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The khat plant has been culturally used in many parts of Africa and the Arabian Peninsula for many years to induce psycho-stimulating effect. Because of the global wide-spreading nature, khat chewing is being considered as a universally growing problem. Catha abbottii, Catha edulis, and Catha transvaalensis are the three species of khat commonly chewed in Saudi Arabia and nearby regions. Khat users usually prefer to chew young leaves over mature ones due to the diverse effects produced by both. Though many of the constituents of khat leaves have been identified, the complete phytochemical profile of young and mature leaves was not performed or compared; also, no evidence is available to affirm the cytotoxicity of young or mature leaves. Therefore, this study aimed to investigate the phytochemical basis of the differential response of the young and mature leaves and to assess the cytotoxicity of young and mature khat leaves. Ethanolic extracts of young and mature leaves of three khat cultivars were subjected to GC-MS. Hierarchical cluster analysis revealed the existence of two major clusters. The extracts of young leaves were found to contain the maximum content of cathinone; however, methoxyamphetamine was found in only one extract of young leaves. Cytotoxicity investigations were also conducted on both types of leaves using three cancer cell lines, human breast adenocarcinoma, human ovary adenocarcinoma, and human colon adenocarcinoma and also normal human fetal lung fibroblast cell line was used. All extracts showed comparable cytotoxicity, IC50 ranging from 22–59 μg/mL on the cancer cells; however, we observed more cytotoxicity against normal cells (IC50: 6–41 μg/mL). The predominant cytotoxicity on normal cells may pose many health hazards to khat consumers.

Purpose. The study evaluated the neuroprotective effect and pharmacokinetic profile of turmeric extract and their metabolites in the blood and brain in an aluminum-induced neurotoxic animal model. Methods. Swiss albino mice received turmeric extract (TE), TE-essential oil combination (TE+EO) at doses of 25 and 50 mg/kg/day orally, vehicle (control), and a positive control group. Neurotoxicity was induced by injecting aluminum chloride (40 mg/kg/day, i.p.), and the effect of the intervention was studied for 45 days. The pharmacokinetic and behavioral biochemical markers of brain function and brain histopathological changes were evaluated. Results. The AUC 0- t showed a 30.1 and 54.2 times higher free curcumin concentration in plasma with 25 mg/kg and 50 mg/kg of TE+EO vs. TE, respectively. The concentration of free curcumin in the brain was 11.01 and 13.71-fold higher for 25 mg/kg and 50 mg/kg of TE+EO vs. TE, respectively. Aluminum impairs spatial learning and memory, which was significantly reversed with TE+EO by 28.6% (25 mg/kg) and 39.4% (50 mg/kg). In the elevated plus maze test, 44.8% (25 mg/kg) and 67.1% (50 mg/kg) improvements were observed. A significant reduction in aluminum-induced lipid peroxidation was observed. Also, the levels of glutathione, acetylcholinesterase, and catalase were improved with TE+EO. Damage to the hippocampal pyramidal cells was averted with TE+EO. Conclusion. The neuroprotective and antioxidant response confirms the benefits of TE+EO against aluminum-induced neurotoxicity. The presence of free curcumin and its metabolites in the brain and plasma establishes its improved bioavailability and tissue distribution. Therefore, the benefits of TE+EO could be harnessed in neurodegenerative diseases.

This study investigated both the mutagenicity and anti-mutagenicity of alpha-lipoic acid (ALA) in the bone marrow cells of mice using a chromosomal aberration assay. Cyclophosphamide (CP) 40 mg/kg was used as a clastogen in the positive control, and a vehicle-treated negative control group was also included. Multiple dose levels (15, 30, and 100 mg/kg of ALA) were given by intraperitoneal injection (IP) alone and in combination with CP (CP was administered 1 h prior to ALA). Bone marrow samples were collected 12 and 24 h after drug administration. The results demonstrated a significant increase in the frequency of chromosomal aberrations (CA) in bone marrow cells with depressions in the mitotic index (MI) of the positive control group of mice. However, in the groups of mice treated with different doses of ALA in the presence of CP, the percentages of CA decreased significantly with increases in mitotic activity. The results also indicate that ALA given alone in different doses had no mutagenic effect on mouse bone marrow cells. ALA has a dose and time-dependent protective effect against the mutagenicity induced by CP.

