Cell death-inducing effect of novel palladium(II) and platinum(II) complexes on non-small cell lung cancer cells in vitro

Purpose  

Treatment for lung cancer is still far from satisfying rates. Therefore, there is a need for novel anticancer agents. For this purpose, novel platinum and palladium complexes {[Pd(sac)(terpy)](sac)·4H₂O (Complex 1), [Pt(sac)(terpy)](sac)·5H₂O (Complex 2), [PdCl(terpy)](sac)·2H₂O (Complex 3), [PtCl(terpy)](sac)·2H₂O (Complex 4)} have been tested against three different non-small cell lung cancer cell lines (A549, H1299, PC-3).     

Synthesis,Structural Characterization,and Antitumor Activity of a Ca(II) Coordination Polymer Based on 1,6-Naphthalenedisulfonate and 4,4′-Bipyridyl

A novel Ca(II) coordination polymer, [CaL(4,4′-bipyridyl)(H₂O)₄]_n (L = 1,6-naphthalenedisulfonate), was synthesized by reaction of calcium perchlorate with 1,6-naphthalenedisulfonic acid disodium salt and 4,4′-bipyridyl in CH₃CH₂OH/H₂O. It was characterized by elemental analysis, IR, molar conductivity and thermogravimetric analysis. X-ray crystallography reveals that the Ca(II) coordination polymer belongs to the orthorhombic system, with space group P2₁2₁2₁. The geometry of the Ca(II) ion is a distorted CaNO₆ pengonal bipyramid, arising from its coordination by four water molecules, one nitrogen atom of 4,4′-bipyridyl molecule, and two oxygen atoms from two L ligands. The complex molecules form a helical chain by self-assembly. The antitumor activity of 1,6-naphthalenedisulfonic acid disodium salt and the Ca(II) coordination polymer against human hepatoma smmc-7721 cell line and human lung adenocarcinoma A549 cell line reveals that the Ca(II) coordination polymer inhibits cell growth of human lung adenocarcinoma A549 cell line with IC50 value of 27 μg/mL, and is more resistive to human lung adenocarcinoma A549 cell line as compared to 1,6-naphthalenedisulfonic acid disodium salt.     

Synthesis and Characterization of Fe(III) and Pb(II) Complexes with 3-Hydroxypyridine-2(1H)-Thiones

Two kinds of 3-hydroxypyridine-2(1H)-thiones were synthesized. The visible (VIS) spectroscopic analysis indicated that 3-hydroxy-1-methylpyridine-2(1H)-thione (4a) and 3-hydroxy-1-(2-hydroxyethyl)pyridine-2(1H)-thione (4b) formed stable 3:1 Fe(III) complexes. The stability constant of the 4b-Fe(III) complex was estimated from the competitive reaction with EDTA and was found to be 36.7 in logβ₃. Treatment of compound 4b with Ga(acac)₃ in D₂O:CD₃OD (9:1) solution afforded 3:1 Ga(III) complex, which was assigned by means of ¹H nuclear magnetic resonance (¹H NMR) spectroscopy. Treatment of compound 4b with Pb(NO₃)₂ gave 4b-Pb(II) complex. The Pb(II) selectivity over biologically relevant Mg(II) and Ca(II) was remarkably improved by adopting N-hydroxyethyl functionality instead of N-methyl group.     

Molecular and Polymer Ln2M2 (Ln = Eu,Gd, Tb,Dy; M = Zn,Cd) Complexes with Pentafluorobenzoate Anions: The Role of Temperature and Stacking Effects in the Structure; Magnetic and Luminescent Properties

