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1.
Pak J Pharm Sci ; 37(1): 163-171, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38741413

RESUMO

Medicinal plants contain a wide variety of bioactive phytoconstituents which can serve as new therapeutic agents for several diseases. This study examines the antidiabetic potential of Aitchisonia rosea in alloxan-induced diabetic rats and identifies its bioactive phytoconstituents using GC-MS. In vitro, antidiabetic potential was established using the α-amylase inhibition assay. In vivo, antidiabetic potential was investigated by employing the oral glucose tolerance test (OGTT). GC-MS analysis was used to identify the bioactive phytoconstituents. The in vitro and in vivo tests showed that the aqueous extract of A. rosea possesses better antidiabetic potential. The α-amylase inhibition assay highlighted an IC50 value of 134.87µg/ml. In an oral glucose tolerance test, rats given an aqueous A. rosea extract significantly lowered their blood sugar levels significant reduction in the blood glucose concentration was observed in the oral glucose tolerance test in rats treated with the aqueous A. rosea extract. GC-MS investigation revealed many phytoconstituents, with serverogenin acetate and cycloheptasiloxane tetradecamethyl being important antidiabetic agents. This study found anti-diabetic properties in A. rosea extract. The phytochemical and GC-MS investigation also found serverogenin acetate and cycloheptasiloxane tetradecamethyl, which could be used to develop new antidiabetic drugs.


Assuntos
Glicemia , Diabetes Mellitus Experimental , Cromatografia Gasosa-Espectrometria de Massas , Hipoglicemiantes , Componentes Aéreos da Planta , Extratos Vegetais , Animais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Componentes Aéreos da Planta/química , Masculino , Glicemia/efeitos dos fármacos , Ratos , Teste de Tolerância a Glucose , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , Ratos Wistar , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Aloxano
2.
Pak J Pharm Sci ; 36(6): 1695-1707, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-38124409

RESUMO

Diabetes mellitus (DM), a prevalent metabolic condition that impairs glucose metabolism, causes morbidity and hospitalization. Thus, there is need to establish novel therapeutics against DM. The current study examined the phytochemical analysis and antidiabetic effects of Carissa grandiflora leave extracts (CGLE) on streptozotocin (STZ)-induced DM in mice. CGLE (n-hexane, chloroform, ethanol) was extracted and phytochemically examined for primary and secondary metabolites. Fourier transformed infrared spectroscopy (FTIR) detected functional groups, while 2,2-diphenyl-1-picrylhydrazyl (DPPH) test assessed antioxidant capacity. Later, antidiabetic potential of CGLE extract was investigated in vivo in STZ induced diabetic mice. Phytochemical investigation revealed sugars, ketones, alkaloids, triterpenoids, and glycosides. FTIR indicated phenol, aldehyde, ketone, alkene, alkyne, alcohol, benzene ring and amines, while DPPH assay demonstrated antioxidant potential of extract. Oral CGLE treatment significantly improved body weight (P<0.05), polyphagia and polydipsia (P<0.05) and FBG (P<0.001). Moreover, CGLE extract reversed histopathological alterations in the pancreas, liver, and kidney of diabetic mice. These outcomes highlighted that C. grandiflora extract could be effective therapeutic approach against DM.


Assuntos
Diabetes Mellitus Experimental , Hipoglicemiantes , Camundongos , Animais , Hipoglicemiantes/uso terapêutico , Estreptozocina , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Glicemia/metabolismo , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Extratos Vegetais/química , Etanol/uso terapêutico
3.
Pak J Pharm Sci ; 30(1): 229-234, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28603137

RESUMO

The present report is a significant effort to explore detail description of N. Sativa, its pharmacognostic characteristics, morphological characteristics, and mechanism of actions, doses and medicinal uses. Nigella sativa (N. Sativa) is greatest form of healing medicine. It is also known as Prophetic Medicine as its use has been mentioned in Prophetic Hadit, as natural remedy for all the diseases except death. It is recommended on daily basis in Tibb-e-Nabwi (Prophetic Medicine). Hazrat Abu Hurairah States ''I have heard from Rasool Allah (PBUH) that there is cure for every disease in black seeds except death and black seeds are shooneeze''. Salim Bin Abdullah narrates with reference to his father Hazrat Abdullah Bin Omar that Rasool Allah (PBUH) said, 'Let all the black seed upon you, these contain cure of all diseases except death'. N. sativa claimed to have anti-inflammatory, analgesic, hepato-protective, neuro-protective, gastro-protective and other useful properties. Biological and pharmacological effects are attributed to its two important constituents Thymoquinone (TQ) and Nigella sativa oil (NSO). TQ has interaction with human serum albumin. Seeds containing volatile oils mainly Melanthin showed toxicity at larger doses. This report is a reference for all pharmaceutical researchers, physicians and biologists researching on N. sativa and will open a door towards novel agent.