Carbosulfan, a wide spectrum pesticide is used to improve crop productivity. During their application, they disperse in the environment exerting harmful consequences on human health. We speculated that exposure to carbosulfan, a carbamate insecticide during early development can affect neurogenesis and synaptic development. In order to test this, pregnant dams were exposed to carbosulfan in four doses (0.5, 1, 2, and 4 mg/kg) during the embryonic period (ED 1–15). Offspring were evaluated for neurobehavioral changes, oxidative markers, acetylcholinesterase levels, and formation of carbonylated proteins. Histopathology of the cerebellum was carried out. Carbosulfan exposure produced alteration in sensorimotor tasks, motor function and elevated anxiety in pups. Carbosulfan affected growth rate of pups in a dose dependent manner. A significant increase in malondialdehyde, a lipid peroxide marker, carbonylated proteins and a dose dependent decrease in the levels of glutathione and glutathione peroxidase were observed. Carbosulfan produced a decline in acetylcholinesterase levels which might contribute to poor exploratory behavior. Distinct changes in the Purkinje cells were observed as the dose of carbosulfan increased. Largely, alteration in behavior can be due to oxidative damage, thereby, affecting neurogenesis, synaptogenesis and myelination. Therefore the propensity of carbosulfan to induce developmental disability is high and should be cautiously avoided during embryonic development.

Objective: To evaluate the Antihypercholesterolemic effect of Boswellia ovalifoliolata Bal. Henry extract by performing invivo studies and to checkout its effects by evaluating parameters like food consumption, weight gain, fecal fat excretion, serum and liver lipid &biochemical profiles. Even the study includes confirmation of activity by the histopathological studies. Methods: Animals were fed with cholesterol rich high fat diet. Food intake, Bodyweight and fecal fat excretion were measured. Serum and liver samples were analyzed for the estimation of lipid profiles and other biochemical parameters by using different kits. Histopathological study on liver, aorta, heart and adipose tissue was done to ensure the activity. Results: The animal group administered with methanolic extract of the plant has shown decreased levels of TC, LDL, VLDL, TG, HDL+VLDL, VLDL+LDL, LDL/TC, AI, SGOT, SGPT and elevated levels of HDL, HDL/TC in a dose dependent manner significantly (p

Stress can lead to the manifestation of functional gastrointestinal disorders, the most prominent being irritable bowel disorder. The present study investigated the impact zingerone in ameliorating chronic water stress induced irritable bowel disorder, brain gut axis dysfunction and dysregulation of the intestinal barrier due to oxidative stress. Rats were randomly allocated to groups and subjected to chronic water stress for a period of 21 days for 1h and the fecal pellet output was measured. At the end of chronic stress, behavioral assessment for anxiety like behavior was recorded and plasma corticosterone levels were measured 60min after water stress. The colonic transit was determined, levels of oxidative and antioxidant biomarkers were measured in the colon homogenate. Myeloperoxidase activity was determined as an indirect index of neutrophil infiltration. Chronic water stress increased the rate of colonic transit, fecal output, induced behavioral changes, and decreased antioxidant levels. An increase in lipid peroxide levels, catalase and corticosterone was observed. Mast cell infiltration was evident in the stressed group. Zingerone significantly reduced colonic transit, fecal output, neutrophil infiltration, and lipid peroxide formation. The levels of catalase were not altered; however, a marginal increase in the levels of glutathione peroxidase was observed. Zingerone significantly enhanced the levels of superoxide dismutase, glutathione and decreased the levels of corticosterone. Zingerone produced marked improvement in stress induced irritable bowel disorder which could be attributed to the powerful antioxidant nature, direct effect on the intestinal smooth muscle and adaptogenic nature.

Capsaicin is employed as a condiment and colorant in the cosmetic and pharmaceutical industries. Metabolism of capsaicin produces reactive phenoxy radicals, which inflict damage to DNA. Micronutrients such as zinc and selenium facilitate the expression of tissue repair factors, and lycopene has natural antioxidant action. The current study investigated the possible protective role of zinc, selenium and lycopene singly and in combination in ameliorating capsaicin induced mutagenicity. Fifty four Swiss albino mice received the vehicle, zinc (10 mg/kg), selenium (2 mg/kg), lycopene (2 mg/kg) alone, capsaicin alone (2 mg/kg), and capsaicin along with zinc (10 mg/kg), selenium (2 mg/kg) and lycopene (2 mg/kg) in combination by the oral route for 32 days. Animals were killed 24 h after the last treatment, and micronuclei formation in bone marrow and peripheral blood were assessed. Antioxidant status in plasma, the total protein, nucleic acids, and DNA fragmentation was assessed in the liver homogenate. Capsaicin substantially damaged nuclear material and increased oxidative stress. Individual therapy with lycopene was most effective in reducing micronuclei formation, lipid peroxidation, and in augmenting ferric reducing ability of plasma. This was closely followed by zinc and selenium. Zinc protected against DNA fragmentation followed by lycopene and selenium. The combination therapy was effective over individual treatment against DNA fragmentation, micronuclei and malondialdehyde formation. The combination did not exert a substantial benefit over individual therapy in enhancing the total antioxidant ability of plasma. The risk of capsaicin induced mutagenicity was lowered with the combination by reducing the generation of free radicals and by enhancing tissue repair.

