Potential Role of Benzoic Acid and its Synthetic Derivatives to Alleviate Cancer: An Up-to-Date Review.

Unregulated cell division is one of the main causes of cancer. These cancerous cells negatively impact nearby healthy cells. Cancer can occur anywhere in the body. Normal cell division occurs when cells grow, reproduce, and divide as the body needs. As a normal cascade of cell growth and division, when the cells get damaged, they undergo death, and normal cells develop. However, sometimes, this process is not followed, and abnormal or damaged cells start to grow and multiply several times more than normal. This particular process may form the basis of cancer. There is a research gap in terms of identifying personalized synthetic anticancer therapy, which may be based on individual patient characteristics with an aim to optimize treatment efficacy and minimize adverse effects. While searching for new bioactive compounds, it has been observed that organic molecules with benzoic acid (BA) moiety possess significant anticancer potential. Several works of literature reported the use of BA from natural or synthetic sources to synthesize bioactive chemicals. It has been observed that several natural products also contain BA moiety, and the presence of this moiety is considered responsible for several important biological activities. Therefore, in order to chemically synthesize a wide variety of potent biologically active compounds, benzoic acid as a basic moiety in the form of a scaffold can be employed. Other synthetic compounds with BA scaffolds include furosemide, tetracaine, and bumetanide. The current article aims to focus on past and present work done on BA derivatives and to emphasize the molecular pathways involved in cancer treatment. The future prospects for research in this area are encouraging as researchers are striving to advance synthetic BA derivatives. This could possibly contribute to more efficient treatments and better results for cancer patients.

In-silico based Designing of benzo[d]thiazol-2-amine Derivatives as Anal-gesic and Anti-inflammatory Agents.

BACKGROUND: Benzo[d]thiazoles represent a significant class of heterocyclic com-pounds renowned for their diverse pharmacological activities, including analgesic and anti-inflammatory properties. This molecular scaffold holds substantial interest among medicinal chemists owing to its structural versatility and therapeutic potential. Incorporating the benzo[d]thiazole moiety into drug molecules has been extensively investigated as a strategy to craft novel therapeutics with heightened efficacy and minimized adverse effects. AIMS: The aim of the present research work was to design, synthesize and characterize the new benzo[d]thiazol-2-amine derivatives as potent analgesic and anti-inflammatory agents. MATERIALS AND METHODS: The synthesis of the presented benzo[d]thiazol-2-amine derivatives was performed by condensing-(4-chlorobenzylidene) benzo[d]thiazol-2-amine with a number of substituted phenols in the presence of potassium iodide and anhydrous potassium carbonate in dry acetone. IR spectroscopy, 1HNMR spectroscopy, 13CNMR spectroscopy and Mass spectroscopy methods were used to characterize the structural properties of all 13 newly syn-thesized derivatives. The molecular properties of these newly synthesized derivatives were estimated to study the attributes of drug-like candidates. Benzo[d]thiazol-2-amine derivatives were molecularly docked with selective enzymes COX-1 and COX-2. Analgesic and anti-inflammatory activities of synthesized compounds were evaluated by us-ing albino rats. RESULTS: Findings of the research suggested that compounds G3, G4, G6, G8 and G11 possess higher binding affinity than diclofenac sodium, when docking was performed with enzyme COX-1. Compounds G1, G3, G6, G8andG10 showed lower binding affinity than Indometha-cin when docking was performed with enzyme COX-2.In vitro evaluation of the COX-1 and COX-2 enzyme inhibitory activities was performed for synthesized compounds. DISCUSSION: Compounds G10 and G11 exhibited significant COX-1 and COX-2 enzyme in-hibitory action with an IC50 value of 5.0 and 10 µM, respectively. Using the hot plate method and the carrageenan-induced rat paw edema model, the synthesized compounds were screened for their biological activities, including analgesic and anti-inflammatory activities. Highest analgesic action was exhibited by derivative G11 and the compound G10 showed the highest anti-inflammatory response. Inhibition of COX may be considered as a mechanism of action of these compounds. CONCLUSION: It was concluded that synthesized derivatives G10 and G11 exhibited significant analgesic and anti-inflammatory effect; therefore, the said compounds may be subjected to further clinical investigation for establishing these as future compounds for the treatment of pain and inflammation.

Recent Advancements in Liquid Chromatographic Techniques to Estimate Pesticide Residues Found in Medicinal Plants around the Globe.

