Ramaraj Thirugnanasampandan

Analysis of chemical composition and bioactive property evaluation of Indian propolis

OBJECTIVEnTo analyze the chemical composition and to evaluate the bioactive potential of hydroalocoholic extract of propolis.nnnMETHODSnEthanol extract of propolis was analyzed by GC-MS, HPTLC and HPLC methods and in vitro antioxidant, anticholinesterase and cytotoxicity assay were performed.nnnRESULTSnGC-MS analysis revealed the presence of fatty acids, alcohols, and quercetin. Quercetin was identified and quantified by HPTLC and HPLC methods. Dose dependent DPPH and hydroxyl radical scavenging activity of hydroalcoholic extract of propolis was calculated as 16.20 and 34.33 µg/mL respectively. Inhibition of lipid peroxidation was significant and the IC50 value was calculated as 55.56µg/mL. Anticholinesterase activity was less observed. The cytotoxic activity against both breast (MCF-7) and lung cancer (A543) cell lines were significant and the IC50 value was calculated as 10 and 13 µg/mL respectively.nnnCONCLUSIONSnThese findings showed that bioactive compounds present in propolis will alleviate many diseases and can be used for better human health.

Synthesis and biological evaluation of new spirooxindoles with embedded pharmacophores

A regioselective synthesis of new mono and bisoxindoles containing bis spiro heterocyclic hybrids has been envisaged via 1,3-dipolar cycloaddition of azomethine ylides with the dipolarophile (E)-3-((2-methoxyquinolin-3-yl)methylene)indolin-2-one, obtained through the base catalyzed condensation of indolin-2-one with substituted 2-methoxyquinoline-3-carbaldehyde. The regiochemistry and stereochemistry of the synthesized products were characterized by 1D and 2D NMR techniques and single crystal X-ray diffraction studies. Many of the compounds were found to show in vitro antioxidant, antidiabetic and acetylcholinesterase inhibitory activities.

Protection of cadmium chloride induced DNA damage by Lamiaceae plants.

OBJECTIVEnTo analyze the total phenolic content, DNA protecting and radical scavenging activity of ethanolic leaf extracts of three Lamiaceae plants, i.e. Anisomelos malabarica (A. malabarica), Leucas aspera (L. aspera) and Ocimum basilicum (O. basilicum).nnnMETHODSnThe total polyphenols and flavonoids were analyzed in the ethanolic leaf extracts of the lamiaceae plants. To determine the DNA protecting activity, various concentrations of the plant extracts were prepared and treated on cultured HepG2 human lung cancer cells. The pretreated cells were exposed to H2O2 to induce DNA damage through oxidative stress. Comet assay was done and the tail length of individual comets was measured. Nitric oxide and superoxide anion scavenging activities of lamiaceae plants were analyzed.nnnRESULTSnAmong the three plant extracts, the highest amount of total phenolic content was found in O. basilicum (189.33 mg/g), whereas A. malabarica showed high levels of flavonoids (10.66 mg/g). O. basilicum also showed high levels of DNA protecting (85%) and radical scavenging activity.nnnCONCLUSIONSnThe results of this study shows that bioactive phenols present in lamiaceae plants may prevent carcinogenesis through scavenging free radicals and inhibiting DNA damage.

Chemical composition analysis and antioxidant activity evaluation of essential oil from Orthosiphon thymiflorus (Roth) Sleesen