Assuntos
Medicina Tradicional , Nigella sativa/química , Extratos Vegetais/uso terapêutico , Óleos de Plantas/uso terapêutico , Animais , Benzoquinonas/efeitos adversos , Benzoquinonas/isolamento & purificação , Benzoquinonas/uso terapêutico , Relação Dose-Resposta a Droga , História Antiga , Humanos , Medicina Tradicional/história , Fitoterapia , Extratos Vegetais/efeitos adversos , Extratos Vegetais/isolamento & purificação , Óleos de Plantas/efeitos adversos , Óleos de Plantas/isolamento & purificação , Plantas Medicinais , Sementes/química
4.
Pak J Pharm Sci ; 28(6): 2019-25, 2015 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-26639495

RESUMO

The purpose of this study was to introduce the technology for the development of rate-controlled oral drug delivery system to overcome various physiological problems. Several approaches are being used for the purpose of increasing the gastric retentive time, including floating drug delivery system. Gastric floating lisinopril maleate and metoprolol tartrate bilayer tablets were formulated by direct compression method using the sodium starch glycolate, crosscarmellose sodium for IR layer. Eudragit L100, pectin, acacia as sustained release polymers in different ratios for SR metoprolol tartrate layer and sodium bicarbonate, citric acid as gas generating agents for the floating extended release layer. The floating bilayer tablets of lisinopril maleate and metoprolol tartrate were designed to overcome the various problems associated with conventional oral dosage form. Floating tablets were evaluated for floating lag time, drug contents and in-vitro dissolution profile and different kinetic release models were applied. It was clear that the different ratios of polymers affected the drug release and floating time. L2 and M4 showed good drug release profile and floating behavior. The linear regression and model fitting showed that all formulation followed Higuchi model of drug release model except M4 that followed zero order kinetic. From the study it is evident that a promising controlled release by floating bilyer tablets of lisinopril maleate and metoprolol tartrate can be developed successfully.


Assuntos
Antagonistas de Receptores Adrenérgicos beta 1/química , Inibidores da Enzima Conversora de Angiotensina/química , Lisinopril/química , Metoprolol/química , Administração Oral , Antagonistas de Receptores Adrenérgicos beta 1/administração & dosagem , Inibidores da Enzima Conversora de Angiotensina/administração & dosagem , Química Farmacêutica , Preparações de Ação Retardada , Estabilidade de Medicamentos , Excipientes/química , Cinética , Lisinopril/administração & dosagem , Metoprolol/administração & dosagem , Modelos Químicos , Solubilidade , Comprimidos , Tecnologia Farmacêutica/métodos
5.
PLoS One ; 19(6): e0304361, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38870190

RESUMO

OBJECTIVES: The irrational dispensing practices are responsible for antibiotic abuse and the spread of antibiotic resistance. Thus, the present study aims to evaluate the knowledge, attitudes, and practices of community pharmacists (CPs) regarding dispensing antibiotics without prescription (DAwP). METHOD: A descriptive, cross-sectional study was conducted between March 1, 2023, and March 31, 2023, in community pharmacy settings of Lahore, Pakistan. A self-administered and pretested questionnaire was used for the data collection. Logistic regression analysis was used to determine the factors associated with the practices of community pharmacists. Data were analyzed using SPSS (version 26) and MS Office (2016). RESULTS: Among 359 respondents, many strongly agreed/agreed with the statements "DAwP is contributing to the development of antimicrobial resistance" (83%, n = 298) and "Antibiotic resistance has become a public health issue" (81.9%, n = 249). Overall, most of the community pharmacists claimed that the unwillingness of patients to visit physicians for non-serious infections (75.2%, n = 270) and good knowledge of pharmacists about the use of antibiotics (51%, n = 183) were the most common reasons attributable to dispensing of antibiotics without prescription. Cephalosporin (n = 260, 72.4%), penicillin (n = 254, 70.8%), and tetracyclines (n = 170, 47.4%) were the most commonly dispensed classes of antibiotics without prescription due to cold, flu and diarrhea. Most community pharmacists never/sometimes warn patients about the potential side effects of medicines (79.1%, n = 284). Logistic regression analysis revealed that community pharmacists 31-40 years of age (OR = 0.568, 95%CI = 0.348-0.927, p-value = 0.024) were significantly less associated with poor practices of dispensing antibiotics without prescription (DAwP) while those who were 'Managers' (OR = 4.222, 95%CI = 2.542-7.011, p-value = <0.001), had 3-5 years of experience (OR = 2.241, 95%CI = 1.183-4.243, p-value = 0.013), dispensed ≤25 antibiotics per day (OR = 12.375, 95%CI = 5.177-29.583, p-value = <0.001), were more likely to be associated with poor practices of dispensing of antibiotics without prescription. CONCLUSION: The community pharmacists had adequate knowledge, positive attitudes, and poor practices towards DAwP. Demographical factors such as age, job status, and work experience were the determinants of community pharmacists' practices towards dispensing antibiotics without prescription (DAwP). Hence, a multifaceted approach, including educational interventions, is needed to reduce the dispensing of antibiotics without prescription (DAwP).