In the present review article, different advanced liquid chromatographic techniques and the advanced techniques other than liquid chromatography that are used to estimate the pesticide residues from different plant-based samples are presented. In the beginning of the article, details of pesticides, their health effects and various cell lines used for the related study has been outlined. Afterward, detailed descriptions regarding pesticides classification are inscribed. In the end, recent advancements in the area of analysis of pesticides for herbal drugs are explained. Solid phase micro extraction (SPME) and solid-phase extraction (SPE) are considered as most common method of sample preparation for pesticides and its residual analysis. The most commonly used analytical separation technique for pesticide analysis is liquid chromatography (LC) integrated with mass spectrometry (MS) and MS/MS as Triple Quadrupole Mass Spectrometer (QqQ) for the samples analysis where high level of sensitivity and accuracy is required in quantification.

Mitigation of zinc toxicity through differential strategies in two species of the cyanobacterium Anabaena isolated from zinc polluted paddy field.

The present study describes the physiological and biochemical mechanisms of zinc tolerance in two heterocytous cyanobacteria i.e. Anabaena doliolum and Anabaena oryzae, treated with their respective LC50 concentrations of zinc (3 and 4.5 mg L-1) for eight days. The feedbacks were examined in terms of growth, metabolism, zinc exclusion, zinc accumulation, oxidative stress, antioxidants and metallothionein contents. Although the growth and metabolic activities were reduced in both the cyanobacterium, maximum adversity was noticed in A. doliolum. The higher order of abnormalities in A. doliolum was attributed to excessive accumulation of zinc and enhanced reactive oxygen species (ROS) production. However, the comparatively higher growth and metabolic activities of A. oryzae were ascribed to the lower accumulation of zinc as a result of released polysaccharides mediated zinc exclusion, synthesis of zinc chelating metallothioneins and subsequent less production of ROS. The oxidative stress and macromolecular damages were prominent in both the cyanobacterium but the condition was much harsher in A. doliolum which may be explained by its comparatively low antioxidative enzyme activities (SOD, APX and GR) and smaller amount of ascorbate-glutathione-tocopherol contents than that of A. oryzae. However, sustenance of 50% growth by A. doliolum under zinc stress despite severe cellular damages was attributed to the enhanced synthesis of phenolics, flavonoids, and proline. Thus, differential zinc tolerance in A. doliolum and A. oryzae is possibly the outcome of their distinct mitigation strategies. Although the two test organisms followed pseudo second order kinetics model during zinc biosorption yet they exhibited differential zinc biosorption capacity. The cyanobacterium A. oryzae was found to be more efficient in removing zinc as compared to A. doliolum and this efficiency makes A. oryzae a promising candidate for the phycoremediation of zinc polluted environments.

Aripiprazole: An FDA Approved Bioactive Compound to Treat Schizophrenia- A Mini Review.

OBJECTIVE: Aripiprazole, a synthetic compound, obtained by chemical modification of the structure of quinolinone is considered as an atypical antipsychotic drug. The present review is an attempt to summarize the updated information related to reported chemistry and pharmacology of Aripiprazole. DEVELOPMENT: Aripiprazole, under development by Otsuka Pharmaceutical, was approved by the U.S. Food and Drug Administration (USFDA) by the end of 2002 with an aim to treat patients with schizophrenia. This drug got approved by European Commission in February 2013 to treat the patients having severe manic episodes in bipolar I disorder Additionally, it got approval in Japan in January 2006 and in Canada in 2014. Pharmacology: Aripiprazole shows high specificity for dopamine receptor especially D2 and D3, serotonin 5-HT1A and serotonin 5-HT2A receptors, reasonable specificity for dopamine D4, serotonin 5- HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors. It also shows moderate specificity for the serotonin reuptake. The major side effects include headache, agitation, akithesia, anxiety, tachycardia, insomnia, postural hypotension, constipation, vomiting, dizziness, nervousness and somnolence. CONCLUSION: The present article embarks the available information on Aripiprazole with emphasis on its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism and clinical trials.

Banded versus nonbanded laparoscopic sleeve gastrectomy: 5-year outcomes.