Varying the temperature of the reaction of [{Cd(pfb)(H₂O)₄}⁺_n·n(pfb)⁻], [Ln₂(pfb)₆(H₂O)₈]·H₂O (Hpfb = pentafluorobenzoic acid), and 1,10-phenanthroline (phen) in MeCN followed by crystallization resulted in the isolation of two type of products: 1D-polymers [LnCd(pfb)₅(phen)]_n·1.5nMeCN (Ln = Eu (I), Gd (II), Tb (III), Dy (IV)) which were isolated at 25 °C, and molecular compounds [Tb₂Cd₂(pfb)₁₀(phen)₂] (V) formed at 75 °C. The transition from a molecular to a polymer structure becomes possible because of intra- and intermolecular interactions between the aromatic cycles of phen and pfb from neighboring tetranuclear Ln₂Cd₂ fragments. Replacement of cadmium with zinc in the reaction resulted in molecular compounds Ln₂Zn₂ [Ln₂Zn₂(pfb)₁₀(phen)₂]·4MeCN (Ln = Eu (VI), Tb (VIII), Dy (IX)) and [Gd₂Zn₂(pfb)₁₀(H₂O)₂(phen)₂]·4MeCN (VII). A new molecular EuCd complex [Eu₂Cd₂(pfb)₁₀(phen)₄]·4MeCN (X)] was isolated from a mixture of cadmium, zinc, and europium pentafluorobenzoates (Cd:Zn:Ln = 1:1:2). Complexes II-IV, VII and IX exhibit magnetic relaxation at liquid helium temperatures in nonzero magnetic fields. Luminescent studies revealed a bright luminescence of complexes with europium(III) and terbium(III) ions.     

Molecular mechanism of water oxidation in photosynthesis based on the functioning of manganese in two different environments

We present a model of photosynthetic water oxidation that utilizes the property of higher-valent Mn ions in two different environments and the characteristic function of redox-active ligands to explain all known aspects of electron transfer from H₂O to Z, the electron donor to P680, the photosystem II reaction center chlorophyll a. There are two major features of this model. (i) The four functional Mn atoms are divided into two groups of two Mn each: [Mn] complexes in a hydrophobic cavity in the intrinsic 34-kDa protein; and (Mn) complexes on the hydrophilic surface of the extrinsic 33-kDa protein. The oxidation of H₂O is carried out by two [Mn] complexes, and the protons are transferred from a [Mn] complex to a (Mn) complex along the hydrogen bond between their respective ligand H₂O molecules. (ii) Each of the two [Mn] ions binds one redox-active ligand (RAL), such as a quinone (alternatively, an aromatic amino acid residue). Electron transfer occurs from the reduced RAL to the oxidized Z. When the experimental data concerning atomic structure of the water-oxidizing center (WOC), electron transfer between the WOC and Z, the electronic structure of the WOC, the proton-release pattern, and the effect of Cl^- are compared with the predictions of the model, satisfactory qualitative and, in many instances, quantitative agreements are obtained. In particular, this model clarifies the origin of the observed absorption-difference spectra, which have the same pattern in all S-state transitions, and of the effect of Cl^--depletion on the S states.     

Antibacterial activity of crude ethanolic extract and solvent fractions of Ficus pseudopalma Blanco leaves

ObjectiveTo investigate the antimicrobial properties of Ficus pseudopalma (F. pseudopalma) leaf extracts.MethodsThe antibacterial properties of F. pseudopalma Blanco crude ethanolic leaf extract, and its solvent fractions chloroform (CF), ethylacetate (EF) and water fractions were evaluated through antibacterial agar disc diffusion method and the minimum inhibitory concentration (MIC) was determined. Five Gram-positive and five Gram-negative bacteria were used for the study.ResultsThe zone of inhibitions obtained from the antibacterial agar diffusion disc method showed that CF, and EF exhibited active (14-19 mm) antibacterial activity against Bacillus subtilis UST CMS 1011, and partially active (10-13 mm) antibacterial properties against both Staphylococcus aureus ATCC 25923 and Staphylococcus epidermidis ATCC 12228. Water exhibited no antibacterial properties against all microorgranisms tested. The MIC values observed for all Gram-positive bacteria tested were >5 mg/mL, except for Bacillus subtilis whose MIC value was 5 mg/mL for CF and EF fractions. All extracts exhibited no antibacterial activity against Gram-negative bacteria.ConclusionsFrom this study, it can be concluded that F. pseudopalma extracts may be a potential antibacterial agent against Gram-positive bacteria. The antibacterial property may be attributed to flavonoids and terpenoids present in the crude ethanolic extract, CF and EF.     

