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We have developed an effortless and extremely efficient procedure for the synthesis of quinazolin-4-one derivatives via palladium-catalyzed C-Ccoupling of aryl amide with isocyanides. The reactions are operationally simple and avoid using toxic carbon monoxide and acid chloride, which must be used in an anhydrous system. The structure of the novel compounds was confirmed based on spectral data. We also demonstrated the biological potential of these compounds as novel Antifungal Activity. Based on the MIC results, the most active is 3g.

Simple, precise accurate, novel and safe UV-Spectrophotometric simultaneous equation method developed for the simultaneous estimation of poorly water-soluble drugs Empagliflozin (EMPA) and Linagliptin (LINA) in tablet dosage form using 2M ammonium acetate: 2M sodium citrate and (50:50% W/W) as mixed hydrotropic solution and validated as per ICH guidelines. This Method involves solving of simultaneous equations based on measurement of absorbance at two wavelengths 270 nm and 294 nm (λmax of EMPA and LINA) in hydrotropic solutions. Ammonium acetate and sodium citrate solution did not show any absorbance above 240 nm and thus no interference in the estimation of drugs was seen. EMPA and LINA follow Beers law in the concentration range of 10-50mg/ml and 5-25mg/ml (r2 = 0.999). % Recovery for both the drugs was in the range of 98.50 to99.23 % indicating excellent accuracy. The methods were precise, with a relative standard deviation of less than 2% for both drugs. The developed methods were validated according to ICH guidelines and values of accuracy, precision and other statistical analysis were found to be in good accordance with the prescribed values. Thus, method can be used for routine monitoring of drugs in industry for the assay of bulk drugs and commercial formulation.

Pyrimidobenzothiazoles and its derivatives are important structural scaffolds in the field of synthetic organic chemistry and medicinal chemistry. The review is focused on one pot multicomponent approaches for generating pyrimidobenzothiazoles and its derivatives along with their interesting biological profile over the last ten years. Several eco-benign and cost effective approaches such as nano catalyst, ionic liquid, metal, solid acid, catalyst free, solvent free, etc. for its synthesis have been discussed in this review. Different synthetic strategies of pyrimidobenzothiazole derivatives have been compiled and discussed using 2-aminobenzothiazole, 1,3 diketones, substituted aldehydes, alkynoic acid, bis-methyl thiomethylene malononitrile, Baylis Hillman acetates, etc.

Background and Aims: Ultrasound-guided Transversus Abdominal Plane (TAP) block is an effective and safe regional anaesthesia technique. Our study is aimed to draw a comparison between the analgesic efficacy of Ropivacaine and Bupivacaine using ultrasound-guided TAP block. Materials and Methods: After approval from our Institutional Ethical Committee, 100 ASA I and II patients were recruited. Patients of either sex in age group of 18–65 years, undergoing elective lower abdominal surgeries were included in this prospective double-blind study. Patients were randomized into two groups, A and B. Group A (n=50) patients received ultrasound-guided TAP block with 20 ml 0.5% Ropivacaine and those in group B (n =50) received 20 ml 0.25% Bupivacaine at the end of surgery. The postoperative pain score (Numeric Rating Scale, NRS), patient satisfaction score, total requirement of analgesics in the first 24 hours, and the side effects were observed. Statistical tests were conducted using student’s t-test, chi-square test, or fisher’s exact test whichever was applicable. P Results: Statistically significant difference in the pain scores were observed between the two groups at different time intervals. The mean NRS score was higher for group B at 2nd, 4th, 6th and 14th hour following the block. The duration of analgesia was longer and the total requirement of analgesic was lesser in group A as compared to group B.(p Conclusion: Ultrasound-guided TAP block with 0.5% Ropivacaine provides effective analgesia for longer duration and decreases the total analgesic consumption as compared to 0.25% Bupivacaine in lower abdominal surgeries. Keywords: Bupivacaine, Ropivacaine, Ultrasound-guided transverse, abdominis plane block.