BACKGROUND/OBJECTIVES: Laparoscopic sleeve gastrectomy (SG) is the most commonly performed bariatric/metabolic operation. However, inadequate long-term weight loss remains a problem in some cases, possibly from gastric-sleeve dilation. Adding a reinforcing ring around the proximal gastric sleeve has been proposed, but relevant data are scant. We performed the largest, longest-term study yet of banded SG (BSG) compared to nonbanded SG. SETTING: University hospital. METHODS: In 2012, 68 patients at our institution underwent BSG, and 152 underwent SG. Data were prospectively collected into a standardized database from both cohorts during in-person visits at 0, .5, 1, 2, 3, 4, and 5 postoperative years, enabling this retrospective matched cohort study. RESULTS: The groups were extremely well-matched at baseline for all relevant characteristics. Operative time was longer and blood loss greater with BSG, but these differences were clinically inconsequential. The only major perioperative complications were 1 hemorrhage in each group. Follow-up at 5 years was 81% for BSG and 67% for SG. Weight loss was equivalent between groups at 6 and 12 months. Thereafter, weight loss was substantially greater following BSG compared to SG at 2, 3, 4, and 5 years, with the magnitude of difference increasing at each successive year. At 5 years, total body mass index decrease was 33.0 ± 12.0% for BSG versus 21.7 ± 18.2% for SG (P = .0001). No major late complications occurred in either group. At 5 years, BSG patients reported minimal food intolerances, rare postprandial vomiting, and almost no heartburn. CONCLUSIONS: BSG is safe and produces substantially more weight loss than nonbanded SG at 2 through 5 postoperative years, with minimal side effects.

Physiological mechanisms of aluminum (Al) toxicity tolerance in nitrogen-fixing aquatic macrophyte Azolla microphylla Kaulf: phytoremediation, metabolic rearrangements, and antioxidative enzyme responses.

To investigate the extent of aluminum toxicity tolerance of eco-friendly, fast-growing, fresh water, pteridophytic Azolla-Anabaena symbiotic association in terms of altered physiological signals; Azolla microphylla Kaulf was exposed to 0 (control), 100, 250, 500, and 750 µM AlCl3, at pH 4.5 for 6 days. The adversity of Al was increased in a dose-dependent manner and the highest was recorded at 750 µM AlCl3. Despite the significant loss in membrane integrity (80% electrolyte leakage) due to an enhanced generation of H2O2, A. microphylla reflected only 50% growth inhibition (fresh and dry weight) at 500 µM AlCl3 (LD50). However, the average root length of Azolla was drastically reduced at high concentration due to their direct contact with aluminum-containing growth medium. Contrary to this, the whole association maintained moderate chlorophyll, carbohydrate content, photosynthetic efficiency, nitrogen-fixing ability, and nitrogen content at high Al concentration. Probably, growth protection was pertained through significant detoxification of H2O2 by employing an efficient antioxidative defense system including antioxidative enzymes (SOD, APX, and CAT) and non-enzymatic antioxidant carotenoids. An enhanced level of phenolics and flavonoids in the root exudates possibly maintained a non-toxic level of aluminum inside the cell (195.8 µg Al/g FW) which makes A. microphylla a suitable pteridophytic plant to not only remove toxic Al from the contaminated sites but also to improve nitrogen status of those regions. Graphical abstract ᅟ.

Ozenoxacin: A Novel Drug Discovery for the Treatment of Impetigo.

OBJECTIVE: Ozenoxacin is one of the potent quinolone antibiotics, recently approved by the United States Food and Drug Administration (USFDA) with reported pharmacology to treat the impetigo. The demand for better acting topical formulation is increasing day by day. The present review is an attempt to summarize the facts behind the chemistry and biological applications of Ozenoxacin. Mechanism of Action: This novel drug being a quinolone antibiotic compound, acts by inhibiting DNA gyrase A and topoisomerase IV and affects supercoiling, supercoil relaxation, chromosomal condensation, chromosomal decatenation and many others. Pharmacology: Ozenoxacin has demonstrated to have a bactericidal activity against organisms, such as Staphylococcus aureus and Staphylococcus pyogenes. Ozenoxacin is non-fluorinated quinolone and being developed for the other dermatological bacterial infections as well. No sign of genotoxicity was observed when tested experimentally. CONCLUSION: The present review also covers the complete picture of pharmacokinetics, clinical trials, toxicity and future scope and possible avenues in this arena.

Iron deficiency influences NtcA-dependent regulation of fatty acid desaturation and heterocyte envelop formation in Anabaena sp. PCC 7120.

