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Recent studies have shown that, coupled with other environmental factors, aluminium exposure may lead to neurodegeneration resulting in cognitive impairment resembling Alzheimer's disease. Menaquinone, a form of vitamin K2, aids in maintaining healthy bones and avoids coronary calcification. It also has anti-inflammatory and antioxidant properties. Here, we study the neuroprotective effects of vitamin K2 (MK-7) using the animal model of Alzheimer's disease (AD). Aluminium chloride (AlCl3; 100 mg/kg for 3 weeks orally) was administered to Swiss albino mice to induce neurodegeneration and Vitamin K2 (100 g/kg for 3 weeks orally) was applied as treatment. This was followed by behavioural studies to determine memory changes. The behavioural observations correlated with proinflammatory, oxidative, and brain histopathological changes in AlCl3-treated animals with or without vitamin K2 treatment. AlCl3 administration led to memory decline which was partially restored in Vitamin K2 treated animals. Myeloperoxidase levels in the brain increased due to AlCl3-mediated inflammation, which Vitamin K2 prevented. The acetylcholine esterase and oxidative stress markers induced by AlCl3 were reversed by Vitamin K2. Also, Vitamin K2 helps to restore hippocampal BDNF levels and reduced the amyloid β accumulation in AlCl3-administered animals. Additionally, Vitamin K2 protected the hippocampal neurons against AlCl3-mediated damage as observed in histopathological studies. We conclude that Vitamin K2 could partially reverse AlCl3-mediated cognitive decline. It increases acetylcholine and BDNF levels while reducing oxidative stress, neuroinflammation, and β-amyloid deposition, thus protecting the hippocampal neurons from AlCl3-mediated damage. [ABSTRACT FROM AUTHOR]

• Antibiotic mediated gut dysbiosis led to memory decline in mice. • Vitamin K2 co-administration partially reversed the gut dysbiosis associated cognitive decline. • Vitamin K2 reduced the oxidative stress and protected the antibiotic induced neuronal damage. Vitamin K2/ Menaquinones produced predominantly by the gut microbiome improve bone health and prevent coronary calcification. The central nervous system has been linked with gut microbiota via the gut-brain axis and is strongly associated with psychiatric conditions. In the present study, we show the role of Vitamin K2 (MK-7) in gut dysbiosis-associated cognitive decline. Gut dysbiosis was induced in mice by administering Ampicillin (250 mg/kg twice a day orally) for 14 days and Vitamin K2 (0.05 mg/kg) for 21 days with or without antibiotic treatment and altered gene expression profile of intestinal microbes determined. This was followed by behavioural studies to determine cognitive changes. The behavioural observations are then correlated with proinflammatory, oxidative, and brain and intestinal histopathological changes in antibiotic-treated animals with or without vitamin K2 administration. With the use of antibiotics, Lactobacillus, Bifidobacterium, Firmicutes, and Clostridium's relative abundance reduced. When vitamin K2 was added to the medication, their levels were restored. Cognitive impairment was observed in behavioural trials in the antibiotic group, but this drop was restored in mice given both an antibiotic and vitamin K. Myeloperoxidase levels in the colon and brain increased due to gut dysbiosis, which vitamin K2 prevented. The acetylcholine esterase and oxidative stress markers brought on by antibiotics were also decreased by vitamin K2. Additionally, vitamin K2 guarded against alterations in intestine ultrastructure brought on by antibiotic use and preserved hippocampus neurons. So, it can be concluded that vitamin K2 improved cognitive skills, avoided hippocampus neuronal damage from antibiotics, and lowered intestine and brain inflammation and oxidative stress. [Display omitted] [ABSTRACT FROM AUTHOR]