Abstract Objective Orthosiphon thymiflorus (Roth) Sleesen (O. thymiflorus) is an aromatic plant widely distributed in the Western Ghats of South India. The present study investigates the chemical composition and antioxidant activities of O. thymiflorus essential oil isolated from the leaves. Methods The essential oil was hydrodistilled from the leaves by using Clevenger apparatus. Isolated essential oil was chemically analyzed by gas chromatography (GC) and gas chromatography- mass spectrometry (GC-MS). In vitro antioxidant activity of the isolated essential oil was determined. Results Chemical composition analysis of essential oil reported to the presence of thirty three compounds. The major compound was 2-isopropyl-5-methyl-9-methylene-bicyclo-1-decene (4.4.0) (42.62%) followed by carotol (16.48%), α -cadinol (6.14%) and δ-3-carene (5.15%). In vitro antioxidant activity of the isolated oil showed dose dependent free radical scavenging activity against DPPH (IC50 437.12±0.02 ?g/mL) and hydroxyl radicals (IC50 317.88±0.02 μg/mL). Metal chelating and prevention of deoxyribose degradation activities of the oil was observed with the IC50 of 339.78±0.01 μg/mL and 158.33±0.02 μg/mL respectively. Antioxidant activity of the oil was low when compared with the positive controls such as BHT and ascorbic acid. Conclusions The present study shows various chemical components present in the O. thymiflorus essential oil and with its significant antioxidant activity thus has great potential to be used as natural food supplement.

Analysis of chemical composition and evaluation of antigenotoxic, cytotoxic and antioxidant activities of essential oil of Toddalia asiatica (L.) Lam.

Abstract Objective To analyse the chemical composition of essential oil isolated from the leaves of Toddalia asiatica (L.) Lam. and to test its bioactive properties. Methods Gas chromatography-mass spectrometry (GC/MS) analysis and antigenotoxicity, cytotoxicity and antioxidant studies of isolated oil. Results GC-MS analysis of oil revealed the presence of 42 compounds. The major compound in the oil was β-phellandrene (21.35%). DNA protecting activity of oil was considerably significant against H 2 O 2 induced genotoxicity in human lymphocytes. Concentration of oil needed to protect 50% of DNA was calculated as 100 μg/mL. Cytotoxicity of oil against breast (MCF-7) and colorectal (HT-29) cancer cells were observed with the IC 50 value of (7.80±0.03) μg/mL and (100.00±0.16) μg/mL respectively. Considerable DPPH free radical, hydroxyl radical scavenging, iron chelation and inhibition of lipid peroxidation activities of oil were also studied. Conclusions The results of the present study clearly indicate oil could be a promising candidate for food and drug preparation.

Antimetastatic and Anti-Inflammatory Potentials of Essential Oil from Edible Ocimum sanctum Leaves

Antimetastatic and anti-inflammatory activities of Ocimum sanctum essential oil (OSEO) have been assessed in this study. OSEO at the concentration of 250u2009μg/mL and above showed a significant (* P < 0.05) decrease in the number of migrated cancer cells. In addition, OSEO at concentration of 250u2009μg/mL and above suppressed MMP-9 activity in lipopolysaccharide (LPS) induced inflammatory cells. A dose-dependent downregulation of MMP-9 expression was observed with the treatment of OSEO compared to the control. Our findings indicate that OSEO has both antimetastatic and anti-inflammatory potentials, advocating further investigation for clinical applications in the treatment of inflammation associated cancer.

In vitro antioxidant and cytotoxic activities of essential oil of Feronia elephantum Correa.

OBJECTIVEnTo analyse the chemical composition and evaluation of antioxidant, cytotoxic and DNA fragmentation activities of essential oil of Feronia elephantum Correa.nnnMETHODSnChemical composition analysis of hydrodistilled essential oil was determined by gas chromatography-mass spectrometry and in vitro antioxidant activity of oil was determined by DPPH free radical, hydroxyly radical scavenging, metal chelating and prevention of deoxyribose degradation. Cytotoxicity and DNA fragmentation activities against breast cancer cells (MCF-7) were also analyzed.nnnRESULTSnGas chromatography-mass spectrometry analysis revealed the presence of 24 compounds with caryophyllene oxide (62.29%) as major compound. A considerable antioxidant, cyotoxic and DNA fragmentation activities of oils was observed.nnnCONCLUSIONSnThe result of this study clearly indicates oil could be useful for food preservation and preparation.