Cerebellar atrophy during ageing can produce neurobehavioural changes characterized by cognitive and motor impairment. Chronic exposure to D-galactose, a reducing sugar can accelerate ageing by producing an unprecedented rise in oxidative load. This can enhance neuronal damage by promoting the oxidation of protein and lipids. We perceived that the simultaneous administration of piperine and curcumin, two powerful antioxidants can exert neuroprotective effect by inhibiting damage caused by the chronic exposure to D-galactose. Young Wistar rats treated with D-galactose (150 mg/kg, s.c.) were simultaneously treated with piperine alone, curcumin separately; and in combination for a period of 56 days by the oral route. A vehicle control, D-galactose alone and naturally aged control were also evaluated. Cognitive changes, motor impairment, protein carbonyls, protein thiols, advanced oxidation protein products, 4 hydroxynonenol and nitric oxide levels were determined in the brain homogenate. In order to ascertain the impact of cerebellum on motor performance, histopathological changes in the cerebellum were also established. Results obtained from our studies reflect a marked improvement in memory, sensorimotor performance, reduced oxidative and nitrosative burden on simultaneous treatment with piperine and curcumin. Furthermore, alterations produced in the Purkinje cells were minimized on treatment with the combination. Our studies demonstrated the influence of protein and lipid oxidation products on behavioural changes in D-galactose induced ageing model. Incorporation of these antioxidants might reduce the risk of developing neurodegenerative disorders, an important counterpart of advancing age.

The present study was designed to investigate the anti - genotoxic effect of Ocimum sanctum on fluoride induced genotoxicity and its impact on oxidative stress. Exposure to fluoride can mainly occur through drinking water when the levels far exceed th e permissible limit. Fluorosis is a serious problem the world over resulting in damage to DNA. Micronuclei assessment from bone marrow and peripheral blood was used in the present study to assess the damage to DNA. Sodium fluoride in a single dose (30 mg/kg, i.p.) was used to induce micronuclei in albino mice. Treatment with the aqueous extract of Ocimum sanctum was initiated in the single dose study (100, 400 & 800 mg/kg) and as a time cours e for 1 day, 3 days and 7 days (100 mg/kg) . 24 h after injecting sodium fluori de, the animals were sacrificed and m icronuclei were determined from smears prepared from bone marrow and peripheral blood. The antioxidant impact of the e xtract was determined using ferric ion reducing capaci ty of plasma and thiobarbituric acid reactive substances as a measure of lipid peroxidation. All doses were capable of p reventing the formation of micronuclei but 100 mg/kg of the aqueous extract was most efficacious as a single dose and in the time course study. The beneficial effect of Ocimum sanctum is possibly due to the synergistic action of constituents like polyphenols, triterpenoids, and flavonoids.

Aerial parts of Ipomea pes-tigridis were extracted by soxhlet extraction and then subjected to preliminary phytochemical screening. Results exposed similar kind of phytochemicals in the methanolic extract of all the parts. This was further confirmed by thin layer chromatographic analysis. Hence the extracts were pooled and screened for anti-bacterial activity against routine bacterial strains and then the anti acne activity against Staphylococcus epidermidis and Propionibacterium acnes. It was observed that S. epidermidis was more susceptible to the extract than P. acnes as the minimum inhibitory concentration was determined to be 96 μg.mL−1 and 100 μg.mL−1 respectively. Bioautography performed revealed that alkaloids and flavonoids were the potent inhibitors of these micro organisms. The anti-inflammatory activity was screened showed that 100 mg.kg−1 as the most effective dose.

Objective To evaluate the wound healing potency of aqueous extract of Aerva monsoniae (A. monsoniae) by in vitro method using fertilized eggs, in vivo analgesic and anti inflammatory activity in rodents and the anti bacterial activity on the bacterial strains that infect the wound. Methods The whole plant of A. monsoniae was extracted with water and then subjected to preliminary chemical screening. It was then evaluated for in ova angiogenesis on fertilized white leg horn eggs using the concentrations of 200-600 μ g/mL. The analgesic activity was evaluated in mice using the dose 100 and 250 mg/kg. The anti inflammatory activity was evaluated in rats using the dose 250 mg/kg and 500 mg/kg. In both the parameters water was used as the control and diclofenac was used the standard. The anti bacterial activity on Staphylococcus aureus and Pseudomonas aerugenosa was performed. Results The phytochemical screening revealed the presence of tannins, flavonoids and saponins. The in ova angiogenesis revealed a dose dependent activity which proves the wound healing claim of the plant as more number of blood capillaries were formed at the site of the drug. The plant proved to be a potent analgesic and anti inflammatory agent at doses 100 mg/kg and 250 mg/kg. The anti bacterial activity was present but at higher doses. Conclusions The parameters studied in the present investigation proved that the plant is a potent wound healer. Further in vivo wound healing studies on animal model is desired. As the extract showed potent analgesic, anti inflammatory and anti bacterial properties, it can be considered that when formulated into suitable formulation, and it can reduce the pain, inflammation and infections related to wound very well.