Context: Pterospermum acerifolium (L.) Willd (Sterculiaceae) has been traditionally used in the treatment of diabetes mellitus but no scientific data has been published supporting the claimed ethnomedical use. Objective: The present study was designed to estimate the in silico, in vitro α-amylase inhibition potential and anti-diabetic activity of Pterospermum acerifolium bark. Materials and methods: In silico studies were performed between human pancreatic α-amylase (HPA) and β-sitosterol by using autodock 4.2 software. In vitro α-amylase inhibition study was carried out with 50% ethanol extract of the bark (PABEE) and its various fractions. The active ethyl acetate fraction (PABEF) was sub-fractionated into three fractions (PABE1, PABE2 and PABE3). Two doses (15 and 30 mg/kg) based on acute toxicity studies, of the above fractions were subjected to antidiabetic screening in vivo by STZ-nicotinamide induced type II diabetic rats. Results: In silico studies showed the potent inhibition of β-sitosterol on human pancreatic amylase (HPA) with an estimated inhibition constant ( Ki) of 269.35 nmol and two hydrogen bond interactions. PABEF showed marked α-amylase inhibition (69.94%) compared to other fractions. Diabetic rats treated with PABE3 (30 mg/kg) reduced the levels of fasting blood glucose, HbA1c, ALT, AST, ALP, triglycerides, total cholesterol, TBARS significantly ( p < 0.01) and increased the levels of HDL-C, catalase, GSH, SOD significantly ( p < 0.01) as compared to that of diabetic control animals. Histological studies on PABE3 treated group showed remarkable positive changes in β-cells. Conclusion: The present study confirmed the antihyperglycemic activity along with its status on hepatic biomarkers, antihyperlipidemic and antioxidant properties of Pterospermum acerifolium bark. [ABSTRACT FROM AUTHOR]

The present study was designed to estimate the detailed antidiabetic activity of Pterospermum acerifolium (L.) Willd flowers. In vitro alpha amylase inhibition study was carried out on 50% ethanol extract of flowers (PAFEE) and its various fractions. The active ethyl acetate fraction (PAFEF) was subfractionated into three subfractions (PAFE1, PAFE2, and PAFE3) and subjected to acute toxicity studies followed by antidiabetic screening in vivo by streptozotocin-nicotinamide induced type II diabetes. Diabetic animals treated with PAFE2 (30mg/kg) reduced the levels of fasting blood glucose, significantly (P < 0.001) compared to that of diabetic control animals. Histological studies on drug treated groups did not show remarkable positive changes in β-cells. PAFE2 showed 32.6 ± 1.93% glucose uptake over control and, in the presence of PI3K inhibitor wortmannin, declined to 13.7 ± 2.51%. HPLC analysis of PAFE2 reveals the presence of quercetin and apigenin as major constituents and both are inhibiting the glycogen phosphorylase enzyme inmolecularmodelling studies. The study evidenced strongly that the probable glucose lowering mechanism of action of active subfraction PAFE2 is by increasing the glucose uptake in peripheral tissues and by inhibition of gluconeogenesis. [ABSTRACT FROM AUTHOR]

Objective: The present study was designed to evaluate the in vitro antioxidant and DNA nicking potential of various extracts and fractions of Pterospermum acerifolium (L.) Willd (Family: Stericuliaceae). Research design and methods: Antioxidant properties of the extracts and fractions was assayed by DPPH scavenging activity, non-site-specific and site-specific OH radical scavenging activity mediated 2-deoxy- D-ribose degradation, total antioxidant activity and lipid peroxidation assay by using rat liver homogenate. DNA nicking assay was studied by PT257R/T plasmid. Estimation of total phenolic content and total flavonoid content was done. Further HPTLC fingerprint of active fractions was performed. Results: Ethyl acetate fractions of leaves, flowers and bark exhibited potent antioxidant property and DNA protective effect compare to all the other extracts and fractions. Total phenolic and flavonoid content determination was also showed ethyl acetate fractions were rich in phenolic and flavonoid contents. HPTLC fingerprint revealed the total number of peaks present in the active ethyl acetate fractions of leaves, flowers and bark. Conclusion: The present study indicated that, ethyl acetate fractions of leaves, flowers and bark showed effective antioxidant and DNA protection activity and it could be the initiation for various other pharmacological studies on those fractions. [ABSTRACT FROM AUTHOR]

Abstract: Background: This study was designed to assess the effect of one traditionally used antifertility plant, Dendrophthoe falcata (L.f.) Ettingsh (Loranthaceae), on female reproductive system, fertility and safety, by oral administration to adult female Wistar rats. Study Design: After the oral acute toxicity study, the hydroalcoholic extract of the aerial parts was administered at three doses. Treatment started at weaning and continued until Day 0 postpartum. Results: The LD50 value was found to be 4.55 g/kg body weight. Vaginal opening occurred earlier in treated females when compared with controls. Analysis of vaginal smears revealed that all animals were cycling, although the length of the diestrus was longer in treated groups. In postcoital testing, the extract was found to be more effective in causing significant anti-implantation activity and reduction in the number of litters born. The extract also exhibited weak estrogenic activity when given alone, and when given along with ethinyl estradiol, it exhibited slight antiestrogenic activity in immature ovariectomized rats. Conclusion: All observations suggest that the extract has antifertility effect and is safe at effective doses employed in the study. [Copyright &y& Elsevier]