This study aims to compare the hemodynamic response of two commonly used induction agents Propofol and Etomidate in patients with left ventricular ejection fraction ≤40% undergoing Coronary Artery Bypass Grafting surgery. To compare the effects of Propofol and Etomidate on hemodynamics in terms of heart rate, rhythm, blood pressure, and central venous pressure. Narayana Multispeciality Hospital, Jaipur. Prospective, double-blinded, randomized, hospital based study.100 patients with LVEF≤40% scheduled for elective CABG, were randomly assigned to one of the two groups receiving either of the inducing agents, group A (PROPOFOL 2mg/kg) and group B (ETOMIDATE 0.2mg/kg). Unpaired t-test and Chi square test/Fisher exact test, p HR, SBP, DBP and MAP decreased from post induction 1 min. to post induction 3 min. (fall greater in propofol, p>0.005) then increased from post intubation 1 min. to post intubation 5 min. in both the groups (rise greater in etomidate group, p Etomidate is superior to propofol in providing hemodynamic stability before and after laryngoscopy and intubation, but less effective in controlling the pressor response to intubation. Therefore, Etomidate can be used as an induction agent with suitable adjuvants to control pressor response to tracheal intubation in patients undergoing CABG with low LVEF.

Ibutilideis less frequently used drug for atrial fibrillation (AF) in postoperative coronary artery bypass grafting (CABG) patients as compare to amiodarone. We therefore investigated the comparative efficacy of ibutilde and amiodarone for cardioversion in atrial fibrillation after CABG.To compare the efficacy of ibutilide and amiodarone for cardioversion of AF in post CABG patients. Narayana Multispeciality Hospital, Jaipur. Single center, randomized, double blind, comparative prospective study.Total 80 post CABG patients who developed AF were divided into two groups (Group A) Ibutilde and (Group B) Amiodarone respectively. The cardioversion time and cardioversion rate were measured. Unpaired t-test, Paired t-test, Chi square test / Fisher exact test. P value The cardioversion rate at 4hrs in group A was 42.5% and in group B was 50% (p value > 0.001). At 24 hrs cardioversion rate in group A was 95% and in group B was 87.5% (p value > 0.001). The mean time of conversion to sinus rhythm in group A was 382.85 minutes and in group B was 492.30 minutes. (p value= 0.235)Ibutilide was as effective as amiodarone for restoration of sinus rhythm in postoperative coronary bypass grafting patients who developed atrial fibrillation in their postoperative intensive care unit stay. Ibutilide may be superior to amiodarone in terms of hemodynamics and systemic side effects.

Ultrasound guided transversus abdominis plane block is an efficacious abdominal field block. The aim was to determine the effect of adding dexamethasone to 0.375% ropivacaine on the analgesic duration of TAP block in patients undergoing lower abdominal surgeries. A double blinded randomised control study conducted on 60 patients, 30 in each group. Group A: 0.375% ropivacaine (19 ml) with dexamethasone 4mg (1 ml) total 20ml each side. Group B: 0.375% ropivacaine (19 ml) with normal saline (1 ml) total 20ml each side in TAP block after lower abdominal surgery. Primary objective, to compare the duration of postoperative analgesia provided by the block and secondary objectives to compare the total amount of rescue analgesia required in first 24 h postoperatively and any side effect of ropivacaine in TAP block. Numeric rating scale scores used to assess pain between the two groups. Ethical committee approval was obtained.Duration of analgesia was significantly longer in group A with time of first analgesia need (12.44 ± 1.60 h) compared to group B (10.69 ± 1.79 h), P Addition of dexamethasone to ropivacaine in TAP block significantly prolongs the duration of postoperative analgesia.