In Anabaena sp. PCC 7120, iron is an essential trace element and its availability determines proper functioning of several kinds of metabolisms. Iron deficiency leads to several unavoidable consequences including membrane damage. In the present study, we dealt with the impact of iron deficiency on NtcA (global nitrogen regulator)-dependent regulation of two important processes, i.e. fatty acid desaturation and heterocyte envelop formation in cyanobacterium Anabaena sp. PCC 7120. In Anabaena sp. PCC 7120, NtcA regulates fatty acid desaturation by regulating enzyme fatty acid desaturases. The NtcA-based regulation of fatty acid desaturation may be direct or indirect. Furthermore, the expression of genes involved in the heterocyte envelope polysaccharide (HEP) layer formation (hepABCK) and heterocyte-specific glycolipids (HGLs) synthesis (devH, hglEA , prpJ and devB) were also under the control of NtcA and reduced under iron deficiency background. The enhanced expression of furA and early downregulation of ntcA under iron deficiency is responsible for reduction in fatty acid desaturation as well as decrease in the expression of genes involved in HEP layer formation and HGL synthesis. Overall results confirmed that iron deficiency influences the NtcA-based regulation of fatty acid desaturation and heterocyte envelop formation in Anabaena sp. PCC 7120.

Screening of acute and sub-chronic dermal toxicity of Calendula officinalis L essential oil.

The objective of the study is to access the safety of Calendula essential oil by studying acute and sub-chronic dermal toxicity. The dermal toxicities of Calendula essential oil were evaluated in accordance with OECD guidelines number 402 and 411 respectively. The animals were exposed to Calendula officinalis (CO) essential oil dose of 20 mL/kg body weight for acute dermal toxicity, whereas for dermal sub-chronic toxicity study, rats were exposed to CO oil 2.5, 5 and 10 mL/kg body weight, respectively, for 7 times in a week for 90 days. The parameters studies included CNS stimulation, depression, hematological parameters (RBC, WBC, Hb, Lymphocyte % etc), biochemical parameters (total protein, albumin, total bilirubin, ALP, AST, etc), relative organ weight, necropsy and histopathology. In toxicity studies, all animals exhibited normal behavior without any change in hematology, blood biochemistry, necroscopical and histopathology. The no observed effect level (NOEL) and no observed adverse effect level (NOAEL) of CO oil were 2.5 and 10 mg/kg/day, respectively. CO oil is under the herbal medicinal product according to the European Medicines Agency with the claim of an LD50 value of 20 mL/kg body weight. The result indicates that CO essential oil did not produce any significant toxic effects.

Effect of traditional medicine brahmi vati and bacoside A-rich fraction of Bacopa monnieri on acute pentylenetetrzole-induced seizures, amphetamine-induced model of schizophrenia, and scopolamine-induced memory loss in laboratory animals.

OBJECTIVE: Brahmi vati (BV) is an Ayurvedic polyherbal formulation used since ancient times and has been prescribed in seizures associated with schizophrenia and related memory loss by Ayurvedic practitioners in India. The aim of the study was to investigate these claims by evaluation of anticonvulsant, antischizophreniac, and memory-enhancing activities. Antioxidant condition of brain was determined by malondialdehyde (MDA) and reduced glutathione (GSH) levels estimations. Acetylcholinesterase (AChE) was quantitatively estimated in the brain tissue. METHODS: Brahmi vati was prepared in-house by strictly following the traditional Ayurvedic formula. Bacoside A rich fraction (BA) of Bacopa monnieri was prepared by extraction and fractionation. It was than standardized by High Performance Liquid Chromatography (HPLC) and given in the dose of 32.5mg/kg body weight to the different groups of animals for 7days. On the seventh day, activities were performed adopting standard procedures. KEY FINDINGS: Brahmi vati showed significant anticonvulsant, memory-enhancing and antischizophrenia activities, when compared with the control groups and BA. It cause significantly higher brain glutathione levels. Acetylcholinesterase activity was found to be significantly low in BV-treated group. CONCLUSION: The finding of the present study suggests that BV may be used to treat seizures associated with schizophrenia and related memory loss.

Transcriptional regulation of acetyl CoA and lipid synthesis by PII protein in Synechococcus PCC 7942.

