Antidiabetic Properties of Caffeoylmalic Acid, a Bioactive Natural Compound Isolated from Urtica dioica.

The uncontrolled hyperglycemia that characterizes diabetes mellitus (DM) causes several complications in the organism. DM is among the major causes of deaths, and the limited efficacy of current treatments push the search for novel drug candidates, also among natural compounds. We focused our attention on caffeoylmalic acid, a phenolic derivative extracted from Urtica dioica, a plant investigated for its potential against type 2 DM. This compound was tested for its antidiabetic activity in vitro through a glucose uptake assay, in vivo in a mouse DM model and through molecular docking towards α-amylase and α-glucosidase. The effects on glucose blood level, liver enzymes, insulin and creatinine levels as well as on lipid and blood parameters, considered biochemical markers of diabetes, were also evaluated. The results showed an antidiabetic activity in vitro and in vivo, as the compound stimulates glucose absorbtion and reduces blood glucose levels. Moreover, it ameliorates lipid profile, liver and blood parameters, with moderate effect on insulin secretion. Taken together, these findings pave the way for the compounds from this class of caffeoylmalic acid as potential antidiabetic compounds.

Bioactivity of 2-(3,4-Dihydroxyphenyl)-5,7-dihydroxy-2,3-dihydrochromen-4-one from pistacia chinensis on ENPP1 and aldose reductase.

Pistacia chinensis is used as a decorative tree and currently studied as a source of biofuels. Besides, its parts and extracts are endowed with several therapeutic uses which have been widely explored in traditional medicine and that are related to its rich composition in phytochemicals. Molecular docking and enzymatic inhibition tests were used to study the activity of eriodictyol, a flavonoid extracted from the barks of P. chinensis, against ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) and aldose reductase (ALR2). The compound was highlighted as a micromolar inhibitor in vitro (IC50 = 263.76 ± 1.32 µM and 4.21 ± 0.94 µM, respectively) and docking showed that eriodictyol efficiently targets the binding sites of the enzymes. In conclusion, this study unveils the potential of eriodictyol on enzymes that are involved in immunostimulation and in complications of diabetes mellitus.

In vitro and in silico antiproliferative potential of isolated flavonoids constitutes from Pistacia integerrima.

Cancer is one of the most demanding domains for innovative, effective, safe, and affordable therapeutically active chemicals. The main aim of this study is to research new phytochemicals with anticancer activity. The current experiment identified and analyzed six compounds for anti-cancer potential supported by molecular simulation studies. The defatted methanolic extract underwent column chromatography, resulting in the isolation of six flavonoids. These include 3,5,7,4'-tetrahydroxy-flavanone (1), naringenin (2), 3,5,4'-trihydroxy-7-methoxy-flavanone (3), sakuranetin (4), spinacetin (5), and patuletin (6). The isolated compounds (1-6) were assessed for in vitro anti-cancer activity against various cell lines such as HepG2 (hepatoma G2), A498 (kidney), NCI-H226 (lungs), and MDR2780AD (human ovarian). The maximum antiproliferative effect was against HepG2 and MDR2780AD. When compounds 6, 5, and 1 were compared to a standard anti-cancer medicine (paclitaxel) with an IC50 of 7.32, it was shown that compounds 6, 5, and 1 exhibited significant activity against HepG2 with IC50 values of 14.65, 20.87, and 27.09 µM, respectively. All tested compounds showed an IC50 of less than 1 µM and had notable effects against MDR2780 AD cell lines. Compound 6 exhibited notable potency against the HepG2, A498, and MDR2780AD cell lines, among the six compounds that were evaluated. In contrast, compound 3 demonstrated the most pronounced impact on the NCI-H226 cell line. Docking investigations were performed using tubulin as the specific target concerning PDB ID 4O2B. The six compounds under investigation interact hydrophobically and hydrophilically with tubulin-binding site amino acid residues.

Discovery of new α-glucosides, antiglycation agent, and in silico study of 2-(3,4-dihydroxyphenyl)-7,8-dihydroxy-3-methoxy-4H-chromen-4-one isolated from Pistacia chinensis.

Pistacia chinensis is locally practiced for treating diabetes, pain, inflammation, and erectile dysfunction. Therefore, the current studies subjected the crude extract/fractions and the isolated compound (2-(3,4-dihydroxyphenyl)-7,8-dihydroxy-3-methoxy-4H-chromen-4-one) to α-glucosidase inhibitor and anti-glycation activities. The development of long-term complications associated with diabetes is primarily caused by chronic hyperglycemia. Regarding α-glucosidase, the most significant inhibitory effect was observed with compound 1 (93.09%), followed by the methanolic extract (80.87%) with IC50 values of 45.86 and 86.32 µM. The maximum anti-glycation potential was shown by an isolated compound 1 followed by methanolic extract with effect inhibition of 90.12 and 72.09, respectively. Compound 1 is expected to have the highest gastrointestinal absorption rate, with a predicted absorption rate of 86.156%. This indicates oral suitability. The compound 1 is expected to have no harmful effects on the liver. In addition, our docking results suggest that alpha-glucosidase and isolated compounds showed strong interaction with ILE821, GLN900, and ALA901 residues, along with a -11.95 docking score.

