Copyright: 2006 Unisa Webstaff A collaborative research programme between the Council for Scientific and Industrial Research (CSIR) in South Africa and the National Cancer Institute (NCI) in the USA aimed at the screening of plant extracts and identification of potentially new anti-cancer drug leads was initiated in 1999. Plant extracts that exhibited anti-cancer activity against a panel of three human cell lines (breast MCF7, renal TK10 and melanoma UACC62) at the CSIR were screened by the NCI against sixty human cancer cell lines organized into sub panels representing leukaemia, melanoma and cancer of the lung, colon, kidney, ovary and central nervous system.
Present study was designed to evaluate Hypoglycemic and hypolipidemic activity of pioglitazone in normal and Streptozotocin-Nicotinamide induced diabetic in rats. Pioglitazone (10mg/kg, p.o) was administered for 28 days in rats injected with single dose of Streptozotocin (65 mg/kg, i.p, STZ) and nicotinamide (110 mg/kg, i.p, NIC). Administration of STZ-NIC in rats showed a significant (p<0.001) increased in the levels of serum glucose, glycosylated heamoglobin (HbA1c), Total Cholesterol (TC), Triglycerides (TG) and High density lipoprotein (HDL) whereas the levels of Low density lipoprotein (LDL)) were found to be non significant. We concluded that PIO (10 mg/kg) is effective in controlling blood glucose levels and improves lipid profile in euglycemic as well as diabetic rats.
In the present study TRANS-01, a polyherbal formulation was explored for its CNS activity. The CNS activity was tested using mice in several experimental models like exploratory behavior, muscle relaxant activity and pentobarbitone sodium-induced sleeping time tests. The formulation at 200, 400 and 600 mg/kg showed significant dose dependent anxiolytic activity in hole board test and insignificant effect on pentobarbitone induced slleing time and muscle coordation. Whereas Trans -01 at 800 mg/ kg showed significant Sedative effect in hole board test and motor incoordination and muscle relaxant activity in traxction and rota rod tests respectively.
The present paper reports the antianaphylactic, antihistaminic and mast cell stabilization activity of HN-08, a polyherbal formulation in various experimental models. HN-08 is an herbal formulation containing extracts of various plant constituents. The compound HN-08 was evaluated using Wistar rats and Duncan Hartley guinea pigs. The antianaphylactic activity was investigated in rats using the active anaphylaxis model. The effect on mast cell stabilization was performed by ex vivo challenge of antigen in sensitized rat intestinal mesenteries. Antihistaminic activity was studied in guinea pigs using histamine-induced bronchospasm where preconvulsive dyspnea was used as an end point following exposure to histamine aerosol. Dose response studies on test formulation were conducted using different levels of post oral doses (125, 250, and 500 mg/kg, p.o) in anaphylactic shock-induced bronchospasm in rats. Based on the activity profile optimum dose was selected for further studies.
Background: Quinazolinone is a compound made up of two fused six member simple aromatic rings-benezene and pyrimidine ring and have been reported to posses versatile type of biological activities such as anticancer, anticonvulsant, anti-inflammatory, antihelminthic, antimicrobial activities. Methods: A series of novel substituted-[1,2,4]triazolo[1,5c]quinazolinone derivatives (K11-19) were synthesized by mannich reaction using formamide and different secondary amines. Structures of compounds synthesized were confirmed by FT-IR, 1H-NMR and Mass spectroscopic analysis. All synthesized compounds were screened for anti-inflammatory activity. The anti-inflammatory activity was performed at concentration (100 mg/kg body mass) by rat paw oedema model. Diclofenac sodium (50 mg/kg) was used as standard. Results: All synthesized compounds have shown anti-inflammatory activity as all has significant reduction in inflammation when compared to inflammatory control group. Compounds K 15, K 18 and K 19 have shown very good anti-inflammatory activity comparable to standard drug Diclofenac sodium.
The maximal mycelial growth recorded in glucose amended cuture, and in the Production and isolation of extra cellular carbohydrates and proteins the maximum amount of protein 231 mg/L was record in sucrose amended medium besides Ganoderma lucidium produced maximum amount of carbohydrate (975 mg/L) and protein (55.4 mg/L) in synthetic medium. The absorption peaks of polysaccharide isolated from the fruit body of G. lucidium coincide with the 1,3-β-D glucan (Sigma). Effect of polysaccharide on fibrosarcoma 180 induced mice. The body weight of sarcomainduced mice was increased by 11% than the normal mice. In polysaccharide treated mice the body weight significantly decreased and was similar to that of the normal mice, and remarkable increase in the weight of the spleen (336%) and kidney (10.6%) in sarcoma induced mice than normal mice whereas the weight of liver decreased to much as 29.3% in induced mice. In polysaccharide treated mice a remarkable percent of decrease in weigh of the liver (116%), spleen (53.1%) and kidney (35.46%) were observed. The concentration of DNA and RNA were elevated in induced mice.
In present study several substituted 1, 3-oxazolidines were synthesized by condensation of reduced Schiff base of phenylglycinol with different aldehydes. All the synthesized compounds showed good to moderate antimicrobial activity. The antimicrobial activites were performed by disc diffusion method and minimum inhibitory concentration determination by serial agar dilution method. Thus among the ten compounds, 3-[3-2-furyl methyl)-4-phenyl- 1,3-Oxazolidin-2-yl]-1H-indole (4a), 2-(2-furyl)-3-(2-furyl methyl)-4-phenyl-1,3-Oxazolidine (4b) and 4-[3-(2-furylmethyl)-4-phenyl-1,3- oxazolidin-2-yl]-2-methoxy phenol (4h) were found to have a moderate to significant antimicrobial activity against all the strains used. Compound 2-(4-chlorophenyl)-3-(2- furylmethyl)-4-phenyl-1, 3-oxazolidine (4j) showed very good antifungal activity than- the other compounds tested. Further more, compounds containing -Cl-, -OCH3, -OH groups as substituents were found to be potent antimicrobial agents. Moreover the heteroaromatic substitutions also showed very good antimicrobial activities.
Sudden cardiac death is a primary cause of mortality in patients with cardiovascular diseases, is caused by the loss of regular cardiac rhythm. In the present study 1, 3-oxazolidines were synthesized and their physiochemical parameters like melting point, retardation factor were analyzed. All the compounds were screened for their antiarrhythmic activity by calcium chloride- induced arrhythmias in isolated frog heart at graded dose level. Compounds 4-[3-(2-furylmethyl)-4-phenyl-1,3-oxazolidin-2-yl]-2-methoxy phenol (8), 4-[3-(2-furylmethyl)-4-phenyl-1,3-oxazolidin-2-yl]phenol (9) and 2-(4-chlorophenyl)-3-(2-furylmethyl)-4-phenyl-1, 3-oxazolidine (10) showed very good negative chronotropic and inotropic effect by blocking the calcium entry. All other compounds showed moderate activity. Compounds containing 4-hydroxy and 3-methoxy, 4-hydroxy and 4-chloro substitutions were found to increase the antiarrhythmic activity.