PII protein family is widespread in prokaryotes and plants. In this study, impacts of PII deficiency on the synthesis of acetyl CoA and acetyl CoA carboxylase enzyme (ACCase) was analyzed in the Synechococcus sp. PCC 7942 by evaluating the mRNA levels of pyruvate kinase (PK), pyruvate dehydrogenase (PDH), citrate synthase (CS), biotin synthase (BS), biotin carboxylase (BC), biotin carboxyl carrier protein (BCCP), carboxyl transferase (CT) α and ß subunits. The PII deficient Synechococcus sp. PCC 7942 showed upregulation of all the above-mentioned genes, except CS. Analyses of genes required for acetyl coA synthesis exhibited a substantial increase in the transcript levels of PK and PDH in the PII mutant strain. In addition, the PII mutant also displayed reduced acetyl CoA content, high ACCase activity, and increased lipid content. The lessening of acetyl CoA content was attributed to the rapid utilization of acetyl CoA in fatty acid synthesis as well as in the TCA cycle whereas the increased ACCase activity was ascribed to the rise in mRNA levels of BS, BC, BCCP, CT α, and ß genes. However, increased lipid content was correlated with the declined total protein content. Hence, the study suggested that PII protein regulates the synthesis of acetyl CoA and ACCase enzyme at the transcriptional level.

The Combined Use of in Silico, in Vitro, and in Vivo Analyses to Assess Anti-cancerous Potential of a Bioactive Compound from Cyanobacterium Nostoc sp. MGL001.

Escalating incidences of cancer, especially in developed and developing countries, demand evaluation of potential unexplored natural drug resources. Here, anticancer potential of 9-Ethyliminomethyl-12-(morpholin-4-ylmethoxy)-5,8,13,16-tetraaza -hexacene-2,3-dicarboxylic acid (EMTAHDCA) isolated from fresh water cyanobacterium Nostoc sp. MGL001 was screened through in silico, in vitro, and in vivo studies. For in silico analysis, EMTAHDCA was selected as ligand and 11 cancer related proteins (Protein Data Bank ID: 1BIX, 1NOW, 1TE6, 2RCW, 2UVL, 2VCJ, 3CRY, 3HQU, 3NMQ, 5P21, and 4B7P) which are common targets of various anticancer drugs were selected as receptors. The results obtained from in silico analysis showed that EMTAHDCA has strong binding affinity for all the 11 target protein receptors. The ability of EMTAHDCA to bind active sites of cancer protein targets indicated that it is functionally similar to commercially available anticancer drugs. For assessing cellular metabolic activities, in vitro studies were performed by using calorimetric assay viz. 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT). Results showed that EMTAHDCA induced significant cytotoxic response against Dalton's lymphoma ascites (DLA) cells in a dose and time dependent manner with an inhibitory concentration (IC50) value of 372.4 ng/mL after 24 h of incubation. However, in case of normal bone marrow cells, the EMTAHDCA did not induce cytotoxicity as the IC50 value was not obtained even with higher dose of 1,000 ng/mL EMTAHDCA. Further, in vivo studies revealed that the median life span/survival days of tumor bearing mice treated with EMTAHDCA increased significantly with a fold change of ~1.9 and 1.81 corresponding to doses of 5 and 10 mg/kg body weight (B.W.) of EMTAHDCA respectively, as compared to the DL group. Our results suggest that 5 mg/kg B.W. is effective since the dose of 10 mg/kg B.W. did not show any significant difference as compared to 5 mg/kg B.W. Taken together, our findings based on in silico, in vitro, and in vivo analyses suggest that EMTAHDCA has potential anticancer effects, and thus, can be considered for cancer treatment.

Salt stress-induced changes in antioxidative defense system and proteome profiles of salt-tolerant and sensitive Frankia strains.

An appreciation of comparative microbial survival is most easily done while evaluating their adaptive strategies during stress. In the present experiment, antioxidative and whole cell proteome variations based on spectrophotometric analysis and SDS-PAGE and 2-dimensional gel electrophoresis have been analysed among salt-tolerant and salt-sensitive Frankia strains. This is the first report of proteomic basis underlying salt tolerance in these newly isolated Frankia strains from Hippophae salicifolia D. Don. Salt-tolerant strain HsIi10 shows higher increment in the contents of superoxide dismutase, catalase and ascorbate peroxidase as compared to salt-sensitive strain HsIi8. Differential 2-DGE profile has revealed differential profiles for salt-tolerant and salt-sensitive strains. Proteomic confirmation of salt tolerance in the strains with inbuilt efficiency of thriving in nitrogen-deficient locales is a definite advantage for these microbes. This would be equally beneficial for improvement of soil nitrogen status. Efficient protein regulation in HsIi10 suggests further exploration for its potential use as biofertilizer in saline soils.

