4) out of 37 (28.2%) such patients. There was significant association of chronic kidney diseases stages with drug-drug interactions, polypharmacy, dose error and prescribing drugs (p<0.05). The higher incidence of drug-related problems reflected irrational prescribing trends and deficiency of professional staff dealing with kidney disease patients.
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Preparaciones Farmacéuticas , Insuficiencia Renal Crónica , Estudios Transversales , Prescripciones de Medicamentos , Humanos , Prescripción Inadecuada , Masculino , Polifarmacia , Insuficiencia Renal Crónica/epidemiologíaRESUMEN
Biogenic production of nanoparticles is eco-friendly, less expensive method with various medical and biological applications. Nanotechnology along with photodynamic therapy is gaining tremendous importance with enhanced efficacy. The present work was aimed to evaluate methanolic extracts and nanoparticles of two selected plants (Datura suavolens and Verbina tenuisecta) for cytotoxic photodynamic, antioxidant and antimicrobial study. Both extract and silver (5 mM) nanoparticles of Datura plant showed significant activities against bacterial strains. Maximum ZOI of 27.3 ± 1.6 mm was observed with nanoparticles of Datura branches with minimum inhibitory (MIC) value of 32 µg/ml. In case of antifungal and antioxidant assay samples were moderately active. Silver nanoparticles and extracts were effective against rhabdomyosarcoma cell line with lowest IC50 value of 42.5 ± 0.6 µg/ml and percent viability of 25.6 ± 1.3 of Verbena tenuisecta. However, nanoparticles of Datura leaves and branches were more potent with IC50 value of 2.4 ± 0.9 µg/ml and 7.8 ± 1.1 µg/ml respectively. The result of photodynamic study showed that efficacy of photosensitizer was enhanced and percent viability reduced when nanoparticles used as an adjunct. The color change and UV spectra (415â425 nm) indicated the production of nanoparticles. Fourier transform infrared spectroscopy (FTIR) spectra showed presence of different functional groups e.g., hydroxyl, carbonyl and amino. Nanoparticles are sphenoid in morphology and size ranges between 20-150 nm. Current study showed these silver nanoparticles can be used as cytotoxic agent in photodynamic therapy and can play a critical role to establish medicinal potential of selected plants.
Asunto(s)
Datura/química , Metanol/farmacología , Plata/farmacología , Verbena/química , Antiinfecciosos/química , Antiinfecciosos/aislamiento & purificación , Antiinfecciosos/farmacología , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Humanos , Nanopartículas del Metal , Metanol/química , Metanol/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Fármacos Fotosensibilizantes/química , Fármacos Fotosensibilizantes/aislamiento & purificación , Fármacos Fotosensibilizantes/farmacología , Extractos Vegetales/química , Hojas de la Planta/química , Plata/química , Plata/aislamiento & purificaciónRESUMEN
Hepatitis C virus (HCV) has major role in spreading of liver diseases worldwide. The HCV nonstructural NS5B is a polymerase (RdRp) that is present at the carboxylic-end of the polyprotein chain. It is essential and most important for the replication cycle. In current study, the potential of 100 phytochemicals against HCV NS5B polymerase was determined. Phytochemical structures were retrieved from PubChem database. The phytochemicals were docked with the NS5B active site amino acids, in order to discover their attractions as inhibitors. After docking, molecules with top five conformations were selected from 100 molecules by docking scores and RMSD values. The results demonstrated strong interactions of phytochemicals with the NS5B. The selected compounds with best docking scores and RMSD were found to be glycitein, ferulic acid, eugenol, 1-octanol and sebacic acid. These were further evaluated through Lipinski's rule of five to explore their molecular properties and drug-likeliness characteristics and all five selected phytochemicals were found to have drug-likeliness characteristics. Further, according to ADME analysis, the ferulic acid, 1-octanol and eugenol were found to be nontoxic, non-carcinogenic and have the ability to cross the blood brain barriers. Therefore, these phytochemicals could be strong drug candidates for HCV NS5B.