In the development of organic therapeutic agents, pharmaceutical scientists have explored numerous approaches in finding and developing organic compounds that are now available to us in dosage forms suitable for the treatment of our ills and often for the maintenance of our health The present work deals with evaluation of anti-tubercular activity of various aldehyde derivatives synthesized by Knoevenagel condensation method and substitution in the second position of indane-1, 3-dione nucleus. The formation of Spiro-oxirane derivatives by reaction with alkaline hydrogen peroxide was also attempted. The synthesized derivatives were screened for anti-tubercular activity and the compounds demonstrated some remarkable features to be actively considered as anti-tubercular drugs.
A series of novel N-[2-(substitutedphenyl)-5-methyl-4-oxo-1,3-thiazolidin-3-yl]benzamides (4a-g) were synthesized and structurally confirmed by elemental analysis, IR, 1H NMR and MS spectral spectral data. All the synthesized 1,3-thiazolidin-4-one analogues (4a-g) at various concentrations (10, 20, 50, 100 and 200 mcg/ml) have been evaluated for in vitro cytotoxicity against Dalton's lymphoma ascites (DLA) cancer cell line by trypan blue exclusion method, in comparison with standard drug doxorubicin hydrochloride. Out of these seven compounds, three compounds (N-[2-(2,4-dichlorophenyl)-5-methyl-4-oxo-1,3-thiazolidin-3-yl]benzamide (4c), N-[5-methyl-2-(4-nitrophenyl)-4-oxo-1,3-thiazolidin-3-yl]benzamide (4g) and N-[2-(2,3-dichlorophenyl)-5-methyl-4-oxo-1,3-thiazolidin-3-yl]benzamide (4b)) inhibited 100%, 86% and 85% DLA tumor cells at 100 mcg/ml concentration, whereas standard drug doxorubicin exhibit 100% DLA inhibition at a concentration of 100 mcg/ml. From the above study, compound 4b and compound 4c which showed better results (> 60% inhibition) at lowest concentration were further selected for screening in vivo anticancer activity against Dalton's lymphoma ascites (DLA) cancer cell line at the dose of 50 mg/kg body weight/i.p. in comparison with 5-fluorouracil (20 mg/kg body weight/i.p.) by determining different parameters like body weight analysis, packed cell volume, viable tumor cell count, increase in life span (%), followed by hematological profiles [red blood cell (RBC), white blood cell (WBC), hemoglobin (Hb) and platelet count] and serum biochemical parameters [aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), total cholesterol (TC) and triglycerides (TG)] of DLA bearing mice. In the in vivo anticancer evaluation, among three compounds screened, compound 4c emerged as more potent inhibitor of DLA with an increase in life span (ILS) of 74.01%, whereas standard drug 5-fluorouracil exhibit ILS of 92.20%. The in vivo anticancer experimental results indicated that, compound 4c (p < 0.05) and 5-fluorouracil showed significant (p < 0.01) decrease in body weight gain, packed cell volume, viable tumor cell count and increased the life span of DLA tumor bearing mice, followed by hematological and serum biochemical profiles were significantly restored to normal levels in compound 4c (p < 0.05) and 5-fluorouracil (p < 0.01) treated groups as compared to DLA control mice.
The synthesis and activity of 1,3-indandione derivatives as acetylcholinesterase (AChE) inhibitors are reported. The synthetic keystep consists of the Knovenagel olefination between 1,3-indandione and a substituted (1-benzylpiperidin-4-yl)methanal followed by selective double bond reduction. AChE inhibitory activity was measured by a quick fluorimetric method. One of the new compounds showed a significant interaction with the enzyme. Molecular modelling studies were performed in order to propose the binding modes within the AChE gorge compared to the known inhibitor Donepezil.
Haematoxylin and eosin Immunohistochemical staining of gastric ulcers after ulcer induction in rats. As illustrated in Fig. specimen (a) shows Intact Mucous membrane in control treated rat showing granular tissues composed of macrophages, fibroblasts and endothelial cells forming microvessels. Congestion of mucosal blood vessels in diclofenac treated group, specimen (b). No damage was seen to mucosa of rat treated with test compound, 3d, specimen (c), 3k, specimen (d) and 4b, specimen (e), these specimens c-e were identical to that of the control, specimen (a). Original magnification 200·.
Results of analgesic activity of synthesized compounds against acetic acid induced writhing tests in mice
Diclofenac sodium is an important component of prescriptions of arthritis patients since last 25 years. But even this drug is not an exception to the limitations of gastrointestinal adverse effects associated with the traditional non-selective NSAIDs. The free -COOH group is reported to be the main culprit responsible for GI toxicity of these NSAIDs. Derivatives of 1, 3, 4-oxadiazole are also known to have a broad spectrum of biological activities. Schiff bases and 1, 3, 4-oxadiazole derivatives of diclofenac were tested in vivo for their anti-inflammatory activity. The compounds, which showed significant analgesic and anti-inflammatory activities comparable to the standard drug diclofenac, were screened for their ulcerogenic potential to make sure that designed and synthesized compounds lack ulcerogenecity associated with parent prototype Diclofenac Sodium from traditional non-selective NSAIDs. The study showed that compound 3k possessed most significant anti-inflammatory and analgesic activity compared to parent drug Diclofenac Sodium. The compound also showed non ulcerogenic action at 12 times the therapeutic dose in animal models. The ulcers in rats were analyzed by histopathological studies. Results showed that compound 3e, 3g, 3k, 4c, 4e and control group were unremarkable, and were also devoid of mucosal hemorrhages, mucosal congestion and ulceration compared to that of standard drug Diclofenac.
Comparison of Anticonvulsant activity of test compound (PTZ) Data was analyzed by one way ANOVA followed by Dunnett’s test (n =6),* P<0.05 **P<0.01 
Comparison of Anticonvulsant activity test compounds of MES model Data was analyzed by one way ANOVA followed by Dunnett’s test (n =6),* P<0.05 **P<0.01 
Comparison of Behavioral studies of test compounds using Actophotometer model Data was analyzed by one way ANOVA followed by Dunnett’s test (n =6),* P<0.05 **P<0.01 
Thiadiazole with styryl and quinazoline are reported to exhibit wide range of anticonvulsant, sedative, tranquilizer, analgesic, antimicrobial, anesthetic, anticancer, antihypertensive, anti-inflammatory, diuretic and muscle relaxant properties. With the intention to develop potent anticonvulsant agents we have designed, synthesized 3-[5-substituted 1, 3, 4-thiadiazol-yl]-2-styryl quinazolin-4(3H)-ones derivatives. The synthesized derivatives were tested in vivo for their anticonvulsant activity using MES, PTZ and Actophotometer model. The synthesized compounds, showed significant anticonvulsant activity comparable to the standard phenytoin, diazepam and phenobarbital. The compounds BJ-1 (5.68Sec), BJ-7 (5.68Sec) and BJ-8 (6.3 Sec) were found to induce a significant anticonvulsant activity against MES model compared to standard drug Phenytoin 5.67 Sec and the compound BJ-8 (124 Sec), BJ-9 (122Sec), BJ-7 (122Sec) were most potent against PTZ model (standard drug diazepam). Around five compound were found to be significantly potent against Actophotometer model BJ-1 (2.59Sec), BJ-5 (264Sec), BJ-2 and BJ-9 (266Sec), BJ-4 (270Sec) and BJ-3 (272Sec) were found to exhibit significant anticonvulsant activity (decrease locomotor activity) compared to std drug phenobarbital (257Sec). Thus, in conclusion, the compound BJ-1 was found to be most potent in MES whereas BJ-8 in actophotometer model exhibited significant activity against PTZ model indicating the critical role played by substituted on phenyl ring. This has complied us to get detailed insights of structure activity relationship studies of the synthesized derivatives. And it can be said that one electron rich [–N (CH 3) 2, –OH, OCH 3 O] and another electron withdrawing group [-F,-NO2] are required for potent anticonvulsant activity of these type of compound.