Sophora is a genus of the Fabaceae family, contains about 52 species, nineteen varieties, and seven forms that are widely distributed in Asia, Oceanica, and the Pacific islands, in the family Fabaceae of herbaceous (Sophora flavescens Aiton) to trees (Sophora japonica L.). More than fifteen species in this genus have a long history of use in traditional Chinese medicines. In the last decades the use of this genus in traditional Chinese drugs has led to rapid increase in the information available on active components and reported to posses various pharmacological/therapeutic properties. The paper reviews the ethnopharmacology, the biological activities and the correlated chemical compounds of genus Sophora, Fabaceae. More than 300 compounds has been isolated, among them major are quinolizidine alkaloids particularly matrine and oxymatrine and flavonoids particularly prenylated and isoprenylated flavonoids. Modern pharmacological studies and clinical studies demonstrated that these chemical constituens possess wide reaching pharmacological actions like anti oxidant, anticancer, anti-asthamatic, anti-neoplastic, antimicrobial, antiviral, antidote, anti pyretic, cardiotonic, antinflammatory, diuretic and in the treatment of skin diseases like eczema, colitis and psoriasis.

Objective To develop transfersomal formulation integrated with piperine intended for vitiligo. Methods Film hydration technique was employed in the preparation of transfersomes. Modified diffusion cell, consistency tester were fabricated for ex vivo diffusion studies and spreadability studies respectively while tape stripping method was integrated with tissue extraction in the determination of tissue drug concentration. Results When film hydration technique was used for, ultradeformable vesicles (transfersomes) of piperine in soabean phosphatidylcholine was formed with (67.11±0.22) to (70.55±3.62) and (60.12±1.04) to (80.43±0.14) mean size (μ) and entrapment efficiency (%) respectively. Transfersomes are capable of crossing the pores in permeability barriers extremely efficient even if the transfersome radius (tr) is much greater than the pore size (rpore) ie., tr/rpore⩾ 0.25 the driven flux rate depends on the transdermal osmotic gradient. The vesicles describes elasto-mechanical character of vesicles while penetrating through the pores. The proviso is that the vesicular membrane elasticity is dynamically to the local stress by the external. Diffusion and Spreadability studies showed maximum diffusion when the lipid was kept minimum. Tape stripping and tissue extraction method for the tissue drug retention showed that (75.25±1.72)% drug was retained in the dermis. Conclusion Span 80 was preferred over tween 80 in terms of dermal retention. Size and encapsulation was slightly altered by phosphatidylcholine concentration. The kinetics, efficiency and the transfersome mediated transport can be tailored for trans-epidermal, deep tissues and systemic depending on the vesicular composition, dose and form. Thus we have offered a successful drug delivery of piperine targeting the deep epidermis.

Spices have become the source of therapy in most of the countries and are especially commonly used in India where herbs and spices are the indigenous part of the curing system. From previous studies, spices are known to have digestive stimulant actions and thus may be helpful in treating the digestive disorders.[1, 2] Piperine, the most common spice of Indian kitchen, has previously been shown to have the anti ulcer activity. [3,4,5] Piperine was found to be effective for gastric ulcers in rats and mice at a dose range of 25 to 100 mg/kg.[6] Apart from its gastro protective activity, piperine has also been investigated for other beneficial gastro intestinal effects including antileishamnial activity,[7] antidiarrheal activity,[8] improved gastric mucosal integrity,[9] muco-protective activity[10] and hepato protection,[11] along with the improved absorption[12] and bio availability[13] of several classes of drugs.

Objective: Millingtonia hortensis Linn is an abundant resource of flavonoids, which might be beneficial in protecting liver tissue from injury. The hepatoprotective and antioxidant potential of ethanolic extract of M. hortensis on carbon tetrachloride (CCl 4 ) induced hepatotoxicity and the possible mechanism involved therein were investigated in rats. Materials and Methods: Preliminary phytochemical studies were carried out to determine the total phenol and flavonoid contents. 30 adult Wistar rats were allocated into 5 groups. Control group received vehicle, group-2 received CCl 4 alone (1 ml/kg body weight, intraperitonially), groups 3 - 5 received the ethanolic flower extract in 2 dose levels (200 and 400 mg/kg) and Curcumin (100 mg/kg) as a standard for 8 days orally, followed by CCl 4 as a single dose on the 8 th day. 48 hours later, blood was withdrawn, serum was subjected to biochemical assessments, and liver homogenate was examined for lipid peroxides, glutathione, superoxide dismutase, catalase and total protein levels. Furthermore, hepatic tissues were subjected to histopatological studies. Results: CCl 4 treatment produced a profound increase in the levels of malondialdehyde, hepatic marker enzymes and bilirubin content compared with the control (P < 0.05). Pre-treatment with the flower extract of M. hortensis significantly enhanced the levels of endogenous antioxidants and reduced the levels of hepatic marker enzymes in relation to the CCl 4 treated group (P < 0.05). Balloning degeneration and fatty changes in hepatocytes was prevented by pre-treatment with the flower extract. Conclusion: The antioxidant nature of the flower extract of M. hortensis could be responsible for averting damage to the liver.