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Antivirales/farmacología , Desarrollo de Medicamentos , Inhibidores Enzimáticos/farmacología , Hepacivirus/efectos de los fármacos , Simulación del Acoplamiento Molecular , Fitoquímicos/farmacología , Proteínas no Estructurales Virales/antagonistas & inhibidores , Absorción Fisiológica , Antivirales/química , Antivirales/farmacocinética , Dominio Catalítico , Vías de Eliminación de Fármacos , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacocinética , Hepacivirus/enzimología , Humanos , Modelos Biológicos , Fitoquímicos/química , Fitoquímicos/farmacocinética , Unión Proteica , Distribución Tisular , Proteínas no Estructurales Virales/química , Proteínas no Estructurales Virales/metabolismoRESUMEN
Current outbreak of dengue has shown serious health concerns in Pakistan. The present study reports the anti-dengue potential of Carica papaya natural compounds. The leaves of C. papaya have previously shown promising results in cure of Dengue fever. The aim of this project is to find specific bioactive compounds by computational screening and biological activities of C. papaya against serine NS2B, NS3 and NS5 proteases of dengue virus. Docking study resulted in the screening of nine bioactive compounds having highest docking scores. However, three compounds namely epigallocatchin, catechin and protocatechuric acid had the strongest binding affinity with the active residues i.e., Ser135, His51 and Asp75 of dengue virus serine proteases. Results also indicated that the extract of C. papaya was a strong antimicrobial and antioxidant agent. It is concluded that the C. papaya compounds can be commercially applied for medical formulations against dengue virus.
Asunto(s)
Carica , Virus del Dengue/efectos de los fármacos , Fitoquímicos/farmacología , Inhibidores de Proteasas/farmacología , Serina Endopeptidasas , Proteínas no Estructurales Virales/antagonistas & inhibidores , Dengue/tratamiento farmacológico , Virus del Dengue/enzimología , Humanos , Simulación del Acoplamiento Molecular/métodos , Fitoquímicos/uso terapéutico , Inhibidores de Proteasas/aislamiento & purificación , Inhibidores de Proteasas/uso terapéutico , Serina Endopeptidasas/metabolismo , Proteínas no Estructurales Virales/metabolismoRESUMEN
The current study is an attempt to explore the effect of varying quantities of hydroxypropyl cellulose (HPC) polymer on carbamazepine (CBZ) cocrystal formation with dicarboxylic acid coformers i.e., malonic acid (MA), succinic acid (SA), glutaric acid (GA), and adipic acid (AA). The cocrystals were first prepared without polymer by slurry crystallization method and then tried with different quantities of the polymer. The prepared samples were characterized by Powder X-ray Diffraction (XRPD). The characterization results indicate that in methanol pure carbamazepine-malonic (CBZ-MA) and carbamazepine-adipic acid (CBZ-AA) cocrystal can be prepared, while in ethanol and acetone pure carbamazepine-succinic (CBZ-SA) and carbamazepine-glutaric acid (CBZ-GA) cocrystals can be obtained respectively. The same cocrystals were tried using HPC polymer in three different quantities. The characterization results showed that a higher quantity of HPC polymer transforms CBZ-MA cocrystal polymorph-I to polymorph-II. The CBZ-SA and CBZ-GA cocrystal formation somehow inhibited as the concentration of HPC polymer increases. But on the other side, the formation of CBZ-AA cocrystal utterly not inhibited in the presence of varying quantities of HPC polymer. Furthermore, 11 different quantities of HPC were tried to know about the inhibitory concentration of HPC on CBZ-AA cocrystal formation. The CBZ-AA cocrystal preparation was not inhibited even at higher quantities of HPC compared to the coformer. Additionally, the effect of three different quantities of HPC on the thermal stability of the CBZ-AA cocrystal was investigated. Moreover, the stability of pure CBZ at 92% relative humidity (RH) condition was compared to CBZ-AA cocrystal with and without HPC polymer. The CBZ-AA cocrystal with and without HPC polymer was more stable than pure CBZ.