Crystal Structure,Spectroscopic Characterization,Antioxidant and Cytotoxic Activity of New Mg(II) and Mn(II)/Na(I) Complexes of Isoferulic Acid

The Mg(II) and heterometallic Mn(II)/Na(I) complexes of isoferulic acid (3-hydroxy-4-methoxycinnamic acid, IFA) were synthesized and characterized by infrared spectroscopy FT-IR, FT-Raman, electronic absorption spectroscopy UV/VIS, and single-crystal X-ray diffraction. The reaction of MgCl₂ with isoferulic acid in the aqueous solutions of NaOH resulted in synthesis of the complex salt of the general formula of [Mg(H₂O)₆]⋅(C₁₀H₉O₄)₂⋅6H₂O. The crystal structure of this compound consists of discrete octahedral [Mg(H₂O)₆]²⁺ cations, isoferulic acid anions and solvent water molecules. The hydrated metal cations are arranged among the organic layers. The multiple hydrogen-bonding interactions established between the coordinated and lattice water molecules and the functional groups of the ligand stabilize the 3D architecture of the crystal. The use of MnCl₂ instead of MgCl₂ led to the formation of the Mn(II)/Na(I) complex of the general formula [Mn₃Na₂(C₁₀H₇O₄)₈(H₂O)₈]. The compound is a 3D coordination polymer composed of centrosymmetric pentanuclear subunits. The antioxidant activity of these compounds was evaluated by assays based on different antioxidant mechanisms of action, i.e., with ^•OH, DPPH^• and ABTS^•+ radicals as well as CUPRAC (cupric ions reducing power) and lipid peroxidation inhibition assays. The pro-oxidant property of compounds was measured as the rate of oxidation of Trolox. The Mg(II) and Mn(II)/Na(I) complexes with isoferulic acid showed higher antioxidant activity than ligand alone in DPPH (IFA, IC₅₀ = 365.27 μM, Mg(II) IFA IC₅₀ = 153.50 μM, Mn(II)/Na(I) IFA IC₅₀ = 149.00 μM) and CUPRAC assays (IFA 40.92 μM of Trolox, Mg(II) IFA 87.93 μM and Mn(II)/Na(I) IFA 105.85 μM of Trolox; for compounds’ concentration 10 μM). Mg(II) IFA is a better scavenger of ^•OH than IFA and Mn(II)/Na(I) IFA complex. There was no distinct difference in ABTS^•+ and lipid peroxidation assays between isoferulic acid and its Mg(II) complex, while Mn(II)/Na(I) complex showed lower activity than these compounds. The tested complexes displayed only slight antiproliferative activity tested in HaCaT human immortalized keratinocyte cell line within the solubility range. The Mn(II)/Na(I) IFA (16 μM in medium) caused an 87% (±5%) decrease in cell viability, the Mg salt caused a comparable, i.e., 87% (±4%) viability decrease in a concentration of 45 μM, while IFA caused this level of cell activity attenuation (87% ± 5%) at the concentration of 1582 μM (significant at α = 0.05).     

Enhanced Optical and Antibacterial Activity of Hydrothermally Synthesized Cobalt-Doped Zinc Oxide Cylindrical Microcrystals

Cobalt (Co) doped zinc oxide (ZnO) microcrystals (MCs) are prepared by using the hydrothermal method from the precursor’s mixture of zinc chloride (ZnCl₂), cobalt-II chloride hexahydrate (CoCl₂·6H₂O), and potassium hydroxide (KOH). The smooth round cylindrical morphologies of the synthesized microcrystals of Co-doped ZnO show an increase in absorption with the cobalt doping. The antibacterial activity of the as-obtained Co-doped ZnO-MCs was tested against the bacterial strains of gram-negative (Escherichia coli, Klebsiella pneumonia) and gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes) via the agar well diffusion method. The zones of inhibition (ZOI) for Co-doped ZnO-MCs against E. coli and K. pneumoniae were found to be 17 and 19 mm, and 15 and 16 mm against S. Aureus and S. pyogenes, respectively. The prepared Co-doped ZnO-MCs were thus established as a probable antibacterial agent against gram-negative bacterial strains.     