Objectives: The objective of present study was to evaluate the effect of active principle (Cg-1) from Cassia glauca leaf on serum glucose and lipid profile in normal and diabetic rats. Materials and Methods: Diabetes was induced by streptozotocin in neonates. Oral administration of petroleum ether, chloroform, acetone, and methanol of C. glauca leaf (100 mg/kg, p.o.) for 21 days caused a decrease in fasting blood glucose (FBG) in diabetic rats. Among all the extracts, acetone extract was found to lower the FBG level significantly in diabetic rats. Glibenclamide was used as standard antidiabetic drug (5 mg/kg, p.o). Acetone extract was subjected to column chromatography that led to isolation of an active principle, which was given trivial name Cg-1. Cg-1 (50 mg/kg, p.o.) was studied for its hypoglycemic and hypolipidemic potential. The unpaired t-test and analysis of variance (ANOVA) followed by post hoc test was used for statistical analysis. Results: Cg-1 caused a significant reduction in FBG level. It also caused reduction in cholesterol, triglycerides, and LDL levels and improvement in the atherogenic index and HDL level in diabetic rats. Conclusion: Improvement in the FBG and the atherogenic index by Cg-1 indicates that Cg-1 has cardioprotective potential along with antidiabetic activity and provides a scientific rationale for the use as an antidiabetic agent. [ABSTRACT FROM AUTHOR]

Many herbal remedies individually or in combination have been recommended in various medical treatises for the cure of different diseases. In the search of natural hypoglycemic agents as alternatives to synthetic ones and to justify the use of Syzygium cumini seeds in folklore system of medicine for diabetes, the hypoglycemic and hypolipidemic activity of Syzygium cumini seeds were investigated in normal and non insulin dependent diabetes mellitus (NIDDM) rats. Diabetes was induced by streptozotocin in neonates. Administration of petroleum ether, chloroform, acetone, methanol and water extracts of Syzygium cumini seeds (100 mg/kg, p.o.) for 21 days caused a decrease in fasting blood sugar in diabetic rats (FBS). Among all the extracts methanol extract was found to lower the FBS significantly in diabetic rats. Glibenclamide at a dose of 5 mg/kg p.o was used for comparision. Methanol extract was subjected to column chromatography which led to the isolation of an active principle, which was given trivial name Cuminoside. Cuminoside (50 mg/kg, p.o.) caused significant reduction in fasting blood sugar in diabetic rats. Further it also caused a significant reduction in cholesterol, triglycerides, low density lipoprotein (LDL), hepatic enzymes such as aspartate aminotransferase (AST), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) level and improvement in the level of high density lipoproteins (HDL) in diabetic rats. Reduction in the fasting blood sugar, normalization of liver enzymes level and improvement in the lipid profile by Cuminoside indicates that Cuminoside has cardio protective potential with antidiabetic activity and provides a scientific rationale for the use of Cuminoside as an antidiabetic agent. [ABSTRACT FROM AUTHOR]

Objective: The objective of the present study was to investigate the hypoglycemic and hepatoprotective effect of Cassia glauca leaf extracts on normal and non insulin dependent diabetes mellitus (NIDDM) in rats. The study was further carried out to investigate the effect of different fractions of the active extract of Cassia glauca, on normal and NIDDM rats, and the effect of active fraction on the blood glucose and hepatic enzymes level. Methods: Diabetes was induced by streptozotocin (STZ) at a dose of 90mg/kg, i.p. in neonates. Different extracts of cassia glauca (100mg/kg, p.o.) were administered to the diabetic rats. Acetone extract was found to lower the serum glucose level significantly in diabetic rats. Further, the acetone extract was subjected to column chromatography and four fractions were obtained on the basis of TLC. All the four fractions (100mg/kg, p.o.) were administered to the diabetic rats. Fraction 1 (F1) caused the maximum reduction in the blood glucose level. The results of the test were compared with the standard antidiabetic drug glibenclamide (5mg/kg, p.o.). Results: Fraction 1 of acetone extract caused a significant reduction in the levels of hepatic enzyme Aspartate transaminase (AST), alanine transaminase (ALT), creatine kinase (CK), and lactate dehydrogenase (LDH) in STZ-induced diabetic rats. Conclusion: Improvement in the blood sugar level and normalization of liver functions by Cassia glauca indicates that the plant has hepatoprotective potential, along with antidiabetic activity, and it provides a scientific rationale for the use of Cassia glauca as an antidiabetic agent. [ABSTRACT FROM AUTHOR]