Methotrexate is employed in low doses for the treatment of rheumatoid arthritis. One of the major drawbacks with methotrexate is hepatotoxicity resulting in poor compliance of therapy. Curcumin is an extensively used spice possessing both anti-arthritic and hepatoprotective potential. The present study was aimed at investigating the effect of curcumin (30 and 100 mg/kg) in combination with subtherapeutic dose of methotrexate (1 mg/kg) is salvaging hepatotoxicity, oxidative stress and producing synergistic anti-arthritic action with methotrexate. Wistar albino rats were induced with arthritis by subplantar injection of Freund's Complete Adjuvant and pronounced arthritis was seen after 9 days of injection. Groups of animals were treated with subtherapeutic dose of methotrexate followed half an hour later with 30 and 100mg/kg of curcumin from day 9 up to days 45 by intraperitoneal route. Methotrexate treatment in Freund's Complete Adjuvant induced arthritic animals produced elevation in the levels of aminotransferases, alkaline phosphatase, total and direct bilirubin. Enhanced oxidative stress in terms of measured lipid peroxides was observed in the methotrexate treated group. Curcumin significantly circumvented hepatotoxicity induced by methotrexate as evidenced by a change in biochemical markers possibly due to its strong anti-oxidant action. Hepatoprotective potential of curcumin was also confirmed from histological evaluation. Sub-therapeutic dose of methotrexate elicited substantial anti-arthritic action when used in combination with curcumin implying that the latter potentiated its action. Concomitant administration of curcumin with methotrexate was also found to minimize liver damage.

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.O propósito deste trabalho foi preparar ziprasidona. HCl NR 40 mg e triexifenidila.HCl SR 4 mg na forma de comprimidos efervescentes bicamada de liberação controlada. Os comprimidos foram preparados utilizando HPMC K4M / HPMC K15M sódico como polímero bioadesivo e bicarbonato como camada efervescente. Os comprimidos foram avaliados quanto a diferentes parâmetros, como espessura, dureza, friabilidade, variação de peso, dissolução in vitro, conteúdo do ingrediente ativo e estudos de IV. As propriedades físico-químicas dos produtos finais cumprem as especificações. A liberação in vitro da formulação foi estudada de acordo com o procedimento de dissolução da USP XXIII. As formulações resultaram em liberação normal, seguida por liberação controlada por 12 h, o que indica a liberação bimodal de cloridrato de ziprasidona dos comprimidos matriz. Os dados obtidos se adequaram aos modelos de Peppas. A análise de valores de n da equação de Korsmeyer indicou que a liberação do fármaco envolveu mecanismos não difusionais. Por este estudo, pode-se concluir que os comprimidos bicamada de ziprasidona.HCl e de triexifenidila.HCl serão um bom caminho para estender o metabolismo e para melhorar a biodisponibilidade de ziprasidona.HCl e de triexifenidila.HCl.

Mucoadhesive drug delivery systems interact with the mucus layer covering the mucosal epithelial surface, and mucin molecules and increase the residence time of the dosage form at the site of absorption. The drugs which have local action or those which have maximum absorption in gastrointestinal tract (GIT) require increased duration of stay in GIT. Thus, mucoadhesive dosage forms are advantageous in increasing the drug plasma concentrations and also therapeutic activity. In this regard, this review covers the areas of mechanisms and theories of mucoadhesion, factors influencing the mucoadhesive devices and also various mucoadhesive dosage forms.

The present study involves the determination of antioxidant capacity and in vitro α-amylase and lipase inhibitory activity of the Crotalaria juncea Linn extract. The content of polyphenols, flavonoids, and tannins in the extracts was estimated by spectrophotometry. Antioxidant activity on goat liver lipid peroxidation and linoleic acid emulsion were determined and α-amylase and lipase inhibitory activity was also evaluated. All the extracts had shown antioxidant property, α-amylase, and lipase inhibitory properties. Aqueous extract was found to show maximum antioxidant activity on goat liver. Antilipid peroxidation and antioxidant activity were determined to be 66.94 ± 0.616 (p < .01) and 59.54 ± 0.2 (p < .01), respectively. Maximum α-amylase and lipase inhibitory activities of 71.42 ± 1.37 (p < .01) and 57.14 ± 2.74% (p < .01), respectively, were exhibited by macerated methanol extract. The results had shown that all the extracts exhibited low inhibition and antioxidant activity as compared to st...