Asunto(s)
Carbamazepina/química , Ácidos Carboxílicos/química , Polímeros/química , Rastreo Diferencial de Calorimetría/métodos , Cristalización/métodos , Glutaratos/química , Malonatos/química , Polvos/química , Solubilidad/efectos de los fármacos , Difracción de Rayos X/métodosRESUMEN
Aim of this study was to synthesize new inhibitors on the basis of active site of aspartic protease enzyme and to evaluate their intended biological activity. A3D model of an enzyme was generated via homology modeling and series of novel amide ligands were synthesized by using a short high yield process, subsequently, analyzed in-silico and in-vitro anti-leishmanial activities. Characterization and identification was accomplished via NMR (H1& C13), infrared and mass spectroscopic techniques. Among all compound (4) was found to show significant activity (IC50 58±0.01) against Leishmania major (L. major) species. Furthermore, docking studies confirmed the inhibition of a targeted enzyme that supported the interaction of potent compound (4) with key residues (aspartic protease) via hydrogen bonds. Present study conferred about novel compound (4) as a promising compound to antagonize L. major activities in future.
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Amidas/síntesis química , Antiprotozoarios/síntesis química , Leishmania/efectos de los fármacos , Simulación del Acoplamiento Molecular/métodos , Amidas/metabolismo , Amidas/farmacología , Antiprotozoarios/metabolismo , Antiprotozoarios/farmacología , Leishmania/metabolismo , Ligandos , Estructura Molecular , Estructura Secundaria de Proteína , Relación Estructura-ActividadRESUMEN
OBJECTIVE: To assess the knowledge, attitude and practice of hepatitis B and C patients towards the disease. METHODS: The cross-sectional, descriptive, questionnaire-based study was conducted at the Rawalpindi Medical University (RMU) and its allied hospitals, Rawalpindi, Pakistan, from October to December 2017, and comprised hepatitis B and C patients aged ≥18 years who were visiting the outpatient department. A structured, close-ended, 30-item questionnaire was used to collect data which was then analysed using SPSS 23. . RESULTS: Of the 399 patients, 230(57.6%) were women, 103(26%) did not have any formal education, and TV, radio and the internet was the main source of information regarding hepatitis for 138(34.6%) patients. The overall mean age was 42.82}11.78 years. The sample showed poor knowledge with a mean score of 7.33}2.03, adequate attitude with a mean of 4.33}1.19, and poor practice with a mean of 2.97}1.05. Correlation was statistically significant between knowledge and practice (p<0.01). CONCLUSIONS: Lack of imperative knowledge of hepatitis in patients was the main reason for negative attitude and poor practices.
Asunto(s)
Conocimientos, Actitudes y Práctica en Salud , Hepatitis B Crónica , Hepatitis C Crónica , Adolescente , Adulto , Información de Salud al Consumidor , Escolaridad , Femenino , Humanos , Internet , Masculino , Persona de Mediana Edad , Servicio Ambulatorio en Hospital , Pakistán , Encuestas y Cuestionarios , Televisión , Centros de Atención Terciaria , Adulto JovenRESUMEN
Sofosbuvir along with ribavirin is being widely used for treatment of HCV in Pakistan but it may show delayed response and reoccurrence of disease in some cases. The aim of the study was to investigate pharmacokinetics and concentration effect analysis of sofosbuvir. HCV patients (n=100) received 400 mg sofosbuvir along with low dose or weight based ribavirin (400 mg). Nonlinear mixed effects modeling (NONMEM) and unpaired t-test were used for the association of concentrations and treatment outcomes. Average day 10 sofosbuvir metabolite BM 331007 concentration was higher in patients having haemoglobin nadir value <10 g/dl compared to the patients having heamoglobin nadir value >10 g/dl (5.34 versus 4.87 pmol/106 cells; p=0.03). The average concentration trends of GS331007 at day 10 was towards being higher in the patients achieved sustained virologic response (SVR) as compare to the patients relapsed (5.19 versus 4.86 pmol/106 cells; p=0.05). Sofosbuvir (GS331007) thresholds concentration (suggested at day 10 through receiver operating characteristic curve) was 5.4 pmol/106 cells for SVR (p=0.05) and haemoglobin nadir cells was 6.3 pmol/106 with sensitivity and specificity of >60%. Dosing simulations shows that 400 mg sofosbuvir twice daily produce day 10 concentration range of 5.4 to 6.7 pmol/106 cells. The range of therapeutic values was identified for HCV patients receiving sofosbuvir in combination with ribavirin for 24 weeks, suggesting a potential pharmaceutical basis for individualized therapeutic dosing.
