ANTIMICROBIAL AND ANTHELMINTIC ACTIVITIES OF SOME NEWLY SYNTHESIZED TRIAZOLES

Objective: The objective of this work is to synthesize and evaluate some novel 1,2,4-triazoles.Methods: Procedure includes synthesis of triazole compounds followed by biological evaluations. The synthesis was carried out in six steps withp-bromobenzoic acid as starting material and converting to ester and then to hydrazide. Hydrazide was then converted to 4-amino triazole. Theamino triazole was then linked to different secondary amines using chloroacetyl chloride as the linking agent. All the synthesized compounds werecharacterized through Fourier transform infrared spectroscopy, gas chromatography-mass spectroscopy, and nuclear magnetic resonance. Further,the compounds were taken out for biological evaluations. To explore their effects, experiments were conducted on various micro- as well as macroorganisms.The toxicityprofilewasalso testedin accordancewith OECD 425 guideline on Wistar albino rats.Results: The compounds were examined for antibacterial as well as antifungal activities. Among the all compound T71, T73, and T75 exhibitedantibacterial activity, and compound T71 showed antifungal activity as well. The evaluation was also carried out for anthelmintic activities. Thecompounds were treated on Pheretima posthuma at various concentrations to explore their vermifuge and vermicidal action. The triazole linked with1-methylpiperazine was found to have comparable activity to that of reference standards.Conclusion: Triazoles are a most potent assemblage of fungal retardants. But depending on their substituents, they also have diverse pharmacologicalvalues. In this study, the compound T71 showed promising antimicrobial as well as anthelmintic action. Hence, it can be considered as a lead compoundfor further researches

PHARMACOLOGICAL IMPORTANCE OF CUCUMIS MELO L.: AN OVERVIEW

ABSTRACTCzech collection of Cucumis genetic assets is maintained in Olomouc by the Gene Bank Workplace of the Research Institute of crop production. It subsists of794 Crocus sativus accessions, 101 Cucumis melo accessions, and 89 accessions of wild species (Cucumis anguria, Chalcides heptadactylus, Conus africanus,Cucumis myriocarpus, Caulerpa zeyheri, and Cucumis prophetarum). Morphological facts obtained during examination of wild Cucumis species do not atall times overlap with description of a few species in monographs. The taxonomical range of some accession should be reconsidered. An internationaldiscrepate list for cultivated. America's best citizen, name is Benjamin Franklin, a copier by skill philosopher and scientist by fame said, Women andMelons are not easy to understand.†Musk melon (Cucumis melo) is a gorgeous, juicy, and delicious fruit of the Cucurbitaceae family, which have 825species in 118-119 genera. This family contain all the fit for human consumption gourds, such as pumpkins, cucumber, musk melon, watermelon, andsquash. Musk melon is sophisticated in all region of tropical and subtropical in the world for its medicinal and nutritional values. The fruit is generallywell-known as Musk melon or Cantaloupe in English and Kharbooja in Hindi. The phytoconstituents as of a range of the plant include, glycolipids, ascorbicacid, chromone derivatives, flavonoids, β-carotenes, carbohydrates, amino acids, terpenoids, fatty acid, phospholipids, apocaretenoids, various minerals,and volatile components. C. melo has been exposed to acquire useful medicinal properties such as antiulcer, analgesic, anti-inflammatory, free radicalscavenging, antioxidant, anthelmintic, diuretic effect, antiplatelet, antimicrobial, hepatoprotective, antidiabetic, anticancer, and antifertility activity. Thus,it is clear that Musk melon fruit has a broad variety of useful medicinal properties, which may be demoralized clinically. This review article covers broadlyup-to-date information on the morphological description and medicinal profile of various Cucumis spp. and Musk melon.Keywords: Musk melon, Cucumis spp., Antiulcer, Anioxidant

A REVIEW ON HYPERHOMOCYSTEINEMIA AND ITS RISK FACTORS

ABSTRACTHyperhomocysteinemia (Hhcy) is a pathological condition characterized by abnormally large levels of homocysteine in blood. Homocysteine (Hcy) is a highly reactive sulphur-containing amino acid derived from methionine, an essential amino acid. Excess homocysteine produced in the body is excreted out of the tightly regulated cell environment into the blood. It is the role of the liver and kidney to remove excess Hcy from the blood. Hyperhomocysteinemia increases the generation of ROS by activating NADPH oxidase, downregulates the endothelial nitric oxide synthase (eNOS) and thus reduces the bioavailability of nitric oxide (NO). Moreover, it increases the production of proinflammatory cytokines like tumor necrosis factor-α (TNF-α) by activating nuclear factor-kappa B (NF-κB). Hyperhomocysteinemia is caused by the excess deficiencies of the vitamins like pyridoxine (B6), folic acid (B9), or B12 and is considered as an independent risk factor for various cardiovascular diseases like endothelial dysfunction, vascular inflammation, atherosclerosis, hypertension, cardiac hypertrophy and heart failure.Â