D-galactose, a reducing sugar, induces oxidative stress resulting in alteration in mitochondrial dynamics and apoptosis of neurons. Curcumin and hesperidin are antioxidants possessing multimodal functions; hence, their contribution in minimizing D-galactose induced ageing was assessed in the present study. A week prior to D-galactose treatment (150 mg/kg; s.c. for 56 days), animals were treated with curcumin alone, hesperidin alone and a combination of curcumin (50 and 100 mg/kg; orally) with hesperidin (10 and 25 mg/kg; orally) for 63 days. A naive control was also maintained. Behavioural studies, tricarboxylic acid cycle enzymes, mitochondrial complexes, protein and lipid oxidation and glutathione levels were assessed in the brain mitochondrial fraction. Western blot analysis of caspase-3, cleaved caspase-3 and histological assessment of the CA1 region of the hippocampus were carried out. D-galactose induced significant cognitive deficits, biochemical changes and histological alterations. Individually, curcumin was more effective than hesperidin in reducing the levels of oxidized lipids, proteins, cleaved caspase-3 expression and mitochondrial enzymes. The combination reduced the expression of cleaved caspase-3, malondialdehyde, improved mitochondrial enzymes and glutathione levels. In combination, curcumin and hesperidin protect the morphological facets and improve biochemical functions of neurons thereby improving cognition.

In this review article the basic principle of separation process during Micellar electro kinetic chromatography (MEKC) are described. The separation mechanism in MEKC is based on differences in equilibrium between an aqueous Phase and micellar Phase. These Phases are moving different velocities, due to a combination of electrophoresis & electro osmosis. It is a useful branch of capillary electrophoresis (CE) that utilizes surfactant above critical micelle concentration (CMC) as pseudo-stationary phase. MEKC can be employed to separate both charged and neutral molecules, individually or simultaneously, including chiral compounds. MEKC benefits from high peak efficiency due to electro-osmotic flow (EOF) in the separation capillary, compounded with large variety of synthetic surfactants, organic modifiers, temperature and variable separation voltage has made MEKC the method of choice for separation scientists. In this review, we present the introduction of CE, fundamentals of surfactant chemistry as it relates to MEKC, separation principles in MEKC including equations involved in calculating separation parameters (capacity factor, resolution etc.).

The present study evaluated the therapeutic benefit of the combination of carvacrol, an isoprenoid having potential anti-inflammatory action, with methotrexate in suppressing Complete Freund's Adjuvant induced arthritis and attenuating methotrexate induced hepatic damage. Arthritis was induced in rats with Complete Freund's Adjuvant. Animals received methotrexate (2 mg/kg) intraperitonealy once a week for 5 weeks alone and along with carvacrol orally (50 and 100 mg/kg) respectively from the 10th to the 42nd day. Control and carvacrol alone group were also studied. Paw volume, hypernociception, and erythrocyte sedimentation rate were evaluated as arthritic markers. Hepatic marker enzymes in serum; myeloperoxidase, protein oxidation, and oxidative measures were determined in the liver homogenate. Liver histological assessments were also carried out. Methotrexate significantly controlled arthritis; however, liver damage was evident due to oxidative stress and rise in myeloperoxidase levels. Carvacrol suppressed the hyperalgesic response, significantly alleviated arthritis and reduced damage to the hepatocytes owing to a decline in the levels of myeloperoxidase and oxidative markers. High dose of the combination reduced the levels of glutamic oxaloacetic transaminase, glutamic pyruvic transaminase and alkaline phosphatase by 24.74%, 30.2% and 28.14% compared with methotrexate treatment. Histological assessment also revealed that carvacrol minimizes methotrexate induced liver toxicity. In combination, carvacrol promoted the anti-arthritic action of methotrexate, reduced neutrophils infiltration and peroxidative damage to the liver. Therefore, carvacrol can serve as a useful adjuvant and promote the safe use of methotrexate in the management of arthritis.

The present study evaluated the antihypercholesterolemic effect of Macrotyloma uniflorum (Lam.) Verdc extract by examining its effects on food consumption, weight gain, serum lipid profile, serum glutamate oxaloacetate transamianse (SGOT), serum glutamate pyruvate transaminase (SGPT), and body fat in rats.Animals were fed with experimental high-fat diets (HFD) that contain 10% lard plus, 5% corn oil. Food intake and body weight were measured. Serum samples were analyzed for the estimation of lipid profiles and other biochemical parameters by using kits.The consumption of ethanol and water extract of experimental plant for 5 weeks caused the decrease in total cholesterol (TC), triglycerides, low-density lipoprotein (LDL), very low density lipoprotein (VLDL) SGOT and SGPT significantly (p.01), and increase in high-density lipoprotein (HDL) significantly (p.01). The rat group fed with HFD has shown higher serum TC, TG, LDL, VLDL, SGOT, SGPT, and lower HDL than in the normal control group (p.01). Fecal excretion of cholesterol in the ethanol extract-treated groups was significantly higher than those treated with water extract. Body weight in the water extract-treated groups was significantly lower than that in the ethanol extract-treated groups.This study demonstrated that M. uniflorum (Lam.) Verdc extracts have strong activities against hypercholesterolemia and obesity suggesting a potential usefulness of M. uniflorum (Lam.) Verdc extracts as functional ingredients.