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Antivirales/farmacocinética , Hepatitis C/tratamiento farmacológico , Ribavirina/farmacología , Sofosbuvir/farmacocinética , Adulto , Anciano , Antivirales/administración & dosificación , Antivirales/sangre , Quimioterapia Combinada , Femenino , Semivida , Humanos , Masculino , Persona de Mediana Edad , Curva ROC , Ribavirina/administración & dosificación , Sofosbuvir/administración & dosificación , Sofosbuvir/sangre , Respuesta Virológica SostenidaRESUMEN
Medicinal plants of Pakistan are known for their curative properties against snake bite as rural people have been using natural herbs for such injuries for hundreds to thousands of years. People of rural areas of Pakistan are prone to snakebite, and on the whole death due to snakebite has been increasing worldwide. The objective of this study was to test the neutralizing potential of 17 Pakistani medicinal plant extracts against phospholipase A2 activity in Echis carinatus venom. Plant material was extracted by simple maceration and fractionation of active plant extracts. Venom was collected by manual massage of the venom glands. The PLA2 enzymatic assay was performed to map out the venomous activity of Echis carinatus envenomation. Snake venom released fatty acids at different concentrations (0.1-5 mg/ml) of venom in a dose-dependent manner. Reduction of pH by 01 correlated with 133 µmol of fatty acids released at 5mg/ml of venom. All plants extract inhibited PLA2 activity, however, Curcuma longa, Citrullus colocynthis and Rubia cordifolia inhibited maximum of PLA2 activity (â78%) comparable to the standard antidote (p>0.5). Medicinal plants possess secondary metabolites and many active compounds that may have neutralizing or inhibiting properties against the PLA2 activity of Echis venom. Further studies such as compound analysis could provide an alternative against snakebites injuries resulting from Echis carinatus venom.
Asunto(s)
Fosfolipasas A2/toxicidad , Extractos Vegetales/farmacología , Plantas Medicinales , Venenos de Víboras/toxicidad , Proteínas Sanguíneas/farmacología , Pakistán , Plantas Medicinales/química , Mordeduras de Serpientes/tratamiento farmacológicoRESUMEN
OBJECTIVE: To evaluate the knowledge, attitude and practice of self-medication in medical undergraduate students. METHODS: This cross-sectional questionnaire-based survey was conducted from January to June, 2017, among undergraduate students of Ayub Teaching Hospital, Women Medical College, International Medical College and Frontier Medical College in Abbottabad, Pakistan. The sample comprised students of first, second, third, fourth and fifth professional year. Data was collected using self-generated questionnaire. RESULTS: Of the 400 subjects approached, 300(75%) returned the questionnaire fully completed. Of them, 208 (69.3%) were females and 92(30.66%) were males. The most common age group was 22-25 years 182(60.7%). Self-medication was found to be prevalent among 297(99%) subjects and 139(46.3%) respondents had practised self-medication in the preceding 6 months more than two times. Over-the-counter drugs were commonly used for the self-medication in 295(98.3%) cases. Overall, 285(95%) respondents had a positive attitude towards self-medication. Media was found to be the most common source of information for 93(31%) cases. CONCLUSIONS: High prevalence of self-medication was noticed, with over-the-counter drugs being the most commonly used. Proper educational awareness programmes about self-medication can control the issue.