Antibacterial and antioxidant activities of hydroalcoholic stem bark extract of Schotia latifolia Jacq

ObjectiveTo investigate the antibacterial and antioxidant activities of hydroalcoholic extract of Schotia latifolia (S. latifolia) bark commonly used in South Africa traditional medicine for the treatment of various ailments.MethodsThe antibacterial test and MIC was determined by using agar well diffusion and dilution methods respectively against eight strains of bacteria. The total phenol, proanthocyanidin and flavonoid contents of S. latifolia were assessed using standard methods. The antioxidant activity of the extract was evaluated using ferric reducing power and the free radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2’-azino-bis-3-ethylbenzothiazoline-6-sulfonic-acid (ABTS), nitric oxide (NO), hydrogen peroxide (H₂O₂) and lipid oxidation (LO).ResultsThe antibacterial activity demonstrated an appreciable effect against all the gram positive bacteria at MIC between 0.016 and 10 mg/mL while that of gram negative bacteria was above 10 mg/mL. The plant extract exhibited high concentration of proanthocyanidin [(300.00±0.10) mg CE/g], followed by flavonoid [(12.46±0.04 mg) TE/g] and phenol [(11.06±0.03) mg QE/g] contents. Similarly, the extract at 0.5 mg/mL scavenges DPPH, ABTS, H₂O₂, LO and NO by 87.55%, 89.47%, 77.15%, 86.48% and 77.75% of the radicals respectively. The reducing power was also found to be concentration dependent.ConclusionsOur data suggest that S. latifolia extract has antibacterial and antioxidants activity and thus could be used as alternative therapy against antibiotic resistance bacteria and to prevent many radical related diseases.     

Antimicrobial constituents from three endophytic fungi

ObjectiveTo evaluate the antimicrobial potential of extracts of the endophytic fungi Plectophomella sp., Physalospora sp., and Crataegus monogyna (C. monogyna) and study the tentative identification of their active constituents.MethodsCrude extracts and isolated compounds were screened for antimicrobial activity using the agar well diffusion method. Four compounds were purified from three endophytic fungi using column chromatography and their structures have been assigned based on their ¹H and ¹³C nuclear magnetic resonance spectra.ResultsPlectophomella sp., Physalospora sp., and C. monogyna extracts showed promising antifungal, antibacterial and herbicidal properties. (-)-Mycorrhizin A was isolated from Plectophomella sp. while cytochalasins E and K were isolated from Physalospora sp. Similarly radicinin was purified from the endophytic fungus C. monogyna. The ethyl acetate extract of Plectophomella sp. showed significant antifungal activity towards Ustilago violacea (U. violacea) and Eurotium repens (E. repens) and significant antibacterial activity against Bacillus megaterium. Interestingly, the ethyl acetate extracts of Physalospora sp. and C. monogyna showed strong herbicidal and antifungal activities towards Chlorella fusca, U. violacea, E. repens, Mycotypha microspora (M. microspora), Fusarium oxysporum, Escherichia coli, and Bacillus megaterium. (-)-Mycorrhizin A showed significant antifungal activity towards U. violacea and E. repens. Cytochalasins E and K showed strong antifungal activity against E. repens and M. microspora especially towards fungal Mycotypha microspora. Similarly cytochalasins E and K showed good herbicidal activity towards Chlorella fusca. Radicinin showed strong antifungal activity against E. repens and M. microspora.ConclusionsAntimicrobial activities demonstrated by the extracts of the endophytic fungi Plectophomella sp., Physalospora sp., and C. monogyna and four isolated compounds clearly demonstrate that these fungi extracts and active compounds present a great potential use in the food, cosmetic and pharmaceutical industries.     

Isolation and identification of bioactive antibacterial components in leaf extracts of Vangueria spinosa (Rubiaceae)

ObjectiveThe column chromatographic fraction of ethyl acetate (EA1, EA2, EA3, EA4 and EA5) leaf extracts of Vangueria spinosa (V. spinosa) were screened for antibacterial activity and phytochemical analysis.MethodsEA3 fraction was isolated and identified by column chromatography, thin layer chromatography, spectral data analysis and phytochemical screening were used for analysis.ResultsEA3 fraction was significantly active at 4 to 64 mg/L against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa with minimum inhibitory concentration of 1.5625 to 3.1250 mg/mL. The active fraction (EA3) revealed the presence of flavonoid with retention factor value (R_f) of 0.39. The active antibacterial agent in the most potent fraction (EA3) was isolated and identified as flavonoid (?)–epicatechin–3–O–β–glucopyranoside by thin layer chromatography (TLC) and phytochemical screening. EA1 and EA2 show inhibitory activity at 4 to 64 mg/L against Staphylococcus aureus only where as fraction EA4 and EA5 do not shows any inhibitory activity within that range of concentration against any bacteria.ConclusionsThe results support the ethnomedicinal use of leaf of V. spinosa for the treatment of bacterial diseases.     