Pharmacological basis for the antihypertensive activity of Grewia asiatica fruit extract.

In the management of cardiovascular disorders, medicines from herbal sources have played a vital role through centuries. The following study was commenced in order to lay possible pharmacological foundation associated with medicinal uses of edible fruit of Grewia asiatica in hypertension through in-vitro method. In this study isolated atrial preparation of Guinea pig was used where crude ethanolic extract of Grewia asiatica fruit (Ga.Cr) decreased the force and rate of spontaneous atrial contractions (0.03-10mg/kg). In isolated rat aortic ring preparations previously vasoconstricted by phenylephrine and High K+, it also resulted in dose dependent vasodilation (0.01-10 mg/kg).In the presence of L-NAME, the relaxation curve of Ga.Cr was partially inhibited showing involvement of Nitric oxide (NO) mediated pathway. The speculative analysis contemplated that Ga.Cr has blood pressure reducing potentials through inhibition of Ca++ influx via Ca++ channels, its release from intracellular stores and through other means like NO mediated pathways.

Frequency of Low Birth Weight and its Relationship With Maternal Nutritional and Dietary Factors: A Cross-Sectional Study.

BACKGROUND:  Low birth weight (LBW) is linked with fetal and neonatal mortality and morbidity; also it can slow down growth and cognitive development. Several factors contribute to pregnancy outcomes, including LBW deliveries, maternal nutrition, and additional dietary intake. Our study was aimed to identify the frequency and factors associated with LBW mothers in Karachi, Pakistan.  Methods: A cross-sectional survey was carried out at the Obstetrics and Gynaecological Department of Hamdard Hospital, Karachi. A total of 195 healthy pregnant females were enrolled. All the relevant data were collected from March 1st, 2019 to August 31st, 2019 with the help of a structured questionnaire designed specifically for the study where mothers were also asked about consumption of iron, vitamin, and extra meals since they became pregnant. Written, informed consent was taken from all of the participants before data collection. Data analysis was performed using a statistical package for the social sciences (SPSS) version 20.0. A Chi-square test was used for checking associations between the studied maternal factors and the weight of the children.  Results: There was a total of 195 pregnant females selected for the study. The frequency of LBW infants was found to be 57 (29.2%) in these women. The mean age of the females was 29.29 ± 5.22 years, 142 (72.8%) of them had a body mass index (BMI) of 25.0 kg/m2 or more, 102 (52.3%) of them had hemoglobin (Hb) between 10 and 11 mg/dL. The study results further showed that maternal Hb (p=0.02), vitamin C intake (p=0.037), iron intake (p=0.01), and consumption of extra meals during pregnancy (p=0.021) were significantly associated with a LBW of the children. Mothers whose Hb <10 mg/dL, no intake of vitamin C, or iron, and extra meals during pregnancy were more likely to have a child with LBW than others. CONCLUSION:  It can be concluded that maternal nutritional and dietary factors are very important during fetal development, and they have a significant relationship with the birth weight.

Hepatoprotective and antidiabetic effect of Guaiacum officinale in diabetes induced male albino wistar rats.

The aim of present study is to evaluate the antidiabetic and hepatoprotective effect of Guaiacum officinale in streptozotocin induced male albino rats. The methanolic bark extract of Guaiacum officinale was administered at a dose of 500 mg/kg and Glibenclamide was used as a standard drug at a dose of 0.5mg/kg for 28 days. The animals were divided in to four groups. Control group n=12, received distilled water. Positive control group (STZ group) n=12 received streptozotocin at 30 mg/kg dose through I/P route. Standard group (STZ+ GLB group): n=12 received Glibenclamide. Treated group (STZ+ extracted group): n=12 received bark extract of Guaiacum officinale. Blood glucose level was significantly reduced after oral adminstration of bark extract in streptozotocin induced diabetic rats. The SGOT level significantly reduced in Guaiacum officinale treated group as compare to control, pronounced reduction of ALT level as compared to GLB and the ALP levels was highly significantly reduced in Guaiacum officinale treated group while GLB is unable to improve ALP levels in GLB treated diabetic albino rats. The level of direct bilirubin in Guaiacum officinale treated group was found to be insignificant as compared to control and STZ treated group while the level of indirect bilirubin was significantly reduced in STZ treated group as compare to control. Histopathological studies showed that Guaiacum officianle have hepatoprotective effect in experimental induced male albino rats.