Asunto(s)
Conocimientos, Actitudes y Práctica en Salud , Automedicación , Estudiantes de Medicina , Adulto , Actitud Frente a la Salud , Estudios Transversales , Femenino , Humanos , Masculino , Medicamentos sin Prescripción/uso terapéutico , Pakistán/epidemiología , Prevalencia , Automedicación/métodos , Automedicación/psicología , Automedicación/estadística & datos numéricos , Estudiantes de Medicina/psicología , Estudiantes de Medicina/estadística & datos numéricos , UniversidadesRESUMEN
Neuroendocrine tumors (NET) are the rare tumors which often impose graveyard threat. These tumors are characterized by the over expression of various G-protein coupled receptors including cholecystokinin (CCK) receptors-1 and 2 (A or B). Minigastrin peptides are being investigated for theranostic purposes of CCK-2 receptor positive NET. The minigastrin analogue (APHO70) was modified by engineering enzyme susceptible tetrapeptide sequence into APHO70 peptide to reduce the random degradation by lysosome enzymes which pave the way to random trafficking in patient's body and dipeptide addition at c-terminus. All the four modified minigastrin peptides (MG-CL1-4) were investigated for lysosome cathepsin B (catB) enzyme susceptibility and fate into AR42J cancer cell line. The indium-111 labeled MG-CL1-4 peptides were also studied for target (tumor) and non-target saccumulation by using tumor induced mice. The RP-HPLC analysis result showed nonspecific cleavage of standard 111In-APH070 and 111In-MGCL1 while specific cleavage was noted in case of 111In-MGCL (2-4). The effect of specific and non-specific cleavage on biodistribution in tumor induced nude mice model indicates the promising accumulation of 111In-MGCL2, 111In-MGCL3, and 111In-MGCL4 radiotracers while 111In-MGCL1 showed less accumulation. 111In-MGCL2 and 111In-MGCL3 showed highest target-to-kidney ratio (T/K) i.e. 1.71 and 1.72, respectively whereas standard compound showed T/K 1.13. In conclusion, the two indium-111 labeled analogues i.e. 111In-MGCL2 and 111In-MGCL3 showed promising sensitivity for tumor andcould be tested for further investigation to reach pre-clinical studies.
Asunto(s)
Catepsina B/metabolismo , Gastrinas/metabolismo , Radioisótopos de Indio/metabolismo , Tumores Neuroendocrinos/metabolismo , Fragmentos de Péptidos/metabolismo , Radiofármacos/metabolismo , Animales , Línea Celular Tumoral , Femenino , Ratones , Ratones Desnudos , Tumores Neuroendocrinos/diagnóstico por imagenRESUMEN
Bacterial infection is one of the vital sources of morbidity and mortality. The development of single photon emission computed tomography (SPECT) radiotracer agents using antibiotics, for targeting in-vivo bacteria, helps in antibiotic dose calibration, targeted infection therapy and reduction in mortality rate. The aim of this study was to appraised 99mTc-labeling sulfadiazine as a radiopharmaceutical for bacillus infections imaging. Radiolabeling of sulfadiazine with technetium-99m was carried out by subsequent addition of 1.5 mL aqueous solution of sulfadiazine (1mg/mL), 120µg stannous tartrate, gentistic acid as stabilizing agent and 185 MBq normal saline solution of 99mTcO4-1 (pertechnetate) at pH = 5. The reaction mixture was incubated for 40 min at room temperature with light stirring. The quality control analysis (ITLC-SG and paper chromatography analysis) revealed ~ 98% labeling yield. Biodistribution and scintigraphic study was carried using bacillus bacterial infection induced New Zealand white rabbits. Due to the ease of 99mTc-sulfadiazine conjugation method, high labeling efficiency, shelf stability (>95% up to 6h), blood serum stability (~90% up to 6h) and high uptake in the infected muscle (T/NT =2.21 at 1H), 99mTc-SDZ could be used as radiopharmaceutical of choice for further pre-clinical and clinical studies.