Green synthesis of titanium dioxide nanoparticles using Psidium guajava extract and its antibacterial and antioxidant properties

Objective:To determine the efficacies of antibacterial and antioxidant activities of aqueous leaf extract of Psidium guajava mediated biosynthesis of titanium dioxide nanoparticles(TiO_2,NPs).Methods:Synthesized TiO_2 NPs were tested by disc diffusion method against against human pathogenic bacteria.The total antioxidant activity and phenolic content(Folin—Ciocalteau method) of synthesized TiO_2 NTs and aqueous plant extract were determined.The scavenging radicals were estimated hv DPPH method.The synthesized TiO_2 NPs were characterized by XRD,FTIR.FESEM and EDX,Results:FTIR spectra of synthesized TiO_2 NPs exhibited prominent peaks at 3410 cm~(-1)(alkynes),1 578 cm~(-1).1 451 cm~(-1)(alkanes),and 1 123 cm~(-1)(C-O absorption).The morphological characterization of synthesized TiO_2 NPs was analysed by FESEM which showed spherical shape and clusters with an average size of 32.58 nm.The maximum zone of inhibition was observed in the synthesized TiO_2 NPs(20 μg/mL) against Staphylococcus aureus(25 mm) and Escherichia coli(23 mm).The synthesized TiO_2 NPs showed more antibacterial activity than the standard antibiotic disk,tetracycline which drastically reduces the chances for the development of antibiotics resistance of bacterial species.The plant aqueous extract and synthesized TiO_2NPs were found to possess maximum antioxidant activity when compared with ascorbic acid.The content of phenolic compounds(mg/g) in Leaf aqueous extract and synthesized TiO_2 NPs were found to be 85.4 and 18.3 mgTA/g,respectively.Conclusions:Green synthesized TiO_2 NPs provides a promising approach can satisfy the requirement of large-scale industrial production hearing the advantage of low—cost,eco—friendly and reproducible.     

Phytochemical screening and comparative antimicrobial potential of different extracts of Stevia rebaudiana Bertoni leaves

ObjectiveTo evaluate in vitro antimicrobial potential and phytochemical screening of the crude extracts of leaves of Stevia rebaudiana Bertoni.MethodsThe essential oil and crude extracts were prepared by using different usual method. Antimicrobial and antifungal activities were measured by the well established methods.ResultsHighest antifungal index [(12.13±0.08) mm)] and lowest antifungal index [(9.13±0.04) mm] as well as highest antibacterial index [(11.89±0.07) mm] and lowest antibacterial index [(7.24±0.03) mm] were obtained for extracts B, H, A and F, respectively. Invariably extract C, E, I, J and H did not show antimicrobial activity. The extract F showed all antifungal and antibacterial activity except Bacillus cereus and Bacillus megaterium.ConclusionsThe above findings support the idea that plant extracts of Stevia rebaudiana Bertoni leaves may have a role to be used as pharmaceuticals or preservatives.     

Impact of floral sources and processing on the antimicrobial activities of different unifloral honeys

Objective

To study in vitro antibacterial activity and physicochemical properties of three unifloral honeys (citrus, clover and cotton honeys), and to study the impacts of storage, dilution with water (33%, w/v) and autoclaving (121 °C for 15 min) on honeys characteristics.

Methods

Honey samples from monofloral sources including citrus (Citrus spp.), Egyptian clover (Trifolium alexandrium) and cotton (Gossypium vitifolium) were obtained during three successive seasons (2010-2012). Physicochemical properties and antimicrobial activities of different honey samples were studies.

