Natural plant extracts mediated expression regulation of TGF-ß receptors and SMAD genes in human cancer cell lines.

BACKGROUND: Transforming growth factor beta (TGF-ß) superfamily has key role in cell proliferation which leads to tumor promoting activities at metastatic stage of cancer. Inhibition of transforming growth factor beta receptor (TGFßR) signaling pathway can provide better therapeutic strategy to control cancer. Natural products are best known for their safety, less toxic nature, antioxidant characteristics making them a promising candidate to inhibit TGFßR signaling pathway. METHODS AND RESULTS: Crude methanolic extracts (CMEs) of 16 selected plants were prepared by using maceration method and subjected to phytochemical assays for identification of major phytometabolites particularly cancer chemopreventive antioxidant constituents. Total flavonoid content of all plants CME was > 0.6 mg/ml exhibiting the Cichorium intybus contains comparatively highest amount of total flavonoid content (0.53 mg/ml). Scanvenging activity of all plants was determined having IC50 ranges between 2 and 88 (µg/ml) while Moringa oleifera revealed the maximum scavenging activity (IC50 2.03 µg/ml). Comparative cytotoxicity of plant extracts was evaluated in HUH and MCF-7 cell lines using 3-(4,5-Dimethylthiazol-2-Yl)-2,5-Diphenyltetrazolium Bromide (MTT) colorimetric assay. The nine active plant extracts i.e. Fagonia cretica, Argemone Mexicana, Rubus fruticosus, M. oleifera, Punica granatum, Cichorium intybus, Xanthium strumarium, Carissa opaca, Cyperus rotundus were identified based on their high antiproliferative activity > 50% against cancer cell lines and subjected to relative expression studies. Modulation of TGFß signaling molecules (i.e.TGFßR1, 2 & 3, SMAD3, SMAD5) and ubiquitous proteins i.e. SMURF1 and SMURF2 genetic expression by potent extracts was determined by RT-PCR using GAPDH (housekeeping gene) as gene of reference. CONCLUSIONS: This present study revealed that CME of Fagonia cretica and Argemone mexicana significantly inhibit TGF beta mediated signaling cascade by downregulating the gene expression fold change > 1 of TGFßR 1, 2 & 3 and receptor associated complex protein SMAD3 as compared to control.

Exogenous Application of Green Titanium Dioxide Nanoparticles (TiO2 NPs) to Improve the Germination, Physiochemical, and Yield Parameters of Wheat Plants under Salinity Stress.

Agriculture is the backbone of every developing country. Among various crops, wheat (Triticum aestivum L.) belongs to the family Poaceae and is the most important staple food crop of various countries. Different biotic (viruses, bacteria and fungi) and abiotic stresses (water logging, drought and salinity) adversely affect the qualitative and quantitative attributes of wheat. Among these stresses, salinity stress is a very important limiting factor affecting the morphological, physiological, biochemical attributes and grain yield of wheat. This research work was carried out to evaluate the influence of phytosynthesized TiO2 NPs on the germination, physiochemical, and yield attributes of wheat varieties in response to salinity. TiO2 NPs were synthesized using TiO2 salt and a Buddleja asiatica plant extract as a reducing and capping agent. Various concentrations of TiO2 nanoparticles (20, 40, 60 and 80 mg/L) and salt solutions (NaCl) (100 and 150 mM) were used. A total of 20 mg/L and 40 mg/L improve germination attributes, osmotic and water potential, carotenoid, total phenolic, and flavonoid content, soluble sugar and proteins, proline and amino acid content, superoxide dismutase activity, and reduce malondialdhehyde (MDA) content at both levels of salinity. These two concentrations also improved the yield attributes of wheat varieties at both salinity levels. The best results were observed at 40 mg/L of TiO2 NPs at both salinity levels. However, the highest concentrations (60 and 80 mg/L) of TiO2 NPs showed negative effects on germination, physiochemical and yield characteristics and causes stress in both wheat varieties under control irrigation conditions and salinity stress. Therefore, in conclusion, the findings of this research are that the foliar application of TiO2 NPs can help to improve tolerance against salinity stress in plants.