Design, synthesis and biological evaluation of simplified linear and cyclic peptidomimetic analogues of FR235222 (1), natural immunosuppressant and HDAC inhibitor, bearing hydroxyketone moiety as more stable zinc binding group, have been reported. Linear dipeptides (6a-b) show significant antiproliferative activities and are chosen to be promising lead compounds for further optimization, in order to elucidate molecule-enzyme surface recognition. © 2014, SILAE (Italo-Latin American Society of Ethnomedicine). All rights reserved.
The gum of Boswellia serrata has been widely used in ayurvedic and traditional system of medicine for the treatment of inflammation. 3-acetyl-11-keto-β-boswellic acid (AKBA) is the most potent pentacyclic triterpenic acid present in gum of Boswellia serrata for anti-inflammatory and antiarthritic activity. The objective of the present investigation was to study the anti-inflammatory activity of nanogel formulation of AKBA against carrageenan induced rat paw edema. Topical gel for in-vivo study of AKBA and AKBA polymeric nanoparticles was formulated by using 1% Carbopol 940. Results of in-vivo comparison study showed much higher anti-inflammatory activity of AKBA nanogel compared to AKBA gel of equivalent concentration.
Effect of Amaranthus caudatus on serum triglyceride level in Triton WR-1339 induced hyperlipidemic rats.
Effect of Amaranthus caudatus on serum LDL level in Triton WR-1339 induced hyperlipidemic rats.
This study was designed to determine the effect of methanolic and aqueous extracts of Amaranthuscaudatus (A. caudatus) leaves (Amaranthaceae) on serum lipid profile changes in normal and Triton WR-1339 induced rats with view to elucidate its possible effects on cardiovascular diseases induced hyperlipidemia. To determine hypocholesterolemic activity in normal rats, the adult wistar rats were divided into 8 groups of 6 animals each, normal control, standard(Atorvastatin), methanolic and aqueous extracts of A.caudatus were treated at doses 200, 300 and 400 mg/kg body weight. The treatment period lasted for 8 days. Blood samples were collected from retro orbital puncture. The serum harvested was analysed for triglycerides and total cholesterol. The two extracts of A. caudatus were evaluated in Triton induced hyperlipidemic rats. Wistar rats were divided into 9 groups of 6 animals each, normal control, triton control, standard(Atorvastatin), methanolic and aqueous extracts of A.caudatus were treated at doses 200, 300 and 400 mg/kg bodyweight.Blood samples were collected from retro orbital puncture at 0 hr, 24 hr and 48 hr. The serum harvested was analysed for triglycerides, total cholesterol, HDL, LDL. Results showed that the methanolic extract of A. caudatus at 400 mg/kg bodyweight significantly (P<0.01) reduced the level of total cholesterol and triglycerides in normal rats. Methanolic extract of A.caudatus showed significant decrease(P<0.01) in the level of total cholesterol, triglycerides, LDL and increase in level of HDL at 400 mg/kg p.o. after 24 hr and 48 hr in Triton induced hyperlipidemic rats whereas aqueous extract of A.caudatus showed significant decrease (P<0.05) only in the level of triglycerides at 400 mg/kg p.o. after 24 hr and 48 hr. Hencethe results of this study suggested that leaves of methanolic extract of Amaranthus caudatus possesses anti hyperlipidemic activities.
The lipid lowering activity of Randia dumetorum fruit extract & Paederia foetida aerial part extract has been studied in Triton WR-1339 induced hyperlipidemia in male albino rats. The dried and ground parts of fruit of Randia dumetorum and aerial part of Paederia foetida were subjected to extraction with methanol using a soxhlet apparatus for 72 Hrs. The obtained methanolic extracts were suspended in distilled water and administered orally to Swiss albino rats through oral feeding tube till a period of 2 days. Prior to that male albino rats were randomly divided into five groups. Groups I and II serves as vehicle control (demineralized water) and triton control (Triton WR-1339 - 200 mg/kg; i.p.), respectively. Group III was treated with atorvastatin (7.2 mg/kg).Groups IV and V were treated with test substance Paederia foetida and Randia dumetorum extract, at the dose of 400 mg/kg/day respectively as single dose for two days. The Blood samples of each animal were collected at 0, 18, 24,40and 48 Hr post treatment and the results were analyzed. All the data were analyzed by using one way ANOVA followed by Dunnett's t test to observe any significant difference. The statistical significance of results was tested at two confidence levels viz. p<0.05 and p<0.01.The mean bodyweight of animals of each group was calculated daily till the end of the experiment. In this experiment Paederia extract resulted in lowering of serum total cholesterol from 157.47±17.75mg/dl (18 th Hr) to 133.15±16.52mg/dl (24 th Hr), Randia extract lowers it from 121.38±21.14mg/dl (18 th Hr) to133.44±19.64mg/dl (24 th Hr) and atorvastatin reduces it from 125.80±15.46mg/dl (18 th Hr) to 112.80±18.27mg/dl (24 th Hr). In case of serum triglycerides, atorvastatin treatment resulted in lowering from 661.72±153.31mg/dl (18 th Hr) to337.34±105.01mg/dl (24 thHr), Paederia extract non-significantly lowers it from 865.47±134.87mg/dl (18 th Hr) to 457.03±96.84mg/dl (24 th Hr), and incase of randia extract there was non-significant decrease from 557.13±197.66mg/dl to 345.99±118.45mg/dl.The results of the present study demonstrated lipid lowering activity in fruit extract of Randia dumetorum.
Brain derived neurotrophic factor (BDNF) concentration has a relationship with Alzheimer's dementia. BDNF is a neurotropin that has a neuroprotective effect on Alzheimer's disease. The BDNF increase in the area around the lesion is closely related to the progress of nerve function recovery. Coix lacryma-jobi leaf ethanol extract is thought to increase the expression of matureBDNF. The purpose of this study was to observe the effect of ethanol extract of hanjeli leaves on the expression of mBDNF in rat brain cells induced by traumatic brain injury as Alzheimer's disease. This research was design in the form of a post test only control group. The number of samples was 33 mice divided into 3 groups, normal mice without treatment (A), trauma model without hanjeli ethanol extract (B) and trauma model group given oral hanjeli ethanol extract 200 mg per weight (kg)
A 14-day subchronic genotoxicity of Nimesulide was evaluated by employing mouse bone marrow chromosomal aberration test. The Nimesulide administered orally for 2 weeks at the rate of 1.5, 2.5, 5 mg/kg body weight in swiss albino mice. The results show decreased mitotic activity in all groups of Nimesulide treatments. Similar results concerning the chromosomal aberrations revealed in all treated animals. However statistically significant genotoxicity was seen only with the higher dose of Nimesulide. The obtained results indicate that 2 weeks continuous treatment of Nimesulide is moderately genotoxic in the bone marrow cells of swiss albino mice.
