RESUMO
Diabetes mellitus (DM) is a metabolic disorder majorly arising from the pathophysiology of the pancreas manifested as a decline in the insulin production or the tissue's resistance to the insulin. In this research, we have rationally designed and synthesized new succinimide-thiazolidinedione hybrids for the management of DM. In a multistep reaction, we were able to synthesize five new derivatives (10a-e). All the compounds were new containing a different substitution pattern on the N-atom of the succinimide ring. Initially, all the compounds were tested against the in vitro α-glucosidase, α-amylase, PTP1B, and DPP4 targets. In all of these targets, the compound 10d was observed to be the most potential antidiabetic agent. Based on this, the antidiabetic activity of the compound 10d was further investigated in experimental animals, which overall gave us encouraging results. The molecular docking studies of the compound 10d was also performed against the target enzymes α-glucosidase, α-amylase, PTP1B, and DPP4 using MOE. Overall, we observed that we have explored a new class of compounds as potential antidiabetic agents.
Assuntos
Diabetes Mellitus , Tiazolidinedionas , Animais , Hipoglicemiantes , alfa-Glucosidases/metabolismo , Inibidores de Glicosídeo Hidrolases , Simulação de Acoplamento Molecular , Dipeptidil Peptidase 4 , Diabetes Mellitus/tratamento farmacológico , Insulina , Succinimidas , alfa-Amilases/metabolismoRESUMO
Therapeutic and/or preventive interventions using phytochemical constituents for ischemic heart disease have gained considerable attention worldwide, mainly due to their antioxidant activity. This study investigated the cardioprotective effect and possible mechanism of juglone, a major constituent of the walnut tree, using an isoproterenol (ISO)-induced myocardial infarction (MI) model in rats. Rats were pretreated for five (5) days with juglone (1, 3 mg/kg, i.p) and atenolol (1 mg/kg, i.p) in separate experiments before inducing myocardial injury by administration of ISO (80 mg/kg, s.c) at an interval of 24 h for 2 consecutive days (4th and 5th day). The cardioprotective effect of juglone was confirmed through a lead II electrocardiograph (ECG), cardiac biomarkers (cTnI, CPK, CK-MB, LDH, ALT and AST) and histopathological study. The results of our present study suggest that prior administration of juglone (1 and 3 mg/kg) proved to be effective as a cardioprotective therapeutic agent in reducing the extent of myocardial damage (induced by ISO) by fortifying the myocardial cell membrane, preventing elevated T-waves, deep Q-waves in the ECG, heart to body weight ratio, infarction and also by normalizing cardiac marker enzymes (cTnI, CPK, CK-MB, LDH, ALT and AST) and histopathological changes, such as inflammation, edema and necrosis. In conclusion, this study has identified phytochemical constituents, in particular juglone, as a potential cardioprotective agent.
RESUMO
Diabetes mellitus is a metabolic disorder and is a global challenge to the current medicinal chemists and pharmacologists. This research has been designed to isolate and evaluate antidiabetic bioactives from Fragaria indica. The crude extracts, semi-purified and pure bioactives have been used in all in vitro assays. The in vitro α-glucosidase, α-amylase and DPPH free radical activities have been performed on all plant samples. The initial activities showed that ethyl acetate (Fi.EtAc) was the potent fraction in all the assays. This fraction was initially semi-purified to obtain Fi.EtAc 1-3. Among the semi-purified fractions, Fi.EtAc 2 was dominant, exhibiting potent IC50 values in all the in vitro assays. Based on the potency and availability of materials, Fi.EtAc 2 was subjected to further purification to obtain compounds 1 (2,4-dichloro-6-hydroxy-3,5-dimethoxytoluene) and 2 (2-methyl-6-(4-methylphenyl)-2-hepten-4-one). The two isolated compounds were characterized by mass and NMR analyses. The compounds 1 and 2 showed excellent inhibitions against α-glucosidase (21.45 for 1 and 15.03 for 2 µg/mL), α-amylase (17.65 and 16.56 µg/mL) and DPPH free radicals (7.62 and 14.30 µg/mL). Our study provides baseline research for the antidiabetic bioactives exploration from Fragaria indica. The bioactive compounds can be evaluated in animals-based antidiabetic activity in future.