Results

In honey samples stored for 12 or 24 month, colour, hydroxymethyl furfural and acidity increased, while refractive index, water activity, total soluble solids, electrical conductivity and pH remained relatively unaffected, but H₂O₂ values decreased. Types of honey exhibited various degrees of antibacterial activity against different indicator bacteria, wherein the highest antibacterial activity was recorded for clover honey followed by citrus and cotton honeys, respectively. Different species of bacteria were differed in their sensitivity to honey, wherein Salmonella enteritidis was the most sensitive followed by Staphylococcus aureus, Listeria monocytogenes and Escherichia coli, respectively. Storage up to 24 months at room temperature slightly reduced the antibacterial activity. The reduction levels were about 2.6% and 4.6% after 12 and 24 months, respectively. Diluting honeys with water increased the antibacterial activity by ca. 8.3%, while autoclaving decreased the antibacterial activity by ca. 13.5%. The relative contribution of the peroxide and non-peroxide components in the total antibacterial activity of fresh honeys was investigated. The antibacterial activity of honeys was mainly attributed to non-peroxide antibacterial agents, wherein their contribution was ca. 88%, while the contribution of H₂O₂ was only 12%. The contribution of the thermostable antibacterial components in honey was ca. 86.8%. The antibacterial activity of the fresh clover honey was compared with the effect of 16 antibiotics on indicator bacteria. Clover honey exhibited antibacterial activity comparable to that exhibited by the tested antibiotics. Moreover, antibacterial activity of water diluted fresh clover honey was higher compared to some of tested antibiotics. Clover honey appeared to deserve further investigations, since it may prove to be a promise therapeutic honey.

Conclusions

Honey samples tested in this study exhibited antibacterial activity against tested pathogenic bacteria, and this activity was mainly due to non-peroxide antibacterial factors. Clover honey appeared to deserve further investigations, since it may prove to be a promising therapeutic honey.     

Ferricenium complexes: A new type of water-soluble antitumor agent

Summary The antitumor activity of a series of iron complexes, i.e., of ferrocene [Cp₂Fe], of tetrachloroferrates(III) [R₄N]⁺[FeCl₄]^-, and of ferricenium complexes [Cp₂Fe]⁺X^- (X^-=[FeCl₄]^-, 1/2[Cl₃FeOFeCl₃]^2-, [H₅Mo₇O₂₄]^-·2H₂O, [2,4,6-(NO₂)₃C₆H₂O]^-, or [CCl₃COO]^-·2 CCl₃COOH) was investigated against EAT in CF1 mice. Whereas ferrocene and the ammonium tetrachloroferrates(III) did not show recognizable tumor-inhibiting activity, such activity was exhibited by the water-soluble, salt-like ferricenium complexes; the best antineoplastic properties, with optimum cure rates of 100%, were found for ferricenium picrate and ferricenium trichloroacetate.The ferricenium compounds are the first iron complexes for which antineoplastic activity has now been shown. They represent a new type of antitumor agent insofar as they differ fundamentally from known inorganic and organometallic antitumor agents (a) by their ionic, salt-like character, which is responsible for their high water solubility, and (b) by the absence of a cis-dihalometal moiety; this moiety has been recognized as important for the intracellular action of other known inorganic cytostatics.Abbreviations Cp C₅H₅, cyclopentadienyl ring ligand - EAT Ehrlich ascites tumor - IP intraperitoneal(ly) - p.t.t. post transplantationem tumoris Supported by the Fonds der Chemischen Industrie and by Council, University of the Witwatersrand     

Evaluation of wound healing and antimicrobial potentials of Ixora coccinea root extract

ObjectiveTo evaluate the wound healing and antimicrobial activity of root extracts of Ixora coccinea (I. coccinea).MethodsTo investigate the wound healing efficacy of root extract of I. coccinea Linn, five groups of animals were divided each containing six animals. Two wound models including incision and excision wound models were used in this study. The parameters studied were tensile strength on incision wound model and in terms of wound contraction for excision wound model were compared with standard Nitrofurazone (NFZ) ointment (0.2% w/w). Six extracts (ethanol, aqueous, petroleum ether, benzene, chloroform and ethyl acetate) of I. coccinea were screened for in vitro growth inhibiting activity against different bacterial strains viz, Staphylococcus aureus, Bacillus pumilius, Enterococcus faecalis, Escherichia coli, Salmonella typhi and Pseudomonas aeruginosa and fungi Candida albicans and Aspergillus niger were compared with the standard drugs ciprofloxacin and chloramphenicol for antibacterial and griseofulvin for antifungal screening. The serial dilution and cup (or) well plate methods were used for the antimicrobial study and MIC was determined.ResultsThe ethanolic extract showed significant (P<0.001) wound healing activity when compared to standard drug NFZ with respect to normal control group. Amongst all, ethanolic extract showed highly significant antibacterial activity against all bacterial strains used in this study when compared to standard. The aqueous extract showed moderate significant inhibition against all bacterial strains when compared to standard. All the extracts were shown negligible activity against the fungal strains used in this study.ConclusionsThe ethanolic root extract of I. coccinea showed pronounced wound healing and antibacterial activity. The probable reason to heal the wound was that the external application of the extract prevented the microbes to invade through the wound thus the protection of wound occurs against the infection of the various organisms.     