Correlation of C-reactive protein levels, gene polymorphism and platelets count in Dengue infection.

OBJECTIVE: To determine the correlation of polymorphism in C-reactive protein gene with variation in serum levels in dengue patients. METHODS: The cross-sectional study was conducted at Pir Mehr Ali Shah Arid Agriculture University, Rawalpindi, Pakistan, from October 2017 to October 2018, and comprised blood samples from dengue patients which were used to measure the serum levels of C-reactive protein. Deoxyribonucleic acid extraction followed by tetra amplification-refractory mutation system polymerase chain reaction was used to analyse the genotype variation T>G for single nucleotide polymorphism rs199953854 using allele-specific primers. Correlation of serum C-reactive protein levels with the C-reactive protein polymorphism in dengue patients was explored. Data was analysed using SPSS 21. RESULTS: Of the 200 patients, 108(54%) had very high C-reactive protein levels, 48(24%) had levels slightly higher than the upper limit, 14(7%) had low and 30(15%) had normal levels. Also, 162(81%) patients had low platelets count. Amplification of only T alleles was noted. CONCLUSIONS: C-reactive protein levels were found to be increased with suppressed platelets count in dengue patients. Single nucleotide polymorphism rs199953854 appeared to have no polymorphism.

Bioactivity evaluation and HPLC UV-VIS based quantification of antioxidant secondary metabolites from extract and fractions of Bistorta amplexicaulis rhizome.

Bistorta amplexicaulis is a popular medicinal plant and reported as rich source of antioxidant compounds. The present study was designed for antioxidant and anticancer potential of polarity based fractions of B. amplexicaulis and its correlation to the secondary metabolites quantified by HPLC-UV/VIS.Crude extract was prepared by maceration method and polarity based fractions were prepared by solvent-solvent extraction. Antioxidant and anticancer potential was investigated by using various physiological and non-physiological assays while secondary metabolites rutin, naringin and quercetin present in extract and fractions were quantified by using HPLC- UV/VIS. All extracts showed Antioxidant potential but highest activity was obtained with ethyl acetate fraction (DPPH IC50 5.76±0.03 µg/ml, ABTS IC50 0.74±0.1 µg/ml, Total Antioxidant Assay 72.55±0.098 Ascorbic acid equivalents, Super oxide radical scavenging assay IC506.86±0.1909 µg/ml, Hydroxyl radical scavenging assay IC50 0.96±0.1690 µg/ml). The cytotoxicity of fractions against HepG2 cell lines showed lowest ell viability in n-hexane fraction (11%). The results revealed that ethyl acetate fraction of B. amplexicaulis can be a potential source of novel antioxidant compounds while n hexane fraction could provide anticancer compounds. A new method of simultaneous quantification of three flavonoids by using UV/VIS detector is reported in this study.

Knowledge, attitude and practices (KAP) of the families of b-thalassaemia children in thalassaemia centers of Rawalpindi and Islamabad, Pakistan.

The present study was designed to assess the Knowledge, Attitude and Practices (KAP) of the parents of b-thalassaemia children (410) selected from public (73.2%) and private (26.8%) thalassaemia centers of Rawalpindi-Islamabad. Qualitative and quantitative approaches were used to collect the data, which was analyzed by using SPSS. Majority of the respondents (70%) were rural young parents with no knowledge of thalassaemia before marriage. However, now 81.2% were aware about this. Majority of the respondents (89%) had the knowledge about premarital screening, 86.1% were opposed to intermarriages of carrier and 57% believed that if carrier got married then prenatal diagnosis or Chorionic villus sampling test is necessary. About 76.8% of the couples were screened and 42.2% had an experience of Chorionic villus sampling among which 20% abortions were reported. Overall 82% parents had received genetic counselling. The present study suggests that parent's regular visits and genetic counseling at thalassaemia centers have played important role about awareness.