Assuntos
Fragaria , alfa-Glucosidases , Animais , Antioxidantes/química , Fragaria/metabolismo , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismoRESUMO
The exclusive breastfeeding (EBF) intention conceived by pregnant women is the most important predictor of breastfeeding (BF) initiation, duration, and continuation. This study explores the associated factors of EBF intention among pregnant women. This was a descriptive cross-sectional study conducted from November 2022 to January 2023 with 382 pregnant women who came to the outpatient clinic in the Maternal and Children Hospital (MCH). Four instruments were used for data collection: the Infant Feeding Intention scale, the Gender-Friendly BF Knowledge scale (GFBKS), the Iowa Infant Feeding Attitude scale (IIFAS), and the basic data questionnaire. The study findings indicated that 51.8% and 75.9% of gravida women had adequate knowledge and a positive attitude regarding BF. Furthermore, 56.3% of the participants had a high intention for EBF. Binary logistic regression illustrated that occupational status, antenatal care, plan for the current pregnancy, BF practice, last child delivery mode, medical disorder during the current pregnancy, age, BF knowledge, and attitude are potential predictors. The goodness of fit test revealed that 46.8% of the EBF intention could be anticipated through the positive pre-mentioned factors. The low EBF intention is modifiable by addressing the previously positive predictors. BF educational interventions should be tailored based on EBF intention predictors in order to be effective and lead to behavior change.
Assuntos
Aleitamento Materno , Gestantes , Lactente , Criança , Humanos , Feminino , Gravidez , Mães , Intenção , Arábia Saudita , Estudos Transversais , Conhecimentos, Atitudes e Prática em SaúdeRESUMO
OBJECTIVES: To investigate the effect of virtual reality (VR) on anxiety, stress, and hemodynamic parameters during cesarean section (CS). METHODS: This is a randomized controlled clinical trial conducted at the operating theatre / Maternal and Children Hospital, Najran, Saudi Arabia from February to October 2021. The study comprised a random sample of 351(176 study and 175 control) low-risk pregnant women undergoing elective CS with regional anesthesia. Data collection was carried out using 5 instruments. Basic and clinical data sheet, maternal hemodynamic parameters assessment sheet, brief measure of preoperative emotional stress, a novel visual facial anxiety scale, and maternal satisfaction scale. Virtual reality group exposed to 3D natural videos associated with calm Quran or music voices via phone using VR glasses immediately after anesthesia until completion of skin suture. The control group left for routine hospital care. RESULTS: The VR group showed significantly lower stress and anxiety levels immediately after skin suture and 2h postoperative (p=0.000). Maternal satisfaction 2 hours after CS showed that 58% of the VR group were completely satisfied compared to 11.3% of the control group (FET=135.359 p=0.000). Virtual reality have an impact on hemodynamic parameters at some time points while peripheral oxygen saturation did not differ significantly (p>0.05). CONCLUSION: Virtual reality significantly reduced anxiety and stress among women undergoing CS under regional anesthesia. Virtual reality may be added to the routine intraoperative techniques that help induce patient relaxation and increase satisfaction.
Assuntos
Cesárea , Realidade Virtual , Ansiedade/prevenção & controle , Ansiedade/psicologia , Transtornos de Ansiedade , Criança , Feminino , Hemodinâmica , Humanos , GravidezRESUMO
For the precise preoperative evaluation of complex congenital heart diseases (CHDs) with reduced radiation dose exposure, we assessed the diagnostic validity and reliability of low-dose prospective ECG-gated cardiac CT (CCT). Forty-two individuals with complex CHDs who underwent preoperative CCT as part of a prospective study were included. Each CCT image was examined independently by two radiologists. The primary reference for assessing the diagnostic validity of the CCT was the post-operative data. Infants and neonates were the most common age group suffering from complex CHDs. The mean volume of the CT dose index was 1.44 ± 0.47 mGy, the mean value of the dose-length product was 14.13 ± 5.4 mGy*cm, and the mean value of the effective radiation dose was 0.58 ± 0.13 mSv. The sensitivity, specificity, PPV, NPV, and accuracy of the low-dose prospective ECG-gated CCT for identifying complex CHDs were 95.6%, 98%, 97%, 97%, and 97% for reader 1 and 92.6%, 97%, 95.5%, 95.1%, and 95.2% for reader 2, respectively. The overall inter-reader agreement for interpreting the cardiac CCTs was good (κ = 0.74). According to the results of our investigation, low-dose prospective ECG-gated CCT is a useful and trustworthy method for assessing coronary arteries and making a precise preoperative diagnosis of complex CHDs.