Dexmedetomidine a novel αagonist is replacing the conventional sedative agents. Monitored Anesthesia Care has a gained lot of popularity in local surgery and high risk procedures. There is no dictum on use of standard fix maintenance dose of dexmedetomidine. The main objective and aim of our study was to find a better maintenance dose of Dexmedetomidine after a fixed loading dose with stable hemodynamic, good satisfaction scores, minimal side effects and less rescue drug consumption. After ethical committee approval our randomized, prospective double blinded study a total 70 patients ASA I-III aged 18-65 years divided into two groups: both groups received a loading dose of 1 µg /kg over 10 minutes followed by group A receiving 0.2 µg/kg/hr and group B receiving 0.4 µ/kg/hr till end of surgery. Patient and surgeon satisfaction evaluated by Likert scale and sedation by Ramsay sedation score and vital parameters recorded. The results were comparable in terms of mean blood pressure, heart rate, SpO, respiratory rate, pain scores and demographic data. Surgeon satisfaction was higher in group B with statistical significance(pDexmedetomidine maintenance of 0.4 µg/kg/hr is equally safe and effective compared to 0.2 µg/kg/hr but former has better surgeon satisfaction with quicker achievable target sedation. Thus Dexmedetomidine 0.4 µg/kg/hr has a better edge for maintenance.

1% 2-Chloroprocaine could have been an ideal local anaesthetic for ambulatory procedures but it has been neglected in past years and even after re introduction with its preservative and antioxidant free form. To compare the anaesthetic effect of intrathecal 2-Chloroprocaine with or without fentanyl in patients undergoing short duration lower abdominal and lower limb surgeries regarding hemodynamic parameters, mean duration of block, time to ambulation and side effects.Anesthesia Department at Narayana Multispeciality Hospital, Jaipur.Randomised, Comparative, Single Centre StudyA total of 120 patients,18-70 years, weight>50 kg and ASA grade I- II underwent elective lower abdominal and lower limb surgeries with expected duration Chi-Square and Unpaired Student T- Test (p Spinal anesthesia was successful for all patients. Onset time of sensory and motor block, time to achieve peak block height and complete motor block was statistically insignificant (p 2-Chloroprocaine spinal anesthesia provides rapid onset, giving it a promising profile for ambulatory surgery. Addition of fentanyl lengthens regression to S2 and with minimal increase of motor block duration.

Background: Cancer has emerged as a major health problem globally as a consequence to the increased longevity of the population, changing the environment and life style. Chemoprevention is a new and promising strategy for reducing cancer burden. Recently, some natural products have been identified for their chemopreventive activity to reduce the cancer incidence. Ginseng is known for its potential to treat various ailments in human beings. The present study was designed to explore the anticancer and antioxidative potential of Panax ginseng against chemical-induced skin carcinogenesis in mammals. Methods: Skin tumors were induced in Swiss albino mice by a single topical application of 7,12-dimethylbenz(a)anthracene (100 μg/100 μL acetone) and, 2 wks later, promoted by repeated applications of croton oil (thrice in a wk in 1% acetone) till the end of the experiment (i.e., 16 wk). Hydroalcoholic ginseng root extract at a dose of 25 mg/kg body weight/d was orally administered at the peri-initiation, postinitiation, and peri–post-initiation stages. Results: Ginseng root extract treatment caused a significant reduction in tumor incidence, cumulative number of tumors, tumor yield, and tumor burden, as compared to the 7,12-dimethylbenz(a)anthracene–croton oil-treated control group. Further, biochemical assays revealed a significant enhancement in the levels of reduced glutathione, superoxide dismutase, catalase, vitamin C, and total proteins but a significant reduction in lipid peroxidation levels in both the liver and skin with ginseng root extract treatment, as compared to carcinogen-treated control group. Conclusion: These results suggest that P. ginseng has the potential to become a pivotal chemopreventive agent that can reduce cancer in mammals.

Background Reproductive dysfunctions induced by various environmental toxicants are the prime concern in the today's changing global scenario. Living systems are constantly exposed to ionizing radiation that cause cellular as well as genetic alterations leading to mutations and cell death. To evaluate the deleterious effects of low dose of gamma radiation on testicular tissue and their possible inhibition by Tinospora cordifolia root extract (TCE). Methods One group of Swiss albino mice was exposed to 2.5 Gy gamma radiation to serve as the irradiated control, while the other group received TCE (75 mg/kg b. wt./day) orally for 5 consecutive days half an hour before irradiation to serve as experimental. Results Irradiated animals experienced more severe testicular histopathological lesions and a considerable depletion in different spermatogenic cell counts as compared to that of normal animal. Furthermore, TCE pretreatment effectively prevented radiation-induced alterations in body weight, tissue weight, weight index, tubular diameters and anti oxidative parameter viz. lipid peroxidation, glutathione and catalase activity in testes and restored almost a normal structure of testes. Conclusion T. cordifolia root extract can be potentially used as an effective radio-protector against radiation induced testicular injuries in mammals.