Deltamethrin (DLM) is an α-cyano type-II synthetic pyrethroid compound which is extensively used in different agricultural and home pest control. The advantages of pyrethroids over other insecticides are that they are relatively non-toxic to birds and mammals and show high efficacy at relatively lower concentrations. DLM may have dual characteristics i.e. at low molar-concentration, it is nontoxic to normal healthy cells but can induce apoptotic cell death in cancerous cells. There is no reported work based on such hypothesis. Thus, this study has been designed to explore the anticancer property of DLM and the mechanism behind the apoptotic cell death by DLM in cancer cell line (Jurkat J6). Molecular docking study indicates that DLM has the greater binding affinity towards MCL-1 receptor. MTT assay has revealed some significant loss in the viability of cancerous cells by DLM. Further estimation of ROS and GSH have shown the significant oxidative stress induced by DLM in concentration-time dependent manner. DLM has also increased the caspase-3 activity and the apoptotic cells significantly while a decrease in interleukin-2 level has also been observed. The pre-treatment with thiol antioxidant and caspase inhibitor has confirmed the role of oxidative stress and the possibility of other pathways. These observations reveal that DLM may act as anticancer agent at lower concentrations (0.1–1 μM), though the further detailed investigation is warranted. [ABSTRACT FROM AUTHOR]

In this study, the chick embryo model has been used as an alternative to the mammalian model for assessing nephrotoxicity. Resemblance of the chick embryo to mammals in having metanephric kidney has prompted us to explore the possibility of using this system for the assessment of kidney toxicity caused mainly by nephrotoxic drugs, namely gentamicin, cisplatin and doxorubicin. Fertilized hens’ eggs incubated at 38 2C and 58%–60% relative humidity, were injected with the above-mentioned drugs on embryonic day 11. A significant decrease in the uric acid level of amniotic fluid was shown by embryos of cisplatin and doxorubicin-treated groups when compared to control. Embryos of the gentamicin-treated group showed significant increase in urea concentration. Alterations in uric acid, urea and creatinine levels were found in all groups. Histopathological study showed nephron degeneration. Similar results were found in a mouse model. [ABSTRACT FROM AUTHOR]

The present study evaluates possible drug interactions between glimepiride (GLIM) and sildenafil citrate (SIL) in streptozotocin (STZ)-induced diabetic nephropathic (DN) animals and also postulates the possible mechanism of interaction based on molecular modeling studies. Diabetic nephropathy was induced by single dose of STZ (60 mg kg−1, i.p.) and was confirmed by assessing blood and urine biochemical parameters 28 days after induction. Selected DN animals were used to explore the drug interaction between GLIM (0.5 mg kg−1, p.o.) and SIL (2.5 mg kg−1, p.o.) on the 29th and 70th day of the protocol. Possible drug interaction was assessed by evaluating the plasma drug concentration using HPLC-UV and changes in biochemical parameters in blood and urine were also determined. The mechanism of the interaction was postulated from the results of a molecular modeling study using the Maestro module of Schrodinger software. DN was confirmed as there was significant alteration in blood and urine biochemical parameters in STZ-treated groups. The concentration of SIL increased significantly (P < 0.001) in rat plasma when co-administered with GLIM on the 70th day of the protocol. Molecular modeling revealed important interactions with rat serum albumin and CYP2C9. GLIM has a strong hydrophobic interaction with binding site residues of rat serum albumin compared to SIL, whereas for CYP2C9, GLIM forms a stronger hydrogen bond than SIL with polar contacts and hydrophobic interactions. The present study concludes that bioavailability of SIL increases when co-administered chronically with GLIM in the management of DN animals, and the mechanism is supported by molecular modeling studies. [ABSTRACT FROM AUTHOR]

Salvia splendens (Labiatae) is widely used in Indian traditional medicine for the control of diabetes mellitus. In this study, the hypoglycemic effects produced by the acute and subacute administration of various extracts of S. splendens were investigated. Both the aqueous extract (SSAE) and the methanolic extract (SSME) from the aerial parts resulted in significant reductions of glycemia in streptozotocin (STZ)-induced diabetic rats after oral administration at a dose of 100 and 200 mg/ kg, respectively. On oral administration, aqueous and methanolic extracts showed statistically significant (P < 0.001) effect by reducing the effect of glycemia in STZ-induced diabetic rats. These findings suggest the significant antihyperglycemic potential of the S. splendens extracts in ameliorating the diabetic conditions in diabetic rats. No significant effects were found in the normal rats. [ABSTRACT FROM AUTHOR]