Asunto(s)
Antibacterianos/metabolismo , Bacillus , Modelos Animales de Enfermedad , Infecciones por Bacterias Grampositivas/metabolismo , Sulfadiazina/metabolismo , Tecnecio/metabolismo , Animales , Antibacterianos/uso terapéutico , Bacillus/aislamiento & purificación , Evaluación Preclínica de Medicamentos/métodos , Infecciones por Bacterias Grampositivas/diagnóstico por imagen , Infecciones por Bacterias Grampositivas/tratamiento farmacológico , Humanos , Masculino , Tomografía de Emisión de Positrones/métodos , Conejos , Sulfadiazina/uso terapéutico , Tecnecio/administración & dosificación , Distribución Tisular/efectos de los fármacos , Distribución Tisular/fisiología , Tomografía Computarizada de Emisión de Fotón Único/métodosRESUMEN
OBJECTIVE: To investigate the efficacy and impact of Protection Against Harassment of Women at Workplace Act 2010 in the public health sector in its socio-legal perspective. METHODS: This cross-sectional study was conducted from July to December 2014 in Abbottabad, Pakistan, and comprised subjects selected from 53 basic health units managed by the government. SPSS 20 was used for statistical analysis. RESULTS: Of the 450 questionnaires, 430(96.6%) were returned duly filled. Overall, 40% male (120 respondents) and 26% female (34 respondents) knew about the Act. Besides, 39% males (117 respondents) and 63% females (82 respondents) appeared unsatisfied with the complaint mechanism prescribed in the Act; all the respondents established that no case had been registered after the introduction of the Act. Overall, 31% males (93 respondents) and 57% females (74 respondents) thought that without the health governance commitment and social support structure the Act could not work. CONCLUSIONS: The Protection Against Harassment of Women at Workplace Act 2010 was considered ineffective by the respondents who were concerned about the lack of social support system for the Act.
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Personal de Salud/estadística & datos numéricos , Sector Público/legislación & jurisprudencia , Acoso Sexual , Mujeres Trabajadoras/legislación & jurisprudencia , Lugar de Trabajo/legislación & jurisprudencia , Estudios Transversales , Femenino , Humanos , Masculino , Pakistán , Administración en Salud Pública/legislación & jurisprudencia , Acoso Sexual/legislación & jurisprudencia , Acoso Sexual/prevención & controlRESUMEN
Benzylpenicillin acts through binding with beta-lactamase enzyme and inhibiting the bacterial cell wall biosynthesis. Therefore, the radiolabeling of benzylpenicillin with lutetium-177 is expected to serve as a theranostic agent for deep-seated bacterial infections. The radiolabeling of benzylpenicillin resulted ~93% radiochemical yield at optimized reaction conditions. Radiochemical purity analysis was tested with the help of Whatman No. 2 paper and instant thin layer chromatography. Biodistribution study with healthy New Zeeland white rabbit revealed moderate accumulation in different organs. Kidneys are the major organs, showed not more than 4.57±0.89% injected dose per gram organ (ID/gm organ) at 1 h time point and 3.48±1.11% ID/gm organ at 6 h time point. The accumulation of tracer agent in liver was found in the range of 7.42±2.42% to 9.09±2.76 ID/gm organ. The glomerular filtration rate studies revealed rapid clearance - omitting the chance of nephrotoxicity. The radiolabeling yield, biodistribution and glomerular filtration rate results revealed 177Lu-benzylpencillin could be a potential candidate to diagnose the deep-seated bacterial infection.