The present study was designed to evaluate the effect of green tea catechin (7500 µg/kg/animal/day) against cadmium-induced testicular dysfunctions and oxidative stress in the testes of mice. For this purpose, Swiss albino mice were divided into six groups: group I, negative control; group II, catechin-treated control; group III, cadmium chloride (CdCl2)-treated control; group IV, experimental group I; group V, experimental group II; and group VI, experimental group III. Animals from all of these groups were necropsied at various post-treatment intervals between 12 hours and 30 days for various biochemical alterations in the testes. CdCl2 intoxication resulted in a significant decline in testicular total proteins, cholesterol, and alkaline phosphatase, whereas acid phosphatase and lipid peroxidation exhibited a noticeable augmentation as compared to negative control. Catechin treatment effectively protected CdCl2-induced alterations in all such parameters throughout the experiment. Catechin was effective in reducing the CdCl2-induced augmentation of phase I (P450 and CYPB5) as well as phase II (DT-diaphorase and glutathione-S-transferase) enzymes in testes. Furthermore, CdCl2 intoxication was found to attenuate the antioxidant potential of testes, which was however augmented when supplemented with green tea extract. Compared to CdCl2-treated control mice, superoxide dismutase, glutathione peroxidase, glutathione, and catalase levels were significantly decreased in testes. Indeed, green tea catechin significantly increased testicular antioxidant enzymatic activities compared to those given CdCl2 alone. In conclusion, the use of green tea extract appeared to be beneficial to a great extent in inhibiting and restoring the testicular injuries induced by CdCl2 intoxication in mammals.

Chemoprevention is a novel approach to study the anti-initiating and anti-tumor-promoting efficacy of medicinal plants and their active principles. The present study investigated the chemopreventive potential of Aegle marmelos fruit extract in 7,12-dimethylbenz[a]anthracene-induced skin carcinogenesis and its influence on oxidative stress and the antioxidant defense system. The oral administration of A marmelos at 100 mg/kg body weight/day during peri-initiational, postinitiational, and peri- & postinitiational phases of papillomagenesis showed significant reduction in tumor incidence, tumor yield, tumor burden, and cumulative number of papillomas when compared with carcinogen-treated control. The average latent period significantly increased (7.88 weeks; control group) to 9.45, 11.11, and 11.54 weeks in different A marmelos extract (AME) experimental groups. Enzyme analysis of skin and liver showed a significant elevation in antioxidant parameters such as superoxide dismutase, catalase, glutathione, and vitamin C in AME-treated groups when compared with the carcinogen-treated control. The elevated level of lipid peroxidation in the positive control was significantly inhibited by AME administration. These results indicate that AME has the potential to reduce chemical-induced skin papillomas by enhancing the antioxidant defense system.