The study investigated the role of Spirulina platensis in reversing sodium fluoride-induced thyroid, neurodevelopment and oxidative alterations in offspring of pregnant rats. The total antioxidant activity, phycocyanins, and β carotene content were quantified in Spirulina. Thirty female pregnant rats were allocated to six groups and treatment initiated orally from embryonic day (ED) 6 to postnatal day (PND) 15. Treatment groups included control, Spirulina alone, sodium fluoride (20 mg/kg) alone, and sodium fluoride along with Spirulina (250 and 500 mg/kg). Serum fluoride levels were determined on ED 20 and PND 11. Offspring were subjected to behavioural testing, estimation of thyroid levels, oxidative measurements in brain mitochondrial fraction and histological evaluation of the cerebellum. Fluoride-induced alterations in thyroid hormones, behaviour and increased oxidative stress. Spirulina augmented the displacement of fluoride, facilitated antioxidant formation, improved behaviour and protected Purkinje cells. Supplementing Spirulina during pregnancy could reduce the risk of fluoride toxicity in offspring.

Ipomoea pes-tigridis is an annual herbaceous twining vine which belongs to the family Convolvulaceae. Each part of the plant is used for multitude biological uses. The current work is oriented towards exploring the microanatomical, physicochemical and phytochemical aspects of the plant. The transverse section (TS) of the leaf and TS and longitudinal section (LS) of the stem were studied. The powdered microscopical studies of leaf, stem and fruits were observed. The chemo microscopical studies using various staining reagents like toluidine blue, safranin, schules reagent and sudan III were performed. The physicochemical parameters performed were determination of ash values, extractive values and fluorescence analysis. The aerial parts of the plant was dried and powdered and then after defatting with petroleum ether was extracted with methanol and then subjected to phytochemical screening. The thin layer chromatographic (TLC) analysis was carried out for the methanolic extract followed by the high performance thin layer chromatographic (HPTLC) standardization. The anatomy of the leaf, stem and fruits showed abundant long, slender, uniseriate covering trichomes and sessile glandular trichomes. The main tissue of diagnostic tissue of the stem was found to be spiral shaped vessels. The vascular bundles were bicollateral which was considered to be a typical character of Convulvulaceae family. The chemomicroscopical studies revealed the presence of suberin, cutin, lignin and cellulose in the cell walls. Stomatal number was determined to be high in the upper epidermis than the lower one. Microscopic measurements revealed the length of trichomes to be high in the stem region. Fluorescence analysis showed wide range of fluorescence colours and all the three parts showed similar colours with slight changes in intensity. Water soluble extractive values were found to be high which shows that most of the phytoconstituents may be polar soluble. The aerial part after defatting with petroleum ether was extracted with methanol and the percentage yield obtained was found to be 12.55% w/w. The preliminary phytochemical chemical tests performed showed the presence of flavonoids, alkaloids, tannins and cardiac glycosides. The TLC studies foe flavonoids showed five prominent spots with yellow and blue colour fluorescence. The HPTLC standardization revealed the presence of scopoletin, flavonoid I and flavonoids glycoside and six unknown compounds. The pharmacognostical studies performed has identification of the significant features and standards for the proper identification of the plant from its related species as well as in the detection of adulteration/substitution. Hence, the matter embodied in this article will be helpful in establishment of suitable monograph for the plant.

Aging is associated with progressive decline in mental abilities and functional capacities. Postmitotic tissues are most vulnerable to alteration due to oxidative damage leading to behavioral and biochemical changes. We hypothesized that the anatomical and functional facets of the brain could be protected with powerful antioxidants such as piperine and curcumin by examining their effects individually and in combination in delaying senescence induced by d-galactose. Young adult male Wistar rats were treated with piperine (12 mg/kg) alone, and curcumin (40 mg/kg) alone; and in combination for a period of 49 days by the oral route with treatment being initiated a week prior to d-galactose (60 mg/kg, i.p.). A control group, d-galactose alone and naturally aged control were also evaluated. Behavioral tests, hippocampal volume, CA1 neuron number, oxidative parameters, formation of lipofuscin like autofluorescent substances, neurochemical estimation, and histopathological changes in CA1 region of hippocampus were established. Our results suggest that the combination exerted a superior response compared to monotherapy as evidenced by improved spatial memory, reduced oxidative burden, reduced accumulation of lipofuscin; improvement in signaling, increase in hippocampal volume and protection of hippocampal neurons. We speculate that the powerful antioxidant nature of both, augmented response of curcumin in the presence of piperine and enhanced serotoninergic signaling was responsible for improved cognition and prevention in senescence.