Structural Elucidation and Molecular Docking of a Novel Antibiotic Compound from Cyanobacterium Nostoc sp. MGL001.

Cyanobacteria are rich source of array of bioactive compounds. The present study reports a novel antibacterial bioactive compound purified from cyanobacterium Nostoc sp. MGL001 using various chromatographic techniques viz. thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Further characterization was done using electrospray ionization mass spectroscopy (ESIMS) and nuclear magnetic resonance (NMR) and predicted structure of bioactive compound was 9-Ethyliminomethyl-12-(morpholin - 4 - ylmethoxy) -5, 8, 13, 16-tetraaza-hexacene - 2, 3 dicarboxylic acid (EMTAHDCA). Structure of EMTAHDCA clearly indicated that it is a novel compound that was not reported in literature or natural product database. The compound exhibited growth inhibiting effects mainly against the gram negative bacterial strains and produced maximum zone of inhibition at 150 µg/mL concentration. The compound was evaluated through in silico studies for its ability to bind 30S ribosomal fragment (PDB ID: 1YRJ, 1MWL, 1J7T, and 1LC4) and OmpF porin protein (4GCP, 4GCQ, and 4GCS) which are the common targets of various antibiotic drugs. Comparative molecular docking study revealed that EMTAHDCA has strong binding affinity for these selected targets in comparison to a number of most commonly used antibiotics. The ability of EMTAHDCA to bind the active sites on the proteins and 30S ribosomal fragments where the antibiotic drugs generally bind indicated that it is functionally similar to the commercially available drugs.

A Systemic Review on Staphylococcal Scalded Skin Syndrome (SSSS): A Rare and Critical Disease of Neonates.

The symptoms of Staphylococcal scalded skin syndrome (SSSS) include blistering of skin on superficial layers due to the exfoliative toxins released from Staphylococcus aureus. After the acute exfoliation of skin surface, erythematous cellulitis occurs. The SSSS may be confined to few blisters localized to the infection site and spread to severe exfoliation affecting complete body. The specific antibodies to exotoxins and increased clearence of exotoxins decrease the frequency of SSSS in adults. Immediate medication with parenteral anti-staphylococcal antibiotics is mandatory. Mostly, SSSS are resistant to penicillin. Penicillinase resistant synthetic penicillins such as Nafcillin or Oxacillin are prescribed as emergency treatment medicine. If Methicillin-resistant Staphylococcus aureus (MRSA) is suspected), antibiotics with MRSA coverage (e.g., Vancomycin or Linezolid) are indicated. Clindamycin is considered as drug of choice to stop the production of exotoxin from bacteria ribosome. The use of Ringer solution to to balance the fluid loss, followed by maintainence therapy with an objective to maintain the fluid loss from exfoliation of skin, application of Cotrimoxazole on topical surface are greatlly considered to treat the SSSS. The drugs that reduce renal function are avoided. Through this article, an attempt has been made to focus the source, etiology, mechanism, outbreaks, mechanism, clinical manisfestation, treatment and other detail of SSSS.

Profenofos induced modulation in physiological indices, genomic template stability and protein banding patterns of Anabaena sp. PCC 7120.

To understand the mechanism underlying organophosphate pesticide toxicity, cyanobacterium Anabaena PCC 7120 was subjected to varied concentrations (0, 5, 10, 20 and 30 mg L(-1)) of profenofos and the effects were investigated in terms of changes in cellular physiology, genomic template stability and protein expression pattern. The supplementation of profenofos reduced the growth, total pigment content and photosynthetic efficiency of the test organism in a dose dependent manner with maximum toxic effect at 30 mg L(-1). The high fluorescence intensity of 2', 7' -dichlorofluorescin diacetate and increased production of malondialdehyde confirmed the prevalence of acute oxidative stress condition inside the cells of the cyanobacterium. Rapid amplified polymorphic DNA (RAPD) fingerprinting and SDS-PAGE analyses showed a significant alteration in the banding patterns of DNA and proteins respectively. A marked increase in superoxide dismutase, catalase, peroxidase activity and a concomitant reduction in glutathione content indicated their possible role in supporting the growth of Anabaena 7120 up to 20 mg L(-1). These findings suggest that the uncontrolled use of profenofos in the agricultural fields may not only lead to the destruction of the cyanobacterial population, but it would also disturb the nutrient dynamics and energy flow.