Assuntos
Antibacterianos , Conhecimentos, Atitudes e Prática em Saúde , Farmacêuticos , Humanos , Antibacterianos/uso terapêutico , Antibacterianos/administração & dosagem , Estudos Transversais , Feminino , Masculino , Adulto , Paquistão , Inquéritos e Questionários , Pessoa de Meia-Idade , Serviços Comunitários de Farmácia/estatística & dados numéricos , Adulto Jovem , Padrões de Prática dos Farmacêuticos , Atitude do Pessoal de Saúde
6.
Pak J Pharm Sci ; 26(4): 665-72, 2013 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23811440

RESUMO

Many locally occurring species of Asteraceae are used as medicinal plants by various tribal and ethnic communities in Pakistan. Carthamus oxycantha is often occurs as weed in cultivated fields. Folk medicines indicated its use as an anti inflammatory and wound healing plant. It is used for wound healing by the local population in the form of powder paste. No scientific Report, about the behavior of this plant has so far been published. The counter irritant studies of locally occurring Carthamus oxycantha was carried out. The main objectives of the project were to evaluate its wound healing effects on animal skin and the identity and characterization of chromatographically isolated fractions. For this purpose, different solvents with a broad range of polarity were successively used to extract non-polar compounds (petroleum ether extract), constituents intermediate polarities (chloroform extract) and polar constituents (methanol extract) from the whole herb of Carthamus oxycantha. The counter irritant activity of the crude extracts and isolated fractions was evaluated on rabbit's skin. Five fractions Co-1 to Co-5 were isolated from the active chloroform extract by column and thin layer chromatography. Co-1, Co-3 and Co-5 appeared to be the most potent counter irritant than others. A possible structure-activity relationship of these active compounds was investigated by using spectroscopy (UV and FTIR analysis).


Assuntos
Carthamus , Irritantes/antagonistas & inibidores , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Carthamus/química , Feminino , Masculino , Coelhos , Relação Estrutura-Atividade
7.
Life Sci ; 289: 120232, 2022 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-34919901

RESUMO

BACKGROUND: Type 2 diabetes mellitus (T2DM) is a worldwide health issue primarily due to failure of pancreatic ß-cells to release sufficient insulin. PURPOSE: The present work aimed to assess the antidiabetic potential of arjunolic acid (AA) isolated from Terminalia arjuna in type 2 diabetic rats. STUDY DESIGN: After extraction, isolation and purification, AA was orally administered to type 2 diabetic Sprague Dawley rats to investigate antidiabetic effect of AA. METHOD: T2DM was induced via single intraperitoneal injection of streptozotocin-nicotinamide (STZ-NIC) in adult male rats. After 10 days, fasting and random blood glucose (FBG and RBG), body weight (BW), food and water intake, serum C-peptide, insulin and glycated hemoglobin (HbA1c) was measured to confirm T2DM development. Dose dependent effects of orally administered AA (25 and 50 mg/kg/day) for 4 weeks was investigated by measuring BW variation, fasting and postprandial hyperglycemia, oral glucose tolerance test (OGTT), and levels of serum HbA1c, serum total cholesterol (TC), triglyceride (TG), low density lipoprotein (LDL), high density lipoprotein (HDL), serum and pancreatic C-peptide, insulin, growth differentiation factor 15 (GDF-15), serum and pancreatic inflammatory cytokines. RESULTS: The oral administration of AA in preclinical model of T2DM significantly normalized FBG and RBG, restored BW, controlled polyphagia, polydipsia and glucose tolerance. In addition, AA notably reduced serum HbA1c, TC, TG, LDL with non-significant increase in HDL. On the other hand, significant increase in serum and pancreatic C-peptide and insulin was observed with AA treatment, while serum and pancreatic GDF-15 were non-significantly altered in AA treated diabetic rats. Moreover, AA showed dose dependent reduction in serum and pancreatic proinflammatory cytokines including TNF-α, IL-1ß and IL-6. CONCLUSION: For the first time our findings highlighted AA as a potential candidate in type 2 diabetic conditions.