A pandemic occurring microscopic virus which is named 'novel coronavirus' causes respiratory illness and gastrointestinal infections spread by animals and winged creatures. By stopping the transmission of respiratory droplets (sniffles, cough), stopping bodily contact with the infected, taking and maintaining extortion about a few severe versatile rules have the ability to put an end in the expansion of this virus. Instead of consumption of foods carrying saturated fat or bad cholesterol, individuals should have a diet rich in minerals, beta-carotene, vitamins (C, D, and E) and zinc to improve the innate and adaptive immune system to fight against this virus. In purpose to decline the risk of this virus, natural growing color varieties vegetable consumption and reject the refrigerated fat consisting of food along meet with expire periods. As excessive intake of vitamin C cause excretory system failure, good and certain of it from cultivated (lemons, tomato, etc.) or artificial sources consumption can improve the immune system against this pandemic and different respiratory problem. Lacking Inhibiting or the presence of vitamin D is certainly a major characteristic in COVID-19 individuals, in taking vitamin D (oily fish, beef liver, etc.) could help resist from its own deficiency and another related malady. Avoiding foods from outside (such as fast foods, msg., beverages) and increasing the consumption of homemade natural food on daily basis will fill the portion against the risk of this global pandemic. In case of maintaining health service issues, provision of certain rules, inhibition of nutrient-rich constituents or particles, and maintaining social distance (6-feet separated) will stop the widespread of this pandemic. Declining the provoke of the global food crisis one should preside in maintaining the nutrition and nourishment across the globe, with extreme results for health and substance. © 2020, SILAE (Italo-Latin American Society of Ethnomedicine). All rights reserved.
The present study was undertaken to evaluate antioxidant activity of the synthesised naphtho [2,1- b] furan derivatives. 3-nitro-2-acetylnaphtho[2,1-b]furan, 3-nitro-2-acetylnaphtho[2,1-b] furanhydrazone, Ethyl-3-aminonaphtho[2,1b]furan-2-carboxylate, Ethyl-3-(2,5-dimethylpyrrole naphtho[2,1-b]furan-2-carboxylate, 3-(2,5-dimethylpyrrole naphtho[2,1b]furan-2-carboxyhydrazide were synthesised from 2-hydroxy-1- naphthaldehyde. The structure of these compounds was confirmed by analytical, IR and 1H NMR spectral data. The above compounds were evaluated for their antioxidant activity by reducing power and DPPH methods. In reducing power the percentage of inhibition of naphtho [2,1- b] furan derivatives 1,2 and 3 were found 86.66%, 87.34% at 150 μg/ml and 85.18% at 125 μg/ml, similarly in DPPH 90.20%, 86.7% at 150 μg/ml and 84.4% at 125 μg/ml and respectively. These results suggest that the antioxidant effect of naphtho [2,1- b] furan derivatives as a powerful source used for suppression of pimples.
SJ 200, a Polyherbal formulation contains active constituents of various plants which were proved individually in the earlier research work effective for their antispasmodic activity. So in the present study we have evaluated SJ-200 for antispasmodic activity in gastrointestinal spasm on various smooth muscles in vitro and intestinal transit rate in vivo. SJ-200 inhibited spontaneous contraction of rabbit jejunum and also acetyl choline and barium chloride induced contraction dose dependently, 5-HT and acetyl choline induced contraction of rat fundus inhibited dose dependently. SJ-200 also inhibited acetyl choline and calcium chloride induced contraction or rat colon dose dependently. Oral administration of SJ-200 dose dependently reduced intestinal transit in mice when compared to atropine at 0.1mg/kg i.p. SJ-200 at (300 mg/kg) protected mice against diarrhoea induced by castor oil significantly as compared to control and standard loperamide at a dose of 5 mg/kg orally. In the present study it is concluded that SJ-200 inhibits the contraction produced by various spasmogens like acetylcholine, barium chloride, histamine, serotonin and calcium chloride. This suggests that the activity of SJ-200 is non-specific to any spasmogen.
The Emergency Division represents a strategic hospital headquarter to implement pharmacovigilance activities. The ease of access, the care availability of 24 hours to 24 and the patient's multidisciplinary approach make Emergency Division is the ideal access to health care. The data reported in this paper are from the year 2011 the project MEREAFaPS. Reporting of adverse drug reactions (ADRs) were analyzed cases from three major hospitals in the region Campania, Azienda Ospedaliera di Rilievo Nazionale "Gaetano Rummo" of Benevento, Azienda Ospedaliera di Rilievo Nazionale "San Giuseppe Moscati" of Avellino and Azienda Ospedaliera Universitaria "S. Giovanni di Dio e Ruggi D'Aragona" of Salerno.
During the last decay, the commercial importance of Neem tree (Azadirachta indica A. Juss) increased exponentially, as well as its global diffusion and the number of derived products in the market. Despite the identification of hundreds of constituents in the seed oil, the main marketed product, a lot of chemistry still must be carried on. The high complexity of chemical composition and the derived multiple activity ask for an exceptional research validation. Azadiractins, among the main constituents of the oil and so far considered the responsible of the insecticide activity, could be only in part involved, calling for investigation on other constituents, including the degradation products. Starting from reliable chemical data, Biology can take the center of the scene to validate neem as the multipurpose tree of the future. Starting from the actual medical and insecticidal applications it is time to explore other possible commercial applications in accordance with the future depicted by the International Research Institutions.
Chronic fructose treatment in rats has repeatedly been shown to elevate blood pressure in association with insulin resistance, hyperinsulinemia and hyperlipedimia. The purpose of the current study was to investigate the effect of a newly synthesized β blocker PP-28 {1-tertbutylamino- 3-[3-(tert-butylamino-methyl)-phenoxy]-propan-2-ol-oxalate.} on blood pressure, heart rate, plasma glucose, insulin, cholesterol, LDL, HDL, VLDL, and triglycerides levels in rats with fructose induced hypertension. Male Wistar rats weighing 180-200 g were divided into five groups of 8 animals each. Control groups were given ordinary drinking water ad libitum throughout the whole treatment course and the remaining groups were given 10% fructose solution to drink ad libitum for nine weeks. After nine weeks, the fructose-treated animals were assigned the following treatment regimens: fructose-fed, fructose plus PP-28 (3, 10 and 30 mg/kg, p.o.) and fructose plus atenolol (10 mg/kg, p.o.). The animals received these treatment regimens orally for the next two weeks. Fructose-fed rats showed significant increase in blood pressure, plasma glucose, insulin, LDL, VLDL, and triglycerides when compared to control groups but not in cholesterol and HDL level and two week after the treatment with PP-28 (10 and 30 mg/kg,p.o.) significantly reversed the high Blood pressure, Heart rate, TG,LDL and VLDL level significantly in fructose feeding rat. In conclusion, PP-28 was able to prevent BP elevation as well as TG, LDL and VLDL level in fructose-fed rats.