Human populations are increasingly exposed to various carcinogens such as chemicals, radiation, and viruses in the environment. Chemopreventive drugs of plant origin are a promising strategy for cancer control because they are generally nontoxic or less toxic than synthetic che-mopreventive agents, and can be effective at different stages of carcinogenesis. The present investigation was undertaken to explore the antitumor activity of topical treatment with aloe vera (Aloe vera) gel, oral treatment with aloe vera extract, and topical and oral treatment with both gel and extract in stage-2 skin carcinogenesis in Swiss albino mice induced by 7,12-dim ethylbenz(a)anthracene (DMBA) and promoted croton (Croton tiglium) oil. The animals were randomly divided into 4 groups and treated as follows: Group I, DMBA + croton oil only (controls); Group II, DMBA + croton oil + topical aloe vera gel; Group III, DMBA + croton oil + oral aloe vera extract; Group I V, DMBA + croton oil + topical aloe vera gel + oral aloe vera extract. Results showed that body weight was significantly increased from 78.6% in the control group (Group I) to 92.5%, 87.5%, and 90.0% in Groups II, III, and I V, respectively. A 100% incidence of tumor development was noted in Group I, which was decreased to 50%, 60%, and 40% in Groups II, III, and I V, respectively. Also in Groups II, III, and IV, the cumulative number of papillomas was reduced significantly from 36 to 12, 15, and 11; tumor yield from 3.6 to 1.2, 1.5, and 1.1; and tumor burden from 3.6 to 2.4, 2.50, and 2.75, respectively, after treatment with aloe vera. Conversely, the average latent period increased significantly from 4.9 (Group I) to 5.23, 5.0, and 6.01 weeks in Groups II, III, and I V, respectively. We conclude that aloe vera protects mice against DMBA/croton oil-induced skin papillomagenesis, likely due to the chemopreventive activity of high concentrations of antioxidants such as vitamins A, C, and E; glutathione peroxidase; several isozymes of superoxide dismutase; the minerals selenium and zinc; and polysaccharides in aloe vera.

The skin, being a cell-renewal system, is one of the first organs to be affected in total-body irradiation during radiotherapy. An attempt has been made in the present study to explore radiation-induced biochemical alterations caused by whole-body gamma irradiation and their modulation in Swiss albino mice by Aloe vera leaf extract (AVE). Mice were selected for this study from an inbreed colony and divided into four different groups: I (double-distilled water-treated group): considered as normal; II (Aloe vera-treated group): the animals were administered 1 g/kg body-wt/day Aloe vera leaf extract; III (radiation-treated group): the animals were exposed to 6 Gy gamma radiation at the dose rate of 0.96 Gy/min; and IV (combination group): animals were administered Aloe vera leaf extract continuously for 15 consecutive days, and on the 15th day they were irradiated to 6 Gy gamma radiation after 30 minutes of extract administration. The animals from the above groups were autopsied after 6 hours, 24 hours, and at 3, 7, 14, and 21 days of radiation. Biochemical estimations of DNA, lipid peroxidation, glutathione, catalase, and superoxide-dismutase were made. Total DNA, catalase, superoxide dismutase (SOD) activity in the skin, and glutathione (GSH) in the liver and blood significantly decreased compared to normal, but lipid peroxidation (LPO) in the liver and blood increased in the irradiated control group. In contrast, in experimental animals, DNA, catalase, and SOD in the skin and GSH in the liver and blood increased significantly, whereas LPO in the liver and blood decreased in comparison to irradiated control animals. Thus, Aloe vera leaf extract is found to have damage-resistant properties against radiation-induced biochemical alterations in Swiss albino mice.

The radioprotective efficacy of a hydro-alcoholic extracted material from the bark of Alstonia scholaris (ASE) was studied in mice against radiation-induced hematological and biochemical alterations. Swiss albino mice were administered ASE (100 mg/kg body weight/d for 5 consecutive day) orally prior to whole-body gamma irradiation (7.5 Gy). Radiation exposure resulted in a significant decline ( P < .001) in erythrocytes and hemoglobin until the third day, following a gradual recovery (ie, day 7), but these values did not reach normal values during the remainder of the animals' life span. Hematocrit percentage declined significantly ( P < .001) until day 15. In contrast, ASE-pretreated irradiated animals had significantly higher erythrocyte, hematocrit, and hemoglobin values than the irradiated controls. Furthermore, a significant elevation in lipid peroxidation level over normal was recorded in gamma-irradiated mice, whereas this increase was considerably lower in ASE-pretreated animals. Pretreatment with ASE caused a significant increase in glutathione levels in serum as well as in liver in comparison to irradiated animals. This study showed that ASE protects against radiation-induced hematological and biochemical alterations in Swiss albino mice.