Effect of leaf extracts of Taraxacum officinale on CCl4 induced hepatotoxicity in rats, in vivo study.

Taraxacum officinale L is a medicinal plant, which has enormous medicinal values against various types of liver disorders and it has traditionally been used for the treatment of liver problems by people from the South East Asia. Previously we have screened the crude methanolic extract of T. officinale against cytotoxicity induced by CCl4. Present study was designed to compare the protective effect of ethanolic and n-hexane extract of leaves in carbon tetrachloride (CCl4) induced liver toxicity in rats. The extract (200 mg/kg and 400mg/kg body weight) along with silymarin (100 mg/kg) a standard drug was administered to experimental animals. It was observed that ethanolic plant extract has significantly reduced the negative effect of CCl4 as compared to n-hexane extract and effect of extract was increased with increasing dose level. Although both leaf extracts decreased the concentration of TBARS, H2O2 and nitrite contents which enhance due to CCl4 toxicity but effect was higher in ethanolic extract. The results clearly indicated that Taraxacum officinale ethanolic leaves extract has better protective effect against CCl4 induced liver tissues toxicity. This claim was also supported by histopathological results obtained during this study and this might be due to presence of various polar phytochemicals that might be more prevent in this extract.

Prediction of Nili-Ravi buffalo bull fertility through Fourier harmonic analysis of sperm.

Fourier harmonic analysis (FHA) is a robust method for identification of minute changes in sperm nuclear shape that are indicative of reduced fertility. The current study was designed to develop a fertility prediction model for Nili-Ravi buffalo bulls through FHA of sperm. In experiment I, FHA technique was standardized, average sperm nuclear perimeter was measured and sperm nuclear shape plot of buffalo bull was constructed. Sperm of buffalo bulls (n = 10) were stained with YOYO-1 and Hoechst-33342 to differentiate live and dead, and digital images were captured using phase contrast and fluorescent microscopy. The images were analyzed by ImageJ software and 100 sperm/bull were evaluated. The results are described as mean ± SEM values of mean harmonic amplitude (mharm), skewness harmonic amplitude (skharm), kurtosis harmonic amplitude (kurharm) and variance harmonic amplitude (varharm) at Fourier frequencies 0-5 along with the cartesian and polar coordinate plots of buffalo bull sperm. In experiment II, a fertility prediction model was developed based on FHA of buffalo bull sperm. Semen samples of low (n = 6), medium (n = 3) and high (n = 8) fertility bulls were investigated for FHA of sperm and harmonic amplitudes (HA) were generated. Firstly, to determine if live and dead sperm population have unique nuclear shape distribution; the mean, skewness, kurtosis and variance HA 0-5 of 1700 live and 1294 dead spermatozoa of 17 bulls were evaluated. T-test signified a difference in the mharm0 (2.363 ± 0.01 vs. 2.439 ± 0.02), skharm0 (-0.0002 ± 0.07 vs. -0.266 ± 0.09), kurharm0 (-0.156 ± 0.07 vs. 0.260 ± 0.18), kurharm2 (0.142 ± 0.11 vs. 1.031 ± 0.32) and varharm4 (0.109 ± 0.00 vs. 0.082 ± 0.00) of live vs. dead sperm population (p < 0.05). Therefore, 100 live sperm/bull were further evaluated for mean, skewness, kurtosis and variance HA 0-5 values among high (n = 6) and low-fertility (n = 6) groups. Results of T-test showed higher values of mharm2 (0.739 ± 0.01 vs. 0.686 ± 0.00), mharm4 (0.105 ± 0.001 vs. 0.007 ± 0.001), and skharm0 (0.214 ± 0.109 vs. -0.244 ± 0.097) in high vs. low-fertility group (p < 0.05). In next step, five significantly different combinations of discriminant measures between high and low-fertility groups were obtained by discriminant analysis. In conclusion, mharm4, skharm0 and varharm2 correctly identified 91.7 % of bulls into their respective fertility groups, and upon cross validation the value of the canonical correlation was 0.928.