Antimicrobial chemical constituents from endophytic fungus Phoma sp.

Objective:To evaluate the antiniicrobial polenlial of different extracts of the endophytic fungus Phoma sp.and the tentative identification of their active constituents.Methods:The extract and compounds were screened for antimicrobial activity using the Agar Well Diffusion Method.Four compounds were purified using column chromatography and tlieir structures were assigned using～1H and～(13)C NMR spectra,DEPT,2D COSY,HMQC and HMBC experiments.Results:The ethyl acetate fraction of Phoma sp.showed good antifungal,antibacterial,and algicidal properties.One new dihydrofuran derivative,named phomafuranol(1),together with tliree known compounds,phomalacton(2),(3R)-5-hydroxymellein(3)and emodin(4)were isolated from the ethyl acetate fraction of Phoma sp.Preliminary studies indicated that phomalacton(2)displayed strong antibacterial,good antifungal and antialgal activities.Similarly(3R)-5-hydroxymellein(3)and emodin(4)showed good antifungal,antibacterial and algicidal properties.Conclusions:Antimicrobial activities of the ethyl acetate fraction of the endophytic fungus Phoma sp.and isolated compounds clearly demonstrate that Phoma sp.and its active compounds represent a great potential for the food,cosmetic and pharmaceutical industries.     

Preliminary phytochemical analysis, antibacterial, antifungal and anticandidal activities of successive extracts of Crossandra infundibuliformis

ObjectiveTo investigate the phytochemical, antibacterial, antifungal and anticandidal activity of successive extracts of Crossandra infundibuliformis (Acanthaceae) leaves.MethodsPreliminary screening on the presence of alkaloids, saponins, phytosterols, phenolic compounds, flavanoids, tannins, carbohydrates, terpenoids, oils and fats were carried out by phytochemical analysis. The antibacterial, antifungal and anticandidal activities were done by agar well diffusion technique.ResultsThe successive extracts have an array of chemical constituents and the MIC values of antibacterial activity ranges from 0.007 8 to 0.015 0 μg/mL. In case of antifungal and anticandidal activities the MIC values were between 0.125 and 0.250 μg/mL.ConclusionsThese findings demonstrate that the leaf extracts of C. infundibuliformis presents excellent antimicrobial activities and thus have great potential as a source for natural health care products.     

Synthesis,Crystal Structure and Luminescent Property of Mg(II) Complex with N-Benzenesulphonyl-L-Leucine and 1,10-Phenanthroline

A new complex [Mg(L)₂(phen)(H₂O)₂](phen)(H₂O)₂ [L= N-benzenesulphonyl-L-leucine] was synthesized by the reaction of magnesium chloride hexahydrate with N-benzenesulphonyl-L-leucine and 1,10-phenanthroline in the CH₃CH₂OH/H₂O (v:v = 5:1). It was characterized by elemental analysis, IR and X-ray single crystal diffraction analysis. The crystal of the title complex [Mg(L)₂(phen)(H₂O)₂](phen)(H₂O)₂ belongs to triclinic, space group P-1 with a = 0.72772(15) nm, b = 1.4279(3) nm, c = 1.4418(3) nm, α = 63.53(3)°, β = 79.75(3)°, γ = 81.83(3)°, V = 1.3163(5) nm³, Z =1, D_c= 1.258 μg·m⁻³, μ = 0.177 mm⁻¹, F(000) = 526, and final R₁ = 0.0506, ωR₂ = 0.1328. The complex comprises a six-coordinated magnesium(II) center, with a N₂O₄ distorted octahedron coordination environment. The molecules are connected by hydrogen bonds and π-π stacking to form one dimensional chain structure. The luminescent property of the Mg(II) complex has been investigated in solid.