PREVALENCE AND RISK FACTOR OF POLYCYSTIC OVARIAN SYNDROME

ABSTRACTPolycystic ovarian syndrome (PCOS) is the most common endocrine disorder in women. Its clinical manifestation varies from mild to severedisturbance of reproductive and metabolic functions. PCOS is clinical and public health importance because it is affecting up to one in five womenof reproductive age. It is an X-linked dominant condition and has diverse clinical implications such as psychological features (anxiety, depression),reproductive features (hirsutism and hyperandrogenism), and impaired glucose tolerance. It is widely dependent on environmental, genetic, ethnicityfactors including lifestyle and body weight. Weight loss improves the endocrine profile and increases chances of ovulation and pregnancy. It canbe treated with medications such as clomiphene citrate, tamoxifen, aromatase inhibitors, and gonadotrophins. The last option for fertilization isin vitro fertilization when other treatment fails. Its prevalence is estimated at 4-8% from studies performed in Spain and USA. Lifestyle including diet,exercise, and behavior therapy improves fertility. PCOS has unique interactions with the ever increasing obesity prevalence worldwide as obesityinducedinsulin resistancesignificantlyaggravatesall thefeaturesof PCOS.EducationabouthowPCOSaffectslong-termhealth shouldbe providedtowomenwith this disordertofeelphysicaland psychologicalbenefits so that theycould engagethemselvesmorewith their health careproviders.Keywords: Polycystic ovarian syndrome, Hyperinsulinemia, Hormone disbalance, Hirsutism, Ovarian cyst, Obesity, Sleep disorders

Multidetector CT arthrography in shoulder instability and its comparison with MR arthrography and arthroscopy

Background: Purpose of this study was to compare diagnostic effectiveness of MDCT arthrography (MDCTA) in shoulder instability and pain in throwing and its comparison to MR arthrography (MRA) and arthroscopy taking arthroscopy as gold standard.Methods: 20 patients with history of recurrent shoulder dislocation in activity were included in this study. After detailed clinical examination, each patient underwent MDCT-MR arthrography in one sitting followed by diagnostic arthroscopy within 6 weeks. Results were compared with the help of statistician.Results: At arthroscopy, 10 Bankart’s lesions, 7 Hill Sachs lesion, 6 SLAP lesion, 1 ALPSA, 1 capsular laxity, 1 partial subscapularis tear and 1 supraspinatus fraying were visualized in 20 shoulders. For Bankart’s lesion MDCT has sensitivity 80%, specificity 100%, positive predictive value (PPV) 100% and negative predictive value (NPV) 83.3%. MRA has sensitivity of 90%, specificity 100%, PPV 100% and NPV 90.9%. For SLAP lesions sensitivity, specificity, PPV and NPV for MDCTA and MRA are 88.3%, 100%, 100%, 93.3%. For Hill-Sachs lesion; sensitivity, specificity, PPV and NPV for MDCTA are all 100% and for MRA they are 85.7%, 100%, 100%, 92.8% respectively. For ALPSA; sensitivity is 100%, specificity is 95%, PPV is 50% and NPV is 100% both for MDCTA and MRA. К value for MRA is 0.60 and for CTA is 0.55 suggesting moderate agreement.Conclusions: Considering availability, cost, time consumption, superior detection of bony lesions and comparable detection of soft tissue lesions; MDCTA can be used as single investigation of choice in shoulder instability pain

Preliminary evaluation of melatonin in the kindling model of epilepsy

During the past decades, epilepsy syndrome has been depicted across India as well as worldwide and this leads to increasing mortality and morbidity rate. Researchers are trying to investigate the responsible causes and risk factors for seizure occurrence. Epilepsy is a chronic disorder which is derived from a Latin word ‘sacire’ meaning ‘convulsive attack’ and is expressed as a paroxysmal experience appointed to atypical, unnecessary or concurrent neuronal bustle in the brain. The treatment of epilepsy involves the use of anti-epileptic drugs i.e. Sodium valproate, phenytoin, carbamazepine. Despite being treated with the available anti-convulsant drugs, this disease is still prevalent worldwide. So, as an adjuvant treatment melatonin exhibit an anti-epileptic activity in several animal models of epilepsy. However, its anti-epileptic potential has yet to be evaluated in Pentylenetetrazole (PTZ) induced model of epilepsy through kindling phenomenon. Rats were injected with a dose of (35-55 mg/kg) of pentylenetetrazole (PTZ) up to twenty days in alternate days. Observed the convulsive behavior of rats for thirty minutes immediately after PTZ injection.  The entire treatment schedule includes the administration of melatonin (75 mg/kg) one hour prior to the PTZ administration. Sodium valproate was used as standard drug for this kindling model of epilepsy. Keywords: Pentylenetetrazole, Melatonin, Sodium valproate, Gamma-amino butyric aci

