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.
BACKGROUND: Saudi Arabia is known to have one of the highest prevalence of diabetes in the world. The impact of Ramadan fasting on the health of type 2 diabetic patients is an important issue that has not been adequately investigated.
AIM: The current study was aimed at assessing the impact of Ramadan fasting on hemoglobin A1C (HbA1c), lipid profile, blood pressure, and body mass index (BMI) in adult Saudis with Type 2 diabetes residing in Najran city.
METHODS: This is a descriptive cross-sectional study which enrolled 289 patients who chose to fast during the month of Ramadan and were attending the outpatient clinics of Najran University Hospital. Fasting blood samples were taken 1 month before and 1 month after Ramadan to determine glycated hemoglobin and fasting lipid profile (low-density lipoprotein [LDL], high-density lipoprotein [HDL], triglyceride [TG], and total cholesterol [TC]) and BMI was also calculated. Information regarding demographics and physical activity was obtained through a questionnaire.
RESULTS: As many as 176 (60.9%) of the participants reported to be physically inactive during Ramadan. There was a statistically significant (p < 0.05) decrease in the mean percentage of HbA1c when comparing before Ramadan (9.85 ± 2.37%) with after Ramadan (7.65 ± 1.70%). Furthermore, statistically significant difference (p < 0.05) was detected in the mean concentrations of LDL before (3.39 ± 1.06 mmol/L) and after (2.40 ± 0.83 mmol/L) Ramadan. The mean concentration of TC (before = 5.98 ± 2.00 mmol/L; after = 4.05 ± 1.18 mmol/L) and TG (before = 2.97 ± 1.95 mmol/L; after = 2.65 ± 1.65 mmol/L) also reduced after Ramadan. The mean concentrations of HDL (before = 1.78 ± 0.74 mmol/L; after= 2.23 ± 0.23 mmol/L) increased after Ramadan. The mean BMI of the study participants (before = 28.30 ± 6.27; after = 27.43 ± 5.92) decreased slightly after Ramadan. The systolic blood pressure (SBP) (before= 128.10 ± 6.32; after, 123.09 ± 5.71) and diastolic blood pressure (DBP) (before = 81.21 ± 8.51; after = 79.83 ± 7.21) showed a slight reduction after Ramadan.
CONCLUSIONS: Type 2 diabetic patients who performed Ramadan fasting displayed a lowering of HbA1c, LDL, TC, and TG, and increased HDL, but had small positive effects on body weight, BMI, as well as SBP and DBP. More studies are needed with a larger population in the future to assess the potential of Ramadan fasting as a therapeutic strategy for managing Type 2 diabetes.
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.
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