The study was undertaken to evaluate the potential of alcoholic extract of Butea frondosa Koen. ex Roxb against gastric lesions induced in rats using acetic acid plus pyloric ligation. The impact of alcoholic extract of Butea frondosa in doses of 100, 200 and 400 mg/kg as single dose schedules and 200 mg/kg for 7, 14, 21 and 28 days was determined. Parameters assessed were ulcer index, total acidity, acid volume, total protein and pH, non protein sulfhydryls and gastric wall mucus. Extract in dose of 400 mg/kg as a single schedule signifi cantly reduced ulcer severity, total protein and pH as against the control (p

A simple, economic, accurate reverse phase isocratic HPLC method was developed for the quantitation of anastrozole in tablet dosage form. The quantification was carried out using Gracesmart RP18, 5 μ (100 mmx4.6 mm) with UV detected at 215 nm. The elution was achieved isocratically with a mobile phase comprising a mixture of buffer (pH 6.0) and acetonitrile (1:1, v/v). The flow rate was 1.0 mL/min The procedure was validated as per ICH rules for Accuracy, Precision, Detection limit, Linearity, Reproducibility and Quantitation limit. The linearity concentration range was 10-20 mcg/mL with the correlation coefficient of 0.9935. The percentage recovery for Anastrozole was found to be 97.31±2.2%. Limit of detection and limit of quantitation values were found to be 0.351 mcg/mL and 1.053 mcg/mL. The method has been successfully used to analyze commercial solid dosage containing 1mg of anastrozole with good recoveries and proved to be robust.

The synthesis of some 4-(arylsydnonyl)-2-(4-arylhydrazono-3-methyl-5-oxo-2-pyrazolin-1-yl)- thiazoles by reacting 1-thiocarboxamido-3-methyl-4-(aryihydrazono)-2-pyrazolin-5-ones with different 4-bromoacetyl-3-arylsydnones is described. A few compounds from this series were screened for their anti-inflammatory, analgesic, and CNS depressant activities. Among the tested compounds 6s, 6d, 6n, and 6u showed significant anti-inflammatory activity comparable with that of standard drug Ibuprofen. Compounds containing chlorine and carboxylic substituents are more active. 6f, 6r, and 6u showed marked analgesic activity and most of the compounds tested showed promising CNS depressant activity comparable with that of standard drug pentobarbitone.

AIM: The aim of this study was to investigate the antioxidant and hepatoprotective activity of ethanolic extract of the leaves of Polygonum glabrum in carbon tetrachloride (CCl4) induced hepatotoxicity in rats. METHODS: Rats were pretreated orally for 8 days with the ethanolic leaf extract of P. glabrum (200 and 400 mg/kg) and curcumin (100 mg/kg) as the standard prior to CCl4 (1ml/kg body weight, intraperitonial) intoxication. Hepatoprotective action was assessed based on the decrease in the levels of hepatic serum markers such as serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), alkaline phosphatase (ALP), total bilirubin (TB), direct bilirubin (DB) and increased total protein levels. Further, liver tissue was subjected to histopathological studies and also assessed for oxidative parameters such as malondialdehyde (MDA), superoxide dismutase (SOD), catalase (CAT) and glutathione (GSH) levels. RESULTS: Pretreatment with curcumin and ethanolic leaf extract of P. glabrum significantly inhibited CCl4 induced increase of SGPT, SGOT, ALP, TB and DB levels in serum and decrease in total protein levels. Significant and dose dependent increase in the hepatic SOD, CAT, GSH activities along with decrease in MDA levels were observed in the curcumin and P. glabrum extract pretreated animals. The liver histological examination also showed lowered damage in the extract pretreated animals. CONCLUSION: The ethanolic leaf extract of P. glabrum exhibited significant hepatoprotective effect which could be attributed to its antioxidant activity.

Floating tablets were designed to prolong the gastric residence time after oral administration and to achieve controlled release of Lansoprazole to treat gastric ulcers. A combination of effervescent and noneffervescent mechanism is used. HPMC (Hydroxy propyl methyl cellulose) was used as swelling polymer and sodium bicarbonate as gas generating agent to reduce the floating lag time. Floating tablets with varying proportions of sodium bicarbonate and HPMC were prepared. The prepared formulations were evaluated for various tablet and floating parameters. Tablet properties were found to be within the limits according to procedures prescribed in USP. They had a floating lag time around 3-7 seconds and floating time more than 24 hours. The cumulative % drug release in simulated gastric fluids after 10 hours was 70% - 95%. The mechanism of drug release was analyzed by fitting the release data into various kinetic models. It was found that all the formulations best fit the Higuchi’s model.