Beta-adrenoceptor blockers are an important class of drugs used in management of patient with cardiovascular diseases. These drugs have been shown to reduced mortility in hypertension. However, the main side effect of these drugs is due to antagonism of β2-adrenoceptors in the airways, resulting in bronchospasm. Therefore, more cardio selective beta-blockers have been developed to offer a lower side effect profile. We have studied a new aryloxypropanolamine derivative (PP-28) with more cardio selectivity and efficacy against hypertension in rats. Oxalate salts of 1-tert-butylamino-3-[3-(tert-butylamino-methyl)-phenoxy]-propan-2-ol. (PP-28) is a novel beta-adrenoceptor antagonist. In-vitro studies in rat isolated right atria, rat uterus and rat distal colon preparations were carried out to investigate the potency of PP-28 towards different beta-adrenoceptor subtypes. The pA2 values of PP-28 for β1, β2, and β3 adrenoceptor were 7.69+/-0.10, 6.03+/-0.08 and 6.10+/-0.14, respectively. The β1/ β2 selectivity ratio calculated was in the order of PP-28 > atenolol > propranolol. PP-28 also blocked significantly isoprenaline induced tachycardia and hypotensive responses in anesthetized rat. Antihypertensive effect of PP-28 was observed in left renal artery ligated (LRA) and 10% Fructose - induce hypertensive rat.Treatment with PP-28 (1, 3 and 10 mg/kg, orally) produced a dose dependent decrease in MAP and heart rate of LRA ligated rats as well as 10% Fructose -induce hypertensive rat. The efficacy of PP-28 was found to be greater then atenolol. In conclusion, PP-28 is a cardioselective beta-adrenoceptor antagonist, possessing potent Antihypertensive effects in left renal artery ligated and 10% Fructose - induce hypertensive rat.
The rapidly growing field of nanotechnology has offered innovative discoveries in medical and industrial fields. The potential risks of these nanoparticles have also been identified via environmental and occupational exposure. Magnesium nanoparticles have gained commercial interest in the areas of waste remediation, water treatment and drug delivery. However, the potential toxic effect of magnesium hydroxide nanoparticles (MgOHNPs) is yet to be unraveled. The present study elucidated the effect of repeated doses of MgOHNPs in rats. Adult Wistar rats were exposed to 0, 50, 100, 200 and 1000 mg/kg body weight of the nanoparticle for 28 days. Exposure to MgOHNPs impaired the functionality of liver and kidney as evidenced by significant elevation in plasma aspartate aminotransferase (AST), alkaline phosphatase (ALP), magnesium, calcium, potassium and creatinine levels compared with control. Also significant reduction in the plasma concentrations of albumin, total protein, globulin and chloride was observed at the tested doses. The altered integrity of these organs was corroborated by a significant elevation in the levels of total protein, AST and ALP and reduction in alanine aminotransferase (ALT), was observed in the kidney. Also, there was a significant reduction in the hepatic total protein. Whereas, a dose dependent significant (p < 0.05) increase was observed in the activities ALP, ALT and AST in the liver. The exposure induced a marked dose-dependent decrease in total cholesterol (TC), triglyceride (TG), and low-density lipoprotein (LDL) and high-density lipoprotein (HDL) cholesterol. However the blood levels of glucose, ALT and hematological parameters remained unaltered throughout the experimental period. These findings suggest that repeated exposure to MgOHNPs may have consequential effects on the liver and kidney functions. © 2019, SILAE (Italo-Latin American Society of Ethnomedicine). All rights reserved.
The Present study was aimed to evaluate the therapeutic effectiveness of 1, 5-benzothiazapine derivative in central nervous diseases. 1,5- Benzothiazipines are the seven-membered heterocyclic ring systems which are reported for their behavioral activities. In the current research, we have investigated the effect of 1,5-benzothiazine derivative for its anti-anxiety, antidepressant and anti-cataleptic activities by using elevated plus maze, forced swim test and chlorpromazine induced catalepsy respectively. Wistar rats were treated with 1, 5- benzothiazapine derivative (5mg/kg, p.o. daily) for 30 days. The results showed significant (p<0.01) anti-anxiety, anti-depressant and anti-cataleptic actions of 1, 5-benzothiazapine derivative. Here we suggested that, these drugs can be further studied in Preclinical and Clinical level for the treatment of central nervous diseases.
The present investigation was carried out to study the antihypertensive activity of the two derivatives (NS1 & NS2) of novel synthetic hybrid compound [N(phenyl)N′{1′6methyl-4-(2-nitrophenyl)-2-thioxo- 1,2,3,4-tetrahydropyrimidine- 5- carboxylic acid ethyl ester} 3′ (4″ imino phenoxy) propane-2- ol thiourea] on 2K1C induced hypertensive rats. The left renal artery (LRA) was ligated by silk suture (no.4) in rats to produce two-kidney one-clip (2K1C) renovascular hypertension and kept for 6 weeks. After 6 weeks, respective treatments were started and continued for 7 days. On 7th day, 30 min after the last dose, the arterial blood pressure and heart rate (HR) of rats were measured by using data acquisition system. LRA ligated rats showed significant (P < 0.01) increment in mean arterial pressure (MAP) compared to non-ligated (normal) rats. NS1 decreased MAP and HR significantly (P<0.01) while NS2 significantly (P<0.01) decreased MAP without affecting heart rate when compared against LRA ligated rats. Standard drugs were significant (P<0.01) in reducing MAP as well as HR of LA ligated rats. In conclusion, both the derivatives (NS1 and NS2) of the novel synthetic hybrid compound showed significant reduction in the blood pressure of 2K1C induced hypertensive rats, while HR was only significantly reduced by NS1. The study needs further investigation to know the exact mechanism of antihypertensive activity of these hybrid compounds.
It is by now well accepted that oxidative stress plays a vital role in initiation and progression of the brain lipid and protein oxidation of Alzheimer patients. Hydrogen peroxide (H 2O 2),as a prooxidant, interacts with transition metals via fenton reaction and produces hydroxyl radicals that initiate lipid peroxidation through malondialdehyde (MDA) production and protein carbonyl oxidation (PCO). Therefore, to back up the system under oxidative stress conditions, it might be beneficial to use antioxidants. Chalcone derivatives (1, 3-diaryl-2-propen-1-ones) are plant flavonoides with free radical scavenging capabilities. The main difference among these derivatives is on their hydroxyl substitution patterns especially on their phenolic rings. The objective of this study was to examine the influence of thirteen different synthetic chalcone derivatives (compound 8-20) on the activity of some of the antioxidant enzymes including CAT, SOD and GPx as well as on the levels of MDA, PCO and GSH against H 2O 2-induced damage on SK-N-MC cells. Our results indicated that chalcone derivatives especially vanilline analogues increased the activities of SOD, CAT and GPx in drug-pretreated relative to H 2O 2-treated cells. In addition, they were capable of reducing the formation of MDA and PCO. The destructive effect of H 2O 2 on the GSH level of the cells was almost totally restored by each of the derivatives. These properties probably are due to free radical scavenging activity of each of the derivatives and thus, it is expected these compounds would attenuate the destructive effects of oxidants.
The known flavone, 5- Hydroxy 3,4′, 6, 7- tetramethoxy flavone from Achillea millefolium L. (Compositae) is found to possess significant antihepatotoxic activity against CCI4 and Paracetamol induced hepatotoxicities (in-vivo) and Thioacetamide and Galactosamine induced hepatoxicities (in-vitro) in rats. The activity was found comparable with Silymarin (50 mg/kg b. w. i. p.). The activity of the compound was reported for the first time.