Tinospora cordifolia (Guduchi), an Indian medicinal plant, was used to explore antitumor promoting activity in a two-stage skin carcinogenesis model. For this purpose, mice were treated by single application of DMBA (100 microg/100 microl of acetone) and two weeks later promoted by croton oil (1% in acetone three times a week) until the end of the experiment (i.e., 16 weeks). Oral administration of the above extract at the preinitiational stage (i.e., seven days before and seven days after DMBA application; group IV), promotional stage (i.e., from the time of croton oil application; group V), and both pre- and postintiational stage (i.e., from the time of DMBA application and continued until the end of the experiment; group VI; on the shaven backs of the mice at the dose of 100 mg/kg body weight/day for 16 weeks) recorded significant reduction in tumor weight, tumor incidence in comparison to control (i.e., mice treated with DMBA and croton oil; group III). Furthermore, cumulative number of papillomas, tumor yield, tumor burden, and tumor weight showed significant reduction along with significant elevation of phase II detoxifying enzymes, and inhibition of lipid peroxidation in liver and skin in the animals administered with such plant extract concomitant to carcinogen exposure. Thus, the present data strongly suggests that the Tinospora cordifolia extract has anti-tumor potential in a two-stage skin carcinogenesis mouse model.

The present investigation was undertaken to explore the antitumor-promoting activity of Aloe vera on 2-stage skin carcinogenesis, induced by a single topical application of 7,12-dimethylbenz(a)anthracene and promoted by treatment of croton oil for 16 weeks in Swiss albino mice. Oral administration of aloe leaf extract at a dose of 1000 mg/kg body weight/d and aloe gel treatment at a dose of 1 mL/ 9 cm2/mice/d was found to be effective in decreasing the number and size of the papillomas. A significant reduction in tumor incidence (40.00 ± 5.10, 30.00 ± 3.25, and 40.00 ± 4.12 for aloe gel, aloe gel and aloe leaf extract combined, and aloe leaf extract alone, respectively) was observed in animals in the aloe extract— and aloe gel—treated groups compared with 100% tumor incidence in the control group. The cumulative number of papillomas during an observation period of 16 weeks was significantly reduced in the aloe-treated groups (8.0 ± 0.34, 6.00 ± 1.10, and 9.00 ± 1.41 for aloe gel, aloe gel and leaf extract, and aloe leaf extract, respectively) compared with a 36 ± 0.98 cumulative number of papillomas in the control group. The average latent period was significantly increased from 4.9 ± 0.10 weeks in the control group to 6.37 ± 0.12, 6.8 ± 0.25, and 6.2 ± 0.21 weeks in the aloe-treated groups, respectively. The tumor burden and tumor yield were significantly decreased (2.0 ± 0.25, 2.00 ± 0.30, and 2.25 ± 0.2 and 0.8 ± 0.25, 0.6 ± 0.32, and 0.9 ± 0.28, respectively) as compared with the 7,12-dimethylbenz(a)anthracene—treated control group (3.6 ± 0.10 and 3.6 ± 0.19). Furthermore, treatment with aloe gel and/or extract by topical and/or oral administration resulted in a significant increase in the reduced glutathione ( P < .05), DNA ( P < .001), catalase ( P < .05), and protein ( P < .001) in the skin of mice. Conversely, lipid peroxidation levels were significantly decreased ( P < .001) in the skin of mice.

This study assessed the chemopreventive potential of the Aegle marmelos plant on mouse skin tumorigenesis initiated by 7,12-dimethylbenz(a)anthracene (DMBA) and promoted by croton oil. A significant reduction in tumor incidence, tumor burden, tumor multiplicity, and the cumulative number of papillomas, along with a significant increase in the average latent period, was recorded in mice treated orally with A. marmelos extract (AME) at peri - and post-initiation phases (i.e., 7 days before DMBA application and continued until the end of the experiment) of papillomagenesis as compared with the carcinogen-treated controls. Furthermore, a significant increase in catalase activity, reduced glutathione and total proteins, and a depleted level of lipid peroxidation were observed in liver and skin of AME-treated animals as compared with the carcinogen-treated controls. Thus, the oral administration of AME, at a dose of 50 mg/kg body wt per day per animal, was found to be significantly effective in reducing skin tumors against chemical carcinogenesis in mice.