[Display omitted] • Expanded porous starch matrix (EPSM) bears akin physicochemical properties of porous starch (PS). • EPSM has higher pore size, surface area, and adsorption capacity than PS. • EPSM bears moisture labile structure, and un-controlled formation of pores. • EPSM can replace PS application after addressing its technical challenges. Exposing the hydrated-soft-starch matrix of intact grain or reconstituted flour dough to a high-temperature-short-time (HTST) leads to rapid vapor generation that facilitates high-pressure build-up in its elastic matrix linked to large deformation and expansion. The expanded starch matrix at high temperatures dries up quickly by flash vaporization of water, which causes loss of its structural flexibility and imparts a porous and rigid structure of the expanded porous starch matrix (EPSM). EPSM, with abundant pores in its construction, offers adsorptive effectiveness, solubility, swelling ability, mechanical strength, and thermal stability. It can be a sustainable and easy-to-construct alternative to porous starch (PS) in food and pharmaceutical applications. This review is a comparative study of PS and EPSM on their preparation methods, structure, and physicochemical properties, finding compatibility and addressing challenges in recommending EPSM as an alternative to PS in adsorbing, dispersing, stabilizing, and delivering active ingredients in a controlled and efficient way. [ABSTRACT FROM AUTHOR]

A simple and sensitive method was developed for estimation of Glimepiride (GLIM) in rat Plasma by reverse phase high performance liquid chromatography (RP-HPLC). The drug samples were extracted by liquid-liquid extraction with 300 ?L of acetonitrile and 5 mL of diethyl ether. Chromatographic separation was achieved on C18 column using methanol: water (85:15 v/v) as mobile phase at a flow rate of 1ml/min and UV detection at 230 nm. The retention time of GLIM was found to be 2.5 min. The developed method was validated for accuracy, precision, linearity and recovery. Linearity studies were found to be acceptable over the range of 100 - 6000 ng/mL. The method was successfully applied for the analysis of rat plasma sample for application in pharmacokinetic study, bioavailability. [ABSTRACT FROM AUTHOR]

Background. Ixora coccinea L. (Rubiaceae) has been documented for traditional use in hypertension, menstrual irregularities, sprain, chronic ulcer, and skin diseases. In the present study, I. coccinea was subjected to in vitro and in vivo wound healing investigation. Methods. Petroleum ether, chloroform, methanol, and water sequential I. coccinea leaves extracts were evaluated for in vitro antioxidant, antimicrobial, and fibroblast proliferation activities. The promising I. coccinea methanol extract (IxME) was screened for in vivo wound healing activity in Wistar rat using circular excision model. Wound contraction measurement, hydroxyproline quantification, and western blot for collagen type III (COL3A1), basic fibroblast growth factor (bFGF), and Smad-2, -3, -4, and -7 was performed with 7-daypostoperative wound granulation tissue. Gentamicin sulfate (0.01% w/w) hydrogel was used as reference standard. Results. IxME showed the potent antimicrobial, antioxidant activities, with significant fibroblast proliferation inducing activity, as compared to all other extracts. In vivo study confirmed the wound healing accelerating potential of IxME, as evidenced by faster wound contraction, higher hydroxyproline content, and improved histopathology of granulation tissue. Western blot analysis revealed that the topical application of I. coccinea methanol extract stimulates the fibroblast growth factor and Smad mediated collagen production in wound tissue. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: Eleutherine indica L. has been used for healing of wound, painful and irregular menstruation, dysentery and lesions, and topically used as antiseptic and antimicrobial agent in folk medicine. In the present study, methanolic extracts of Eleutherine indica was subjected to scientific investigation for in-vivo cutaneous wound healing in wistar rat. Materials and methods: In-vivo wound healing activity of Eleutherine indica was evaluated by using circular excision experimental models, followed by histopathological and western blot analysis. The healing potential was comparatively assessed with a reference gentamicin sulfate hydrogel (0.01% w/w). Wound contraction measurement, hydroxyproline estimation and western blot for COL3A1, bFGF, Smad-2, -3, -4, and -7 were performed. Results: The methanolic extract of Eleutherine indica showed accelerated wound healing activity as evidenced by fast wound contraction rate and higher hydroxyproline content of granulation tissue. Western blot revealed the Smad-mediated collagen production promoting property of Eleutherine indica methanolic extract. Histopathological examinations also supported the experimental findings. Conclusion: The study revealed that Eleutherine indica promotes wound healing by augmenting Smad-mediated collagen production in wound granulation tissue. [Copyright &y& Elsevier]