The title compound (TBO) with bicyclo[3.3.1]nonane skeleton was synthesized in an efficient one pot procedure employing a green methodology. The compound was structurally confirmed by UV-Visible, FT-IR, NMR and single crystal X-ray diffraction analysis. The anticancer activity of TBO was tested against Ehrlich Ascites Carcinoma [EAC] cell lines using In-Vitro methods such as Trypan blue dye exclusion method and MTT assay. The results revealed that TBO showed potent cytotoxicity against EAC cell lines by activating the apoptotic pathway.
Effect of L-33 on Inflexion ratio (IR) in EPM Model, Diazepam induced amnesic model and Scopolamine induced amnesic model in mice (Mean ± Sem)
L-33 (wilmer syrup) is a polyherbal formulation, consisting of plant ingredients of Brahmi (Bacopa monniera), Yastimadhu (Glycyrrhiza glabra), Tagar (Valeriana wallechii) and Ashwagandha (Withania somnifera).The present study was undertaken to investigate the effects of L-33 on learning and memory in experimental animals. Elevated plus-maze (EPM) and passive avoidance paradigm were employed to test learning and memory. Scopolamine (1mg/kg i.p.) and diazepam (1mg/kg i.p.) were used as interoceptive (stimulus inside the body) behaviour model. Three doses (5, 10 and 15 ml/kg p.o.) of L-33 were administered for 7-14 successive days in separate groups of animals. Elevated plus-maze (EPM) and passive avoidance paradigm model results show that dose of 15 ml/kg of L-33 significantly improved learning and memory of mice. Furthermore, this dose significantly reversed the amnesia induced by diazepam (1mg/kg i.p.) and scopolamine (1mg/kg i.p.).Since scopolamine-induced amnesia was reversed by L-33, it is possible that the beneficial effect on learning and memory was due to facilitation of cholinergic-transmission in mouse brain, also diazepam which is a GABA mimetic agent induces memory impairment and the subsequent inhibition of diazepam induced amnesia by L-33 may be due to inhibition of GABA-B receptors has been found to facilitate learning and memory.
At present, it is contradictory to determine if the combination of certain prothrombotic polymorphisms and migraine and also the risk to develop ischaemic vascular disease. Recently, the common Val34Leu polymorphism of the A-chain factor XIII gene, associated with variations in factor XIII activity, has been suggested to play a significant role in the development of arterial and venous thrombotic disorders. Our study analysed the incidence of genetic polymorphism Factor XIII (V34L) in a sample of migraineurs and a control group of the patients with ischemic cardiopaty. In this study 70 consecutive patients aged 10-66 years (mean age 39.2 years), suffering from migraine [1] (58 migraine without aura, 12 migraine with aura, ICHD-II criteria) and 70 patients aged 36-71 years (mean age 45.8 years), with ischemic cardiopathy [2] were studied with Polymerase Chain Reaction (PCR) for genetic polymorphism Factor XIII (V34L). Factor XIII (V34L): 42 subjects (60%) [1] and 27 (38.5%) [2] were heterozygous; 2 subjects (3%) [1] and 2 (2.85%) [2] were mutated. These data evidenced that the incidence the factor XIII Leu 34 allele in two population studied not evidenced meaningful differences. Therefore a role in the pathogenesis of such disturbances is hypothetical and deserves ulterior deepenings in more important casuistries.
L-35 is a polyherbal formulation, consisting plant ingredients of Picrrorhiza kurroa (scrophulariaceae) and Tephrosia purpurea L. (Papilionaceae).The L-35 was investigated for in-vivo hepatoprotective effects. The ethanol was used as toxicant, and silymarin as standard drug. Different groups of wister albino rats were treated with alcohol (3.76gm/kg p.o., BD), silymarin (100mg/kg p.o., BD) and different dose level of L-35 (5 ml/kg, 10 ml/kg and 15ml/kg p.o., BD) for 25 days. The effects of treated groups on wet liver weight, wet liver volume, serum transaminase (SGOT, SGPT), alkaline phosphatase (ALP), bilirubin (Direct and Total), Total albumin and total protein were measured. L-35 at a dose of 15ml/kg shows significant (p < 0.01) hepatoprotective effect compare to that of toxicant group. Histopathological studies also reveal the normal hepatocytes with normal lobular architecture compared to that of toxicant group.
A series of 3-ethyl-2-substituted amino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 3-ethyl-2-hydrazino quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material 3-ethyl-2-hydrazino quinazolin-4(3H)-one was synthesized from ethylamine. The title compounds were investigated for analgesic, anti-inflammatory activities. The compound 2-(1-ethylpropylidene-hydrazino)- 3-ethyl-quinazolin-4(3H)-one (S2) emerged as the most active compound of the series and it is moderately more potent in its analgesic and anti-inflammatory activities when compared to the reference standard diclofenac sodium.
In present study some novel derivatives of 2-(N-substituted amino) methyl-3-(4-chlorophenyl)-quinazolin-4(3H)-ones have been synthesized by the condensation of respective 6, 8-disubstituted-2-chloromethyl-3-(4-chlorophenyl)-quinazolin-4-(3H) ones with different primary amines in equi molar concentrations. The structures of these compounds have been established on the basis of their spectral data. These compounds were tested for anti-inflammatory and antimicrobial potentials by carrageenan-induced rat paw oedema model and cup-plate method respectively, Compound 3-(4-chlorophenyl)-2-[(3-hydroxy phenyl amino)-methyl]-3h-quinazolin-4-one (QN03) showed comparable anti-inflammatory activity with the standard drug used and also showed good antibacterial activity. Other compounds exhibited mild to moderate antibacterial activity.
Quinazolinones are heterocyclic and water insoluble compounds with various pharmacological and biological characteristics (antibacterial, antiswelling, antifungal, parkinson and etc.). They are used for treatment HIV and cancer. This study investigated the effects of 4(3H) quinazlonones-2-ethyl-2-phenyl ethyl (QEPE) as a new quinazolinons compounds on the spleen and immunocompetent cells of newborn Balb/C mice. Pregnant mice were divided into 3 groups (n=10) of control, sham and experimental, received distilled water, methyl cellulose %0.05 (the solvent) and 100 mg/kg Balb/C body weight of QEPE (most effective dose), respectively, by IP injection, on days 8 th to 15 th of gestation Examinations indicated an increase in weight of spleen in experimental group. Pathological studies showed increase in capsule thickness and number of macrophage cells of experimental group. Statistical analysis showed significance differences in morphological studies between experimental, sham and control groups. The statistical data on capsule thickness and number of macrophage cells indicated significance differences between experimental, sham and control groups. Detailed observations showed increase in the volume of monocyte, neutrophile and eosinophile, in response to QEPE but the volume of lymphocyte and basophile were same in experimental, control and sham groups. The damages caused by this dose of QEPE could have been the reason for the increase in the number of immonucompetent and macrophage cells. Some studies showed damages to the organs such as livers and hearts would lead to the increase in the thickness of spleen capsule, consequently, increase in its weight and creation of splenomegaly. So, QEPE can not be an appropriate candidate for drugs development. Maybe QEPE in the lower dose can be an appropriate candidate for increase of immuno system resistance.