The present study evaluates the modulatory potential of Phyllanthus niruri on chemically induced skin carcinogenesis, and its influence on oxidative stress and the antioxidant defense system. Oral administration of P. niruri extract (PNE), during peri- (Gr. III), post- (Gr. IV), or peri- and post- (Gr. V) initiational stages of 7,12-dimethylbenz(a) anthracene (DMBA)-croton oil–induced papillomagenesis considerably reduced tumor burden to 4.20, 4.00, and 3.33(positive control value 6.20); cumulative number of papillomas to 21, 16, and 10, respectively, (positive control value 62); and incidence of mice bearing papillomas to 50, 40, and 30%, respectively (positive control value 100%), but significantly increased the average latent period to 10.14, 10.62, and 11.60, and inhibition of tumor multiplicity to 66, 74,and 83%, respectively. Enzyme analysis of skin and liver showed a significant (p ≤ 0.05, ≤ 0.01, ≤ 0.001) elevation in antioxidant parameters such as superoxide dismutase, catalase, glutathione, and vitamin C in PNE-treated groups (Gr. III–V) when compared with the carcinogen-treated control (Gr. II). The elevated level of lipid peroxidation in the carcinogen-treated positive control group was significantly (p ≤ 0.05, ≤ 0.01, ≤ 0.001) inhibited by PNE administration. These results indicate that P. niruri extract has potentiality to reduce skin papillomas by enhancing antioxidant defense system.

The radioprotective effect of Rosemarinus officinalis extract (ROE) was studied in mice exposed to 3 Gy gamma radiation. Crypt survival, villus length, apoptotic cells, mitotic figures and goblet cells in intestine were studied at different autopsy intervals i.e. 12 hrs to 30 days after irradiation. Maximum changes in all the intestinal parameters were observed on day 3 after irradiation. Irradiated animals with ROE pretreatment exhibited a significant increase in the number of crypt cells, mitotic figures and villus length; whereas a significant decrease in the counts of apoptotic and goblet cells showed a significant decrease respective controls at all the autopsy intervals. Irradiation of animals resulted an elevation in lipid peroxidation and a reduction in glutathione concentration in the intestine at 1 hour post-irradiation. In contrast, ROE treatment before irradiation caused a significant depletion in lipid peroxidation and elevation in glutathione levels.

Chemical radiation protection is an important strategy to protect living beings against the deleterious effects of radiation. In the present study, the radioprotective effect of hydro-alcoholic extract of Panax ginseng extract (PGR-HAE) was studied on radiation-induced deleterious alterations in Swiss albino mice. Oral administration of such extract (25 mg/kg b wt/day/animal) for 5 consecutive days, half an h. before whole-body exposure to 6 Gy gamma radiation, enhanced the 30 days survival and also inhibited the radiogenic sickness, weight loss and life shortening. PGR-HAE ameliorated radiation induced depletion in blood constituents at different necropsy intervals between 12 h to 30 d, and significantly increased the number of femoral spleen colony forming units that survived after irradiation. Furthermore, it checked depletion of glutathione and antioxidant enzymes (superoxide dismutase, catalase, and glutathione S-transferase) as well as elevation of lipid peroxidation (LPO) level in blood and liver. The significant reduction in the yield of LPO demonstrates that PGR-HAE protects the membranes against radiation-induced oxidative damage. These findings conclude that such plant extract provides significant radioprotection, and it may be potentially valuable in the prevention of injuries caused during planned and unplanned radiation exposure.

Alstonia scholaris, commonly known as sapthaparna, has been used for centuries in Ayurvedic medicine for treatment of various disorders. The objective of this study was to investigate the possible chemopreventive and anti-oxidative properties of this medicinal plant on two-stage process of skin carcinogenesis induced by a single application of 7, 12-dimethyabenz(a)anthrecene (100 lg/100 ll acetone), and two weeks later, promoted by repeated application of croton oil (1% in acetone/thrice a week) till the end of the experiment (16 weeks) in Swiss albino mice.The tumor incidence, tumor yield, tumor burden and cumulative number of papillomas were found to be higher in the carcinogen treated control (without ASE treatment) as compared to experimental animals (ASE treated). Furthermore, a significant increase in reduced glutathione, superoxide dismutase and catalase but decrease in lipid peroxidation was measured in ASE administered experimental groups than the carcinogen treated control. The present study demonstrates the chemopreventive potential of Alstonia scholaris bark extract in DMBA-induced skin tumorigenesis in Swiss albino mice.