Chemical composition analysis, antioxidant and antibacterial activity evaluation of essential oil of Atalantia monophylla Correa

Background: Atalantia monophylla Correa. a small tree belongs to the family Rutaceae. It is distributed throughout India and in Tamil Nadu the species is commonly seen in foothills of dry vegetation. Objective: The aim was to hydrodistillate and analyze the chemical composition of essential oil from the fresh leaves of A. monophylla Correa. collected in two different seasons (December, 2013 and May, 2014) and to evaluate antioxidant and antibacterial activities of isolated essential oil. Materials and Methods: Chemical composition of isolated essential oil was analyzed by gas chromatography, gas chromatography coupled with mass spectrometry. Antioxidant activity of oil was assessed using five different antioxidant test systems. Antibacterial activity of oil was tested against six pathogenic bacteria by broth dilution method. Results: Essential oil obtained from the leaves collected during May, 2014 had shown more compounds. Antioxidant activity of oil was moderate when compared with positive control. Minimum inhibitory concentration value of oil was ranges between 139.32 ± 0.001 and 541.11 ± 0.003 µg/mL against all the tested bacteria. Conclusion: Result clearly indicates essential oil collected during May, 2014 showed more bioactive compounds.

Antioxidant activity evaluation of essential oil and RAPD analysis of in vitro regenerated Blumea mollis (D. Don) Merr.

Essential oil obtained from the leaves of Blumea mollis (D. Don) Merr. was analyzed by gas chromatography and gas chromatography coupled with mass spectroscopy (GC and GC–MS). Bicyclic sesquiterpene, β-caryophyllene, was identified as a major compound which accounted for 24.54xa0%. Antioxidant activity of oil was significantly higher than that of methanol extract of callus. Murashige and Skoog (MS) medium supplemented with 4.4xa0μM BA showed multiple shoot induction after 8xa0weeks of culture. 4.6xa0μM Kin showed in vitro flowering and direct organogenesis was observed from the leaf explants on medium containing 4.4xa0μM BA and 5.4xa0μM NAA. Rooted plantlets developed on half strength MS medium fortified with 2.1xa0μM IBA were hardened and percentage survival was recorded up to 70. RAPD analysis revealed a little genetic variation in micropropagated plants.

Molecular Docking and Dynamic Simulation Studies of Terpenoids of I. wightii (Bentham) H. Hara against Acetylcholinesterase and Histone Deacetylase3 Receptors.

BACKGROUNDnGenus Isodon (Lamiaceae) is a prolific source for bioactive terpenoids. Nowadays, people move towards natural products because of undesirable effects of chemotherapeutic drugs.nnnOBJECTIVEnIn silico and in vitro approaches were attempted to screen bioactive terpenoids isolated from Isodon wightii with acetylcholinesterase and histone deacetylase3 receptors.nnnMETHODSnTerpenoids such as abietic acid, oleanolic acid, α-amyrin acetate, β-amyrin acetate were docked with AchE and HDAC3 receptors using AutoDock Vina (version 1.1.2). Further, GROMACS 5.1.2 package was used to perform molecular dynamic simulation. In vitro apoptosis was tested using hoechst 33258 and acridine orange/ethidium bromide.nnnRESULTSnLigplot analysis indicated that abietic acid had strong binding efficiency with AchE and HDAC3 receptors forming one and four hydrogen bonds respectively. Root mean square deviation analysis showed AchE-abietic acid and HDAC3-abietic acid complexes with high deviation which later attains equilibrium around ~25000ps and ~10000ps respectively. Root mean square fluctuation study showed that the complexes have high fluctuations indicates the high flexibility of residues. Solvent accessible surface area revealed the favourable interacting region of AchE and HDAC3 receptors with abietic acid in the range of ~215nm2 to ~235nm2 and ~157nm2 to ~175nm2 respectively. Apoptosis inducing the activity of abietic acid was tested against HeLa cells. Hoechst 33258 staining showed increased apoptosis by abietic acid in a concentration-dependent manner. AO/EtBr dual staining showed early apoptosis at 25-75µg/mL and necrosis at 100-125µg/mL abietic acid.nnnCONCLUSIONnIn silico and in vitro studies suggest that abietic acid could be a promising terpenoid for treating Alzheimers disease and cervical cancer.