Asunto(s)
Antibacterianos/farmacocinética , Lutecio/farmacocinética , Penicilina G/farmacocinética , Radioisótopos/farmacocinética , Radiofármacos/farmacocinética , Nanomedicina Teranóstica/métodos , Tomografía Computarizada de Emisión de Fotón Único , Animales , Antibacterianos/administración & dosificación , Estabilidad de Medicamentos , Marcaje Isotópico , Riñón/diagnóstico por imagen , Riñón/metabolismo , Hígado/diagnóstico por imagen , Hígado/metabolismo , Lutecio/administración & dosificación , Penicilina G/administración & dosificación , Penicilina G/análogos & derivados , Conejos , Radioisótopos/administración & dosificación , Radiofármacos/administración & dosificación , Eliminación Renal , Distribución TisularRESUMEN
Eucalyptus is well reputed for its use as medicinal plant around the globe. The present study was planned to evaluate chemical composition, antimicrobial and antioxidant activity of the essential oils (EOs) extracted from seven Eucalyptus species frequently found in South East Asia (Pakistan). EOs from Eucalyptus citriodora, Eucalyptus melanophloia, Eucalyptus crebra, Eucalyptus tereticornis, Eucalyptus globulus, Eucalyptus camaldulensis and Eucalyptus microtheca were extracted from leaves through hydrodistillation. The chemical composition of the EOs was determined through GC-MS-FID analysis. The study revealed presence of 31 compounds in E. citriodora and E. melanophloia, 27 compounds in E. crebra, 24 compounds in E. tereticornis, 10 compounds in E. globulus, 13 compounds in E. camaldulensis and 12 compounds in E. microtheca. 1,8-Cineole (56.5%), α-pinene (31.4%), citrinyl acetate (13.3%), eugenol (11.8%) and terpenene-4-ol (10.2%) were the highest principal components in these EOs. E. citriodora exhibited the highest antimicrobial activity against the five microbial species tested (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Aspergillus niger and Rhizopus solani). Gram positive bacteria were found more sensitive than Gram negative bacteria to all EOs. The diphenyl-1-picrylhydazyl (DPPH) radical scavenging activity and percentage inhibition of linoleic acid oxidation were highest in E. citriodora (82.1% and 83.8%, respectively) followed by E. camaldulensis (81.9% and 83.3%, respectively). The great variation in chemical composition of EOs from Eucalyptus, highlight its potential for medicinal and nutraceutical applications.
Asunto(s)
Antiinfecciosos/química , Antioxidantes/química , Eucalyptus/química , Aceites Volátiles/química , Extractos Vegetales/química , Antibacterianos/química , Antibacterianos/farmacología , Antiinfecciosos/farmacología , Antioxidantes/farmacología , Cromatografía de Gases y Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/farmacología , Extractos Vegetales/farmacologíaRESUMEN
The 2A proteinase (2A(pro)) is an enterovirally encoded cysteine protease that plays essential roles in both the processing of viral precursor polyprotein and the hijacking of host cell translation and other processes in the virus life cycle. Crystallographic studies of 2A(pro) from enterovirus 71 (EV71) and its interaction with the substrate are reported here. EV71 2A(pro) was comprised of an N-terminal domain of a four-stranded antiparallel ß sheet and a C-terminal domain of a six-stranded antiparallel ß barrel with a tightly bound zinc atom. Unlike in other 2A(pro) structures, there is an open cleft across the surface of the protein in an open conformation. As demonstrated by the crystallographic studies and modeling of the complex structure, the open cleft could be fitted with the substrate. On comparison 2A(pro) of EV71 to those of the human rhinovirus 2 and coxsackievirus B4, the open conformation could be closed with a hinge motion in the bII2 and cII ß strands. This was supported by molecular dynamic simulation. The structural variation among different 2A(pro) structures indicates a conformational flexibility in the substrate-binding cleft. The open structure provides an accessible framework for the design and development of therapeutics against the viral target.