Protective efficacy of diltiazem (a calcium channel blocker) has been studied against cadmium chloride (CdCl2) induced hematological and biochemical alterations in Swiss albino mice. CdCl2 (5 mg/kg b.wt.; i.p.) with or without prior treatment of diltiazem (100 mg/kg b. wt.; i.p.) was given to six-week old mice. Significant increase in the number of bone marrow cells as well as hematological parameters was observed in diltiazem pretreated CdCl2 intoxicated animals. A significant increase in lipid peroxidation (LPO) and acid phosphatase (ACP) level, and decrease in glutathione (GSH) and alkaline phosphatase (ALP) level in blood as well as liver were measured in CdCl2 intoxicated mice, while such values were near normal in DTZ pretreated animals. Furthermore, a significant increase in erythropoeitin (EPO) level was observed in diltiazem (DTZ) pretreated CdCl2 intoxicated animals as compared to CdCl2 alone treated animals. Thus, Diltiazem administration before cadmium intoxication protects bone marrow and hematological constituents in mice.

The radioprotective effect of Rosemarinus officinalis extract (ROE) was studied in mice exposed to 8 Gy of gamma radiation. The optimum dose for radioprotection was determined by administering 100, 200, 400, 800, 1000, 1500, and 2000 mg/kg body weight of ROE orally once daily, consecutively for five days before irradiation. Treatment of mice with ROE, delayed the onset of mortality and reduced the symptoms of radiation sickness when compared with the non-drug-treated irradiated controls. The dose of ROE found to be most effective against radiation was 1000 mg/kg body weight because this dose increased the survival time and reduced the mortality rate of mice significantly. Body weight loss in ROE administered irradiated animals was significantly less in comparison with animals who were given radiation treatment alone. Furthermore, irradiation of animals resulted in an elevation in lipid peroxidation (LPx) and a significant decrease in glutathione (GSH) in blood and liver. Conversely, administration of animals with ROE before irradiation caused a significant decline in LPx accompanied by a significant increase in GSH concentration. The present study demonstrates that Rosemarinus officinalis leave extract is a good radioprotector.

A124 Radiomodulation by rosemary extract Dhanraj Soyal, Abhilasha Sharma, Inder Singh and P.K.Goyal+ Radiation and Cancer Biology Laboratory, Department of Zoology, Rajasthan University, Jaipur 302004 * E-mail; pkgoyal2002@rediffmail.com Rosemary (Rosmarinus officinalis, Labiateae) is widely used for its antioxidant activities in many parts of the world. The present study investigates the radioprotective and antioxidative potential of rosemary leaves extract (ROE). Swiss albino mice were administered ROE orally once daily for 5 consecutive days, then exposed to a single dose of 3, 6 and 9 Gy of gamma radiation. lipid peroxidation (LPx), Glutathione (GSH), acid phosphatase estimations in liver were carried out. Radiation-induced increases in the levels of lipid peroxidation (LPO) and acid phosphatase were significantly ameliorated by ROE pre-treatment, and radiation-induced depletion in the level of glutathione (GSH) was significantly inhibited by ROE administration. These alterations were found to be dose dependent. The life-span was increased in the ROE treated irradiated mice in comparison with their respective control mice. Radiation-induced deficits in body and organ weight were significantly reduced or prevented in ROE pretreated mice. The protection afforded by ROE may be attributed to the constituents of the rosemary, which include rosmarinic acid, rosmanol, carnosol which appear to play an important role in free radical scavenging and singlet oxygen quenching. The study does not rule out the possibility of a prophylactic potential of ROE against radiation-induced degenerative changes in liver. Citation Information: Cancer Prev Res 2008;1(7 Suppl):A124.