Water insoluble heterocyclic compounds such as quinazolinones have variety of biological and pharmacological properties. This study aim to investigate effects of 4(3H)-quinazolinone-2-propyl-2-phenylethyl (QPPE) as a new quinazolinone on spleen and immunocompetent cells of newborn Balb/C mice. Pregnant Balb/C mice were divided into 3 groups (n= 10) of control, receiving distilled water, sham, receiving 0.05% methyl cellulose (the solvent) and experimental group, receiving one of the most effective dose of 100 mg/kg/body weight of QPPE, by IP injections on day 8th to 15th of gestation. Blood samples from heart of newborn Balb/C mice were analyzed for immunocompetent cells and spleens were removed, fixed and stained with H&E, for qualitative and quantitative studies. Data indicated an increase in weight of spleen in experimental group. Pathological studies showed increase in capsule thickness and number of macrophage cells of experimental group. Statistical analysis showed significant differences in morphological studies between expimental, sham and control groups. The statistical data on capsule thickness and number of macrophage cells indicated significance difference between experimental, sham and control groups. Detailed observations showed increase in the volume of monocyte, neutrophile and eosinophile, in response to QPPE but the volume of lymphocyte and basophile were same in experimental, control and sham groups. The damages observed in the liver, intestine, kidney, heart, stomach and brain (in progress), could have been the reason for the increase in the number of immunocompetent and macrophage cells. Some studies showed damages to the organs such as liver and heart would lead to the increase in the thickness of spleen capsule, consequently, increase in its weight and creation of splenomegaly. So, QPPE can not be an appropriate candidate for drugs development.
Quinazolinones are used for treatments of prevalent diseases. They belong to hyponic and potent anticonvulsant drugs, Act strongly, inhibiting human immunodeficiency virus (HIV) and cancer, Enter circulatory system and pass through placenta barrier. In this study, for the first time different aspects of developmental effects of 4(3H) quinazolinone-2- propyl-2-phenyl ethyl (QPPE) on stomach and heart of Balb/C mice embryos were investigated. Pregnant Balb/C mice were divided into 3 groups (n= 10) of control, receiving distilled water, sham, receiving 0.05% methyl cellulose (the solvent) and experimental group, receiving one of the most effective dose of 100 mg/kg/body weight of QPPE, by IP injections on day 8th to 15th of gestation. After anesthetising mothers, stomachs and hearts of 5-day old newborn Balb/C mice were removed,fixed and stained with H & E for light microscopic and quatitative studies. Results showed symptoms of gastritis (hyperaemia and decrease in thickness of mucus layer) in newborn Balb/C mice of treated groups.QPPE also created necrotic cells and an increase in connective tissues of hearts of newborn mice of treated groups. In conclusion by being teratogens and toxins, these two new derivatives affected development of embryonic stomach and heart at histological level.
The present investigation is an attempt to determine the possible toxicity potentials of orally fed triphenyl tin complex [(C6H5)3Sn(Sal. Benz. H.)] in the reproductive system of male rats (Rattus norvegicus) at the dose level of 10mg/kg body weight and 20 mg/kg body weight for 60 days. Treated rats showed decline in the weight of reproductive organs in a dose-response fashion. The treatment also diminished the sperm motility and density highly significantly; the fertility percent was reduced to 95% at 20 mg dose level. Serum testosterone levels were also diminished significantly. Significant reduction was also found in the biochemical parameters such as cholesterol, glycogen, protein and sialic acid content of the reproductive tissues in a dose dependent manner. Investigations through hematology and serology showed no signs of clinical toxicity. Histological studies of the sections of testis of treated rats showed absence of spermatozoa in the lumen of seminiferous tubules along with highly reduced seminiferous tubular diameter and increased intertubular space in the treatment groups when compared to the control counterparts. These results indicate that the complex is antispermatogenic in nature and oral administration in male rats caused sterility i. e. reproductive toxicity. A comparison indicates that 20 mg/kg dose level was more effective pertaining to its antifertility than the corresponding dose level of 10 mg/kg dose level.
In this study, cytotoxic activity of Clerodendrum phlomidis crude extracts was investigated. Petroleum ether, chloroform, ethyl acetate and ethanol extracts prepared from roots of Clerodendrum phlomidis were tested for cytotoxic activity on Mouse embryonic fibroblasts cell line (NIH 3T3) and human cervical cancer cell line (HeLa) using MTT assay. The cells are tested at different concentrations to determine IC 50 (50% growth inhibition) by MTT assay. Chloroform extract shows moderate cytotoxic activity with an IC 50 value of 148.4 μg/ml on (NIH 3T3), while Pet ether and ethyl acetate have weak cytotoxic activity on (NIH 3T3). Ethanol extract has no cytotoxic effect on both NIH 3T3 and HeLa cell line. Ethyl acetate extract has moderate cytotoxic activity with an IC 50 166μg/ml on HeLa cell line, while pet ether and chloroform have weak cytotoxic activity on HeLa cell line.
The Emergency Division represents a strategic hospital headquarter to implement pharmacovigilance activities. The ease of access, the care availability of 24 hours to 24 and the patient's multidisciplinary approach make Emergency Division is the ideal access to health care. The data reported in this paper are from the year 2011 the project MEREAFaPS. It is clear that the presence of the hospital pharmacist in Emergency Division is an important resource for the spontaneous reporting system. A pharmacist infact, reports and supports physician to identify ADR/ADE in Emergency Division, increasing the number of ADR/ADE report forms. In addition, the professional role of hospital pharmacist is an useful tool to create an important network of hospital pharmacovigilance and to increase the number of ADR report forms, their quality and the awareness in safety pharmacology.
Tissue acidosis is an hallmark of inflammatory, ischemic and tumoral processes and although it remains uncertain whether there is a true cause-effect relation between acidosis and adverse clinical outcomes it remains a powerful marker of poor prognosisin critically ill patients. Dysregulation of host defence mechanisms and in particular of the immuno-inflammatory responses occurs during sepsis. Sepsis is always associated with acidosis conditions and is able to alter inflammatory mediators release and thus the immune response. Patients with severe sepsis and septic shock exhibit a complex metabolic pattern of acidosis at intensive care unit admission, caused predominantly by hyperchloremic acidosis, which was more pronounced in non survivors. In this study, conducted in vitro, we analyzed the effects of N-acetylcysteine (NAC), a molecule with antioxidant activity, during the inflammatory process, in acidosis conditions, in J774A.1 murine/macrophages stimulated with Lipopolysaccharide from E.coli (LPS). Our results show that NAC, in hyperchloremic acidosis conditions, reduces cyclooxygenase-2 (COX-2) and heat shock protein 70 (Hsp70) expression without significantly affecting changes in the constitutive isoform Heatshock protein 90β (Hsp90β) expression in LPS-treated macrophages. Our data report a reduced inflammatory response exerted by NAC in hyperchloremic acidosis conditions indicating that the use of NAC during inflammation further impairs immune response associated to acidosis associated disease, asseptic shock. © 2014, SILAE (Italo-Latin American Society of Ethnomedicine). All rights reserved.