Studies on metals and pesticide content in some Ayurvedic formulations containing Bacopa monnieri L.

OBJECTIVE: Ayurvedic formulations are preferred over other formulations as well as commercialized on broad level to treat various ailments. The World Health Organization has established certain guidelines for quality control of heavy metals and pesticide residues. Bacopa monnieri, a popular herb with immunomodulator and memory-enhancing properties is the chief constituent of several Ayurvedic formulations, which include Brahmi Vati (BV), Brahmi Ghrita (BG) and Saraswat Churna (SC), etc. In view of the World Health Organization guidelines, two products of each formulation from six different manufacturers were purchased from Ayurvedic Pharmacy, Bulanala-Varanasi, India for testing heavy metal and pesticide residue. METHODS: In the present study, all the formulations--BV, BG and SC--were selected for estimation of four heavy metals namely lead (Pb), cadmium (Cd), chromium (Cr) and nickel (Ni) by a plasma emission spectrophotometer. Organochlorine pesticidal residues were estimated for dichlorodiphenyl trichloroethane, isomers of hexachlorocyclohexane (HCH) and α-endosulfan, etc. in total 12 samples of test formulations containing Bacopa monnieri L. using gas chromatography technique. RESULTS: Out of 12 samples, Pb, Cd, Cr and Ni were present in all samples but below the permissible limit. Although atrazine, aldrin, dialdrin were in below detection limit, but other pesticides were detected in some samples as oxamyl, hexachlorocyclohexanes (α-HCH, ß-HCH and γ-HCH), dichlorodiphenyl trichloroethane and dichlorodiphenyl dichloroethylene. CONCLUSION: The presence of heavy metals in the formulations was low to cause toxicity. However evaluation of heavy metals and pesticide residue in every batch is necessary.

Synthesis and antimicrobial activity of some new diphenylamine derivatives.

In search of new leads toward potent antimicrobial agent, an array of novel derivatives of 2-hydrazinyl-N-N, diphenyl acetamide has been synthesized from the chloroacetylation reaction of diphenylamine (DPA). For this, a series of DPA derivatives were prepared by replacing chlorine with hydrazine hydrate in alcoholic medium and 2-hydrazino-N, N-diphenylacetamide was synthesized. The 2-hydrazino-N, N-diphenylacetamide was further subjected to reaction with various aromatic aldehydes in presence of glacial acetic acid in methanol. The synthesized compounds were characterized by their IR, 1HNMR spectral data and elemental analysis. The compounds were screened for antibacterial and antifungal activity by cup plate method. 2-(2-Benzylidenehydrazinyl)-N, N-diphenylacetamide (A1); 2-(2-(3-methylbenzylidene) hydrazinyl)-N, N-diphenyl-acetamide (A5) and 2-(2-(2-nitrobenzylidine) hydrazinyl)-N, N-diphenyl-acetamide compounds (A7) showed significant antimicrobial as well as antifungal activity. Diphenylamine compounds may be explored as potent antimicrobial and antifungal compounds.

Development of ultraviolet spectroscopic method for the estimation of metronidazole benzoate from pharmaceutical formulation.

BACKGROUND: The present study was undertaken with an objective to develop a simple, accurate, cost-effective and reproducible ultraviolet spectrophotometric method for the estimation of metronidazole benzoate (MB) from pharmaceutical formulations. MATERIALS AND METHODS: The analysis was performed on λmax 268 nm by using 0.1 NHCl as diluents. The proposed method was validated on International Conference Harmonization guideline including the parameters viz., accuracy, linearity, precision, specificity and reproducibility. The proposed method was also used to access the content of MB in two commercial brands of Indian market. RESULTS: Beer's law was obeyed in the concentration range of 1-10 µg/ml having regression equation y = 0.078 x-0.012. The accuracy value for 4 µg/ml and 5 µg/ml concentration of MB was found to be 99.37% and 98.9% respectively. The relative standard deviation of interday and intraday was lesser than 1%. The developed method was applied on two different marketed brands and contents of MB were found to be 98.62% and 98.59% incompliance with labeled claim. The results were under the limit of acceptance statistically. CONCLUSION: It was concluded that the proposed method can be used for routine analysis of MB in bulk and commercial formulations.