TRAIL mediated apoptosis ruling and anticancer trigger by fine-tuned nano spheres of Fagonia cretica methanolic extracts as novel cancer regime.

Fagonia cretica L. is a tropical plant of family Zygophyllaceae with wide range of medicinally important secondary metabolites. The low cellular uptake of the polar compounds in the extract of the plant limits its biological application. In present study efficacy of F. cretica modified bioactive nano-formulations for in vitro modulation of TRAIL mediated extrinsic apoptotic pathway as cancer therapy was investigated. F. cretica methanolic extracts were formulated at nano-scale for green synthesis of silver nanoparticles, albumin conjugation and liposomes encapsulation to enhance targeted bioactivity against cancer. Physical characterization of the synthesized nanoparticles was done by SEM, EDX and Zeta potential analyzer. In vitro cell viability assay MTT was done for MCF-7, Hep-2, HUH-7 and HCEC cell lines. Relative expression variation of the apoptotic pathway-associated genes was done by qRT-PCR. SEM revealed spherical shape of 56.62 ± 8.04, 143 ± 11.54 and 83.36 ± 38.73 nm size and zeta potential - 18.6, - 15.5 and - 18.3 mV for liposomes, silver and albumin nanoparticles. Silver nanoparticles showed highest anticancer activity in vitro than albumin and liposomes nanoparticles with IC50 0.101 ± 0.004, 0.177 ± 0.03 and 0.434 ± 0.022 mg/mL in MCF-7, Hep-2 and HUH-7 respectively. F. cretica albumin and silver nanoparticles upregulated the in vitro TRAIL, DR4, DR5 and FADD gene expression at statistically significant levels in Hep-2 cell lines. Nano-formulations of F. cretica proved therapeutically important biomolecules in vitro. The hypothesized modulation of extrinsic apoptosis pathway genes through the plant nanoparticles proved novel medicinal options for effective treatment of cancer and enhancing the bioavailability of the active plant metabolites.

Nutraceutical profiling of elite onion germplasm and breeding hybrids with improved nutraceutical quality.

Onion (Allium cepa L) is a major reservoir of important nutraceutical ingredients. Herein, nutraceutical profiling of elite germplasm was assessed and hybrids with improved nutraceutical quality were selected. The nutraceutical components were screened through Fourier Transform Infrared Spectroscopy (FTIR) analysis (scan range 4000-400cm-1) followed by spectrophotometric/colorimetric quantification in oven dried bulb samples. Line × Tester (L×T) analysis was used to identify potential hybrids with better nutraceutical quality. Based on common functional groups obtained from FTIR analysis, as well as bulb color, the onion genotypes were categorized into six groups viz., white, yellowish brown, light brown, dark brown, brown and purplish brown. Results indicated that the purplish brown, yellowish brown and dark brown genotypes had maximum concentration of pyruvic acid, total flavonoids and total phenolic content, while vitamin C content showed weak association with color pigmentation. The onion variety 'Onion Swat' contained the highest level of pyruvic acid (17.18 µM) and 'MKS8823GO' had the highest vitamin C content (13.83mg/100mL). The L×T analysis revealed that out of 35 crosses, 'MKS-77127 × Onion Swat' and 'MKS-77127 × MKS777' were the best hybrids with improved nutraceutical quality. Further, observations for specific combining ability, general combining ability, genetic versus environmental variance, heritability and heterosis indicated that the studied parameters were genetically inherited and could be improved significantly by adopting an appropriate breeding strategy.

Designing of pretreatment filter technique for reduction of phenolic constituents from olive-mill wastewater and testing its impact on wheat germination.

Olive oil extraction produces a great volume of olive mill wastewater (OMW), which is considered a serious ecological challenge. In this study, we have designed and tested a trickling filter consisting of seven different layers of natural material, including (coarse gravel, fine gravel, lime (Ca (OH)2), sand (SiO2), carbon char, sponge/mesh), to treat OMW. The filter process involved physical separation, filtration, coagulation and adsorption with the removal of COD (69.8%), BOD (40.2%), Phenolic contents (90%), pH (41%), EC (41.6%) and total suspended solids (TSS) (69%). Our results have shown that treated OMW has a high potential oxidant activity. T7, Untreated OMW at 1:6 dilutions, had the strongest correlation (i.e. 0.97), while untreated OMW had the lowest IC50 (7.62 g ml-1), which shown the best DPPH radical scavenging capabilities. While pure Untreated OMW has the maximum radical scavenging activity, 63%, treated (1:6) diluted OMW exhibits the lowest value i. e 9% when phosphomolybdate assay was done. HPLC analysis showed that the trickling filter removed the vanillic acid, caffeic acid and reduced the contents of phenolic components such as gallic acid, hydroxytyrosol, vanillin, quercetin and catechol. Filtered OMW was also tested for its germination efficacy at various dilutions (1:0, 1:2, 1:4, 1:6). A remarkable improvement in germination percentage, germination index, seedling length, seedling vigor index, promptness index, stress tolerance index (76.7%, 68.4%, 51.7%, 82.1%, 54.8%, and 66.7%, respectively) has shown the efficiency of treated OMW at 1:6 dilutions. The results from this study show the efficiency of our filter design which can be further used.

Titanium dioxide nanoparticles elicited agro-morphological and physicochemical modifications in wheat plants to control Bipolaris sorokiniana.

The current study involves the biogenesis of titanium dioxide nanoparticles (TiO2 NPs) by using Moringa oleifera Lam. aqueous leaf extract for the reduction of titanium dioxide salt into TiO2 nanoparticles. The biosynthesized TiO2 nanoparticles were observed by using the UV-visible spectrophotometry, SEM, EDX and XRD analytical methods. It was confirmed that the nanoparticles are crystalline and exist in the size range of 10-100 nm. The FTIR analysis confirmed the presence of O-H (hydrogen bonding), N-H (amide), C-C (alkanes) and C-I (Iodo-stretch) functional groups responsible for the stabilization of nanoparticles. Various concentrations (20, 40, 60 and 80 mg/L) of TiO2 NPs were applied exogenously on wheat plants infected with a fungus Bipolaris sorokiniana responsible to cause spot blotch disease at different time intervals. The measurement of disease incidence and percent disease index showed the time-dependent response and 40 mg/L was reported a stable concentration of TiO2 NPs to reduce the disease severity. The effects of biosynthesized TiO2 NPs were also evaluated for agro-morphological (leaf and root surface area, plant fresh and dry weight and yield parameters), physiological (relative water content, membrane stability index and chlorophyll content) and non-enzymatic metabolites (soluble sugar, protein, soluble phenol and flavonoid content) in wheat plants under biotic stress and 40 mg/L concentration of TiO2 NPs was found to be effective to elicit modifications to reduce biotic stress. The current study highlights the significant role of biosynthesized TiO2 NPs in controlling fungal diseases of wheat plants and thus ultimately improving the quality and yield of wheat plants.

Structure elucidation and inhibitory effects of self-assembled organotin(IV) esters of p-tolyl acetic acid on bacterial, fungal, brine shrimp, and potato tumor cells.

Biologically active new organotin(IV) acetates (1-6) of p-tolyl acetic acid have been synthesized and characterized by multinuclear nuclear magnetic resonance ((1)H, (13)C) and mass spectrometry. The X-ray crystallographic data of compounds (3 and 4) were also collected. These studies show that in diorganotin(IV) compounds (compounds 1, 2, 3, and 6), tin exists in skew trapezoidal geometry with four strong and two weaker bonds, whereas triorganotin(IV) carboxylates (compounds 4 and 5) have