Asunto(s)
Cisteína Endopeptidasas/química , Enterovirus Humano A/enzimología , Modelos Moleculares , Conformación Proteica , Secuencia de Aminoácidos , Cristalografía por Rayos X , Cisteína Endopeptidasas/genética , Escherichia coli , Transferencia Resonante de Energía de Fluorescencia , Vectores Genéticos/genética , Datos de Secuencia Molecular , Mutagénesis , Reacción en Cadena de la Polimerasa , Alineación de SecuenciaRESUMEN
Abstract: The objective of this study was to fabricate topical formulations of diclofenac diethylamine (DD) using isopropyl myristate (IPM) and isopropyl palmitate (IPP) as permeation enhancers. Franz cell and bacterial cellulose were used as analytical instrument and diffusion membrane, respectively. Permeation enhancers exhibited significant effect on the permeation characteristics of DD. It was concluded from the results that improved permeation of DD was observed when IPP was used as enhancer.
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Antiinflamatorios no Esteroideos/farmacocinética , Celulosa/metabolismo , Diclofenaco/farmacocinética , Excipientes/química , Administración Cutánea , Antiinflamatorios no Esteroideos/administración & dosificación , Bacterias , Diclofenaco/administración & dosificación , Membranas/metabolismo , Miristatos/química , Palmitatos/química , Permeabilidad , Absorción CutáneaRESUMEN
This research aims to optimize the silk and wool dyeing process using natural dyes from Bixa orellana (annatto) through response surface methodology. Central composite design experiments highlight the significant enhancement of color outcomes achieved through microwave treatment. For silk, the optimal conditions (80â °C for 40â min) with annatto extract yield a color strength (K/S) of 17.8588, while wool achieves a K/S of 7.5329. Introducing eco-friendly bio-mordants, such as pomegranate peel and red sumac tannins, enhances color strength. Pre-dyeing treatments with 2% red sumac, 1.5% pomegranate peel, and weld flower extracts for silk produce high color strength, with K/S values of 16.4063, 16.3784, and 12.1658, respectively. Post-dyeing, the K/S values increase to 40.1178, 17.4779, and 21.6494. Wool yarn exhibits similar improvements, with pre-dyeing K/S values of 13.1353, 13.5060, and 16.3232, escalating to 10.5892, 15.3141, and 23.4850 post-dyeing. Furthermore, this research underscores improved colorfastness properties, including notable enhancements in light, wash, and rubbing fastness for both silk fabric and wool yarn. These findings underscore the efficacy of the proposed sustainable dyeing methods, offering valuable insights for eco-friendly textile production.
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Carotenoides , Árboles , Lana , Animales , Bixaceae , Textiles , Semillas , SedaRESUMEN
The kidney plays a crucial role in regulating homeostasis within the human body. Renal cell carcinoma (RCC) is the most common form of kidney cancer, accounting for nearly 90â¯% of all renal malignancies. Despite the availability of various therapeutic strategies, RCC remains a challenging disease due to its resistance to conventional treatments. Nanotechnology has emerged as a promising field, offering new opportunities in cancer therapeutics. It presents several advantages over traditional methods, enabling diverse biomedical applications, including drug delivery, prevention, diagnosis, and treatment. Lipid nanoparticles (LNPs), approximately 100â¯nm in size, are derived from a range of lipids and other biochemical compounds. these particulates are designed to overcome biological barriers, allowing them to selectively accumulate at diseased target sites for effective therapeutic action. Many pharmaceutically important compounds face challenges such as poor solubility in aqueous solutions, chemical and physiological instability, or toxicity. LNP technology stands out as a promising drug delivery system for bioactive organic compounds. This article reviews the applications of LNPs in RCC treatment and explores their potential clinical translation, identifying the most viable LNPs for medical use. With ongoing advancement in LNP-based anticancer strategies, there is a growing potential to improve the management and treatment of renal cancer.