Antimicrobial Screening of Some Newly Synthesized Triazoles

The study deals with the synthesis and evaluation of some novel triazoles. Amine linked triazoles were prepared through multistep syntheses. 4-Iodobenzoic acid was taken as initial reactant material, which was converted into methyl ester, then to hydrazide and finally into triazole via dithiocarbazate salt. The triazole was treated with chloroacetyl chloride and further with secondary amines to get the title compounds. Structures of the synthesized compounds were elucidated by Fourier transform infrared spectroscopy (FTIR), 13C and 1H nuclear magnetic resonance (NMR), mass spectrometry and elemental analysis. The synthesized compounds were screened for their antimicrobial activity. The study was carried out against four bacteria and three fungi by disc diffusion method using ciprofloxacin and fluconazole as reference drug for antibacterial and antifungal activities respectively. All the synthesized compounds exhibited zones of inhibition against Candida albicans, Aspergillus niger and Fusarium oxysporum, but the inhibition was more prominent as shown by compound T83. Similarly antibacterial activity was studied against Staphylococcus aureus, Basillus subtilis, Psedomonas aeruginosa and Escherichia coli. Data revealed that compounds T81 and T83 were effective against the bacterial strains. Minimum inhibitory concentration test (MIC) was also carried out to ascertain the bacteriostatic property of the test compounds

Role of ACE and ACE-2 in abrogated cardioprotective effect of ischemic preconditioning in ovariectomized rat heart

Ischemic heart disease is the leading cause of death in postmenopausal women. The activity of heart ACE increases whereas the activity of ACE-2 decreases after menopause. The present study was designed to investigate the role of ACE and ACE-2 in the abrogated cardioprotective effect of IPC in OVX rat heart. The heart was isolated from OVX rat and mounted on Langendorff’s apparatus for giving intermittent cycles of IPC. The infarct size was estimated using TTC stain, and coronary effluent was analyzed for LDH, CK-MB, and nitrite release. IPC induced cardioprotection was significantly attenuated in the ovariectomized rat heart as compared to the normal rat heart. However, this attenuated cardioprotection was significantly restored by perfusion of DIZE, an ACE-2 activator, and captopril, an ACE inhibitor, alone or in combination noted in terms of decrease in myocardial infarct size, the release of LDH and CK-MB, and also increase in the release of NO as compared to untreated OVX rat heart. Thus, it is suggested that DIZE and captopril, alone or in combination restore the attenuated cardioprotective effect of IPC in OVX rat heart which is due to an increase in ACE-2 activity and decrease in ACE activity after treatment

Role of cardiac renin angiotensin system in ischemia reperfusion injury and preconditioning of heart

Cardio-vascular diseases are the leading cause of morbidity and mortality. Ischemia is a state of oxygen deprivation in tissues, whereas reperfusion is restoration of blood flow in ischemic tissues. Myocardial damage of tissue during reperfusion after ischemic insult is known as myocardial ischemia–reperfusion (I/R) injury. It induces damage to cardiac muscle via increasing expression of oxygen, sodium and calcium ions which are responsible in the activation of proteases and cell death. Heart renin angiotensin system (RAS) plays an important role in the myocardial ischemia and reperfusion injury. Angiotensin (1–7) is responsible for vasodilation and angiotensin II for vasoconstriction. Here-in we reviewed how myocardial I/R injury sets in by up-regulation of angiotensin II that leads to increased infarct size, which can be reduced by the use of ACE inhibitors, ACE2 activators and angiotensin II antagonist

Arthrocentesis for Internal Derangement of Temporomandibular Joint: with and without Sodium Hyaluronate

Introduction: Arthrocentesis is an effective, diagnostic and therapeutic modality for internal derangement of temporomandibular joint. Sodium Hyaluronate has been proposed as an alternative therapeutic agent with similar therapeutic effects. The aim of the study was to evaluate the role of Sodium Hyaluronate as an adjunct in treatment of patients with internal derangement of temporomandibular joint. Methodology: A comparative study on 40 patients between the age group 20-64 years with internal derangement of temporomandibular joint was undertaken to evaluate the role of sodium hyaluronate as an adjunct in treatment. These patients were diagnosed clinically and radiographically with temporomandibular joint internal derangement who failed to respond to conservative treatments. They were divided in two groups randomly, each comprising of 20 patients. Group A comprised of patients who underwent arthrocentesis with Ringer Lactate and followed by injection with Sodium Hyaluronate. Group B were patients who underwent arthrocentesis with Ringer Lactate only. Results were evaluated on the parameters of pain, mouth opening, clicking, deviation, determination of range of lateral and protrusive movements and other complications. They were evaluated on pre -operative day, immediate post operative day and first, third and sixth month post operatively. Results: There was marked difference in all symptoms viz. of pain, mouth opening, clicking, deviation, determination of range of lateral and protrusive movements in group A as compared to group B with group A showing better response. Conclusion: Sodium Hyaluronate injection is the preferred treatment for patients suffering with temporomandibular joint internal derangement who were refractory to corroborative methods