In this research circadian variation of antinociceptive effect of adenosine and two A1 adenosine receptor agonists, (R) N6-phenylisopropyl adenosine (R-PIA) and 2-chloroadenosine (2-CAdo), and pain were studied in male mice that housed under control light phase for two weeks. Circadian variation of pain was performed on intact mice by using hot plate test. Doses of 40, 2 and 0.6 mg/kg of adenosine, 2-ClAdo and R-PIA, respectively were injected intraperitoneally to three separated groups of six male mice at six hour intervals (09:00, 15:00, 21:00, and 03:00). The control group received normal saline. The result of circadian rhythm of pain showed that the minimum nociceptive effect was observed in dark phase in mice and it was time dependent. The peak of antinociceptive effect of adenosine was in dark phase (21:00 P.M.) at 0.5 h after of injection. The results of 2-ClAdo indicated that maximum of antinociceptive effect was in dark phase and results of R-PIA exhibited that peak of antinociceptive activity was in light phase. This study indicated that the pattern of pain in male mice has circadian variation. The antinociceptive effect of adenosine and its two agonists was time dependent. This circadian variation in antinociceptive activity may be important in the administration of these agents.
Essential oil yields of Abaco bush medicines.
Antimicrobial activity (MIC, µg/mL) of leaf essential oils and their major components of Abaco bush medicinal plants.
Introduction: Four aromatic plants used in traditional "bush" medicine on Abaco Island, Bahamas were studied. Amyris elemifera (Rutaceae), "white torch", is taken as a febrifuge and applied to sores and wounds, to treat influenza, and as an external bath and general tonic. Eugenia axillaris (Myrtaceae), "white stopper", is used as an aphrodisiac, as well as to treat diarrhea and for bathing women after childbirth. Lantana involucrata (Verbenaceae), "wild sage", is used to treat itching of the skin, measles and chicken pox. Myrica cerifera (Myricaceae), "bayberry", is taken as a general tonic and diuretic. Methods: The leaf essential oils of the four aromatic plants were obtained by hydrodistillation and analyzed by GC-MS. The antimicrobial activity against Bacillus cereus, Pseudomonas aeruginosa, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, and Aspergillus niger, and the in-vitro cytotoxicity of the oils on MDA-MB-231, MCF7, Hs 578T, Hep G2, and PC-3 human tumor cells have also been examined. Results: The most abundant components of Amyris elemifera were limonene (45.0%) and linalool (20.8%). Eugenia axillaris leaf oil was largely composed of α-pinene (15.5%) and dihydroagarofuran (9.2%). The leaf oil of Lantana involucrata was made up largely of germacrene D (21.1%), α-humulene (15.2%), and β-caryophyllene (13.7%). The most abundant essential oil components of Myrica cerifera were 1,8-cineole (30.7%) and α-terpineol (14.2%). L. involucrata leaf oil showed slight antibacterial activity against B. cereus and Staph. aureus and was weakly cytotoxic against our panel of cell lines. Neither A. elemifera, E. axillaris, nor M. cerifera leaf oils were appreciably antimicrobial or cytotoxic. Conclusions: The reported biological activities of the major constituents of A. elemifera leaf oil are consistent with the ethnopharmacological uses of this plant. The major components in the leaf oil and slight antimicrobial activity are consistent with the ethnobotanical use of L. involucrata to treat itching skin.
The present study was aimed at investigating the effects of Abana, an Ayurvedic herbomineral preparation on memory in rats. Drug Abana was administered orally in three doses (50, 100 and 200 mg/kg) for fifteen days to different groups of young and aged rats. Elevated plus-maze and Hebb-Williams maze served as the exteroceptive behavioral models for testing memory. Diazepam-, scopolamine-and ageing-induced amnesia served as the interoceptive behavioral models. Abana (50, 100 and 200 mg/kg, p.o.) produced a dose-dependent improvement in memory scores of young and aged rats. Furthermore, it reversed the amnesia induced by scopolamine (0.4 mg/kg, i.p.) and diazepam (1 mg/kg, i.p.). It may prove to be a useful remedy for the management of Alzheimer's disease.
Abarema auriculata crude extract EB689 showed cytotoxic activity against prostate, central nervous system and head-and-neck cancers, and may be useful in veterinary and human care in the future. For the first time, the presence of steroids and phenolic compounds were related to A. auriculata. Spinasterol, a bioactive steroid, was isolated from the non polar fractions of EB689, and the phenolic compounds neoastilbin, astilbin, isoastilbin, neoisoastilbin and engeletin were isolated from polar fractions of EB689. Preliminary toxicological results showed that EB689 exhibited a non-lethal dose of 4.90 mg/kg and a LD50 of 15.0 mg/kg. Higher doses of EB689 IP administered influenced general activity of male mice, provoking significant alterations in sensory system functions, including corneal reflex and tail squeeze and touch responses. Effects were also observed in psychomotor system function, particularly in hindquarter fall, surface-righting reflex, grasp reflex and body tone and in the autonomic nervous system, where piloerection, defecation, hypothermia, cyanosis and breathing were influenced. Significant alterations were observed in general activity, cyanosis and breath after the administration of the non-lethal dose (4.90 mg/kg), corroborating the initial observations. Diminishment of general activity and breathing and appearance of cyanosis are possibly related to intestine hemorrhage observed in necropsy, which led to animal death. The occurrence of the isolated compounds in EB 689 is unlikely related to animal death and it is the first time they are isolated from Abarema auriculata.
Whole blood trough level (C 0) has been traditionally used for Cyclosporine (CsA) dosage adjustments. Absolute C 0 susceptible to extensive variability from toxicity to immunogenic response may not be a dependable guide for adjustment. Prospective studies in renal transplant suggest that CsA dosing based on Two Hour Peak (C 2) results in less rejection and better renal function that C 0 However, ideal TDM for CsA has yet to be defined. With the objective that large across-the-day variation of CsA bioavailability due to circadian and food effects observed even at average steady state, can be incorporated into meaningful monitoring by using a normalized-dose adjusted C 2 / C 0 algorithm accounting for both the drug absorption and elimination, this study using EMIT assay was conducted to assess C 2 /C 0 ratio as abbreviated PK model that could predict rejection and renal function status and help develop guidelines for better CsA TDM. Follow up patients (n=35: male 29, female 6) at varied post-renal transplant period (6 months to 11 years), age (18 to 85 years) and weight (60 to 78 Kg) receiving Cyclosporine 75-200mg daily in 12 hourly increments that were equal in 20 and unequal in 15 patients in which evening dose 83.9±21.2mg was significantly higher (p< 0.001) than morning dose 74.8±24.6mg. C 0 and C 2 at steady state were 194±74.6ng/ml and 1018.7±278.9ng/ml respectively. C 2 /C 2 was 5.6±1.9 with optimal renal function (Sr. creatinine 1.4±1.2mg/dl; Blood Urea 33.5±6.0mg/dl; Uric Acid 5.5±0.7mg/dl; systolic BP 131.8±8.9, diastolic BP 88.5±6.2mmHg and Hb 12.6±1.2g%). Other than direct correlation as expected with C 0 C 2 /C 0 ratio was independent of subjecdt and treatment variables. At 95% C.I. for projected population the C 2 /C 0 ratio was within 5.0 to 6.3. The ratio did not show any difference in spite of di?erent sets of C 0 and C 2 values. In conclusion, C 2 /C 0 may have the potential of an algorithm for monitoring safety and predict risk of cyclosporine immunosuppression following renal allograft.
Top-cited authors
Mohammad Ali Ebrahimzadeh
  • The School of Pharmacy
Hossein Hosseinzadeh
  • Mashhad University of Medical Sciences
M. Imran Qadir
  • Bahauddin Zakariya University
Karthik Loganathan
  • Salem microbes private limited
Bhaskar Rao
  • VIT University