Assuntos
Glicemia/metabolismo , Citocinas/sangue , Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Regulação para Baixo/efeitos dos fármacos , Triterpenos/farmacologia , Animais , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/tratamento farmacológico , Inflamação/sangue , Inflamação/tratamento farmacológico , Masculino , Ratos , Ratos Sprague-Dawley , Terminalia/química , Triterpenos/química
8.
J Coll Physicians Surg Pak ; 30(11): 1193-1196, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33222739

RESUMO

OBJECTIVE: To determine the perinatal outcome of pregnancies complicated by Rh-alloimmunisation, requiring intrauterine blood transfusion. STUDY DESIGN: Observational study. PLACE AND DURATION OF STUDY: Feto-maternal Unit of Gene Tech Laboratory, Lahore, from 2007 to 2019. METHODOLOGY: A retrospective analysis was done on the data of cases of intrauterine, intravascular blood transfusion given to at-risk foetuses to correct foetal anaemia due to Rh-alloimmunisation or parvovirus B19. All cases, who were eligible to receive IUBT were included in the study. Cases where historic data was not available have been excluded. RESULTS: A total of 305 intrauterine blood transfusion (IUBT) procedures were performed on 127 foetuses. The gestational age ranged from 18-32 weeks at the time of referral. Infra-hepatic part of umbilical vein was preferred for transfusion, but in some cases of anterior placenta, the cord insertion was approached with exception of only two cases where intra-cardiac route was employed. In this study, 71.6% of the babies survived, 14.2% were loss to follow and 14.2% died. CONCLUSION: IUBT is a safe procedure, especially when performed by experienced hands, and helps save the foetuses at risk. Mothers with Rh-alloimmunisation should be referred before developing hydrops fetalis for better outcome. Key Words: Red cell alloimmunisation, Intrauterine intravascular blood transfusion, Foetal anaemia.


Assuntos
Transfusão de Sangue Intrauterina , Doenças Fetais , Feminino , Sangue Fetal , Humanos , Hidropisia Fetal/terapia , Lactente , Paquistão , Gravidez , Estudos Retrospectivos
9.
Biology (Basel) ; 9(8)2020 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-32751610

RESUMO

Withania coagulans (W. coagulans) is well-known in herbal medicinal systems for its high biological potential. Different parts of the plant are used against insomnia, liver complications, asthma, and biliousness, as well as it is reported to be sedative, emetic, diuretic, antidiabetic antimicrobial, anti-inflammatory, antitumor, hepatoprotective, antihyperglycemic, cardiovascular, immuno-suppressive and central nervous system depressant. Withanolides present in W. coagulans have attracted an immense interest in the scientific field due to their diverse therapeutic applications. The current study deals with chemical and biological evaluation of chloroform, and n-butanol fractions of W. coagulans. The activity-guided fractionation of both extracts via multiple chromatographic steps and structure elucidation of pure isolates using spectroscopies (NMR, mass spectrometry, FTIR and UV-Vis) led to the identification of a new withanolide glycoside, withacogulanoside-B (1) from n-butanol extract and five known withanolides from chloroform extract [withanolid J (2), coagulin E (3), withaperuvin C (4), 27-hydroxywithanolide I (5), and ajugin E (6)]. Among the tested compounds, compound 5 was the most potent α-glucosidase inhibitor with IC50 = 66.7 ± 3.6 µM, followed by compound 4 (IC50: 407 ± 4.5 µM) and compound 2 (IC50: 683 ± 0.94 µM), while no antiglycation activity was observed with the six isolated compounds. Molecular docking was used to predict the binding potential and binding site interactions of these compounds as α-glucosidase inhibitors. Consequently, this study provides basis to discover specific antidiabetic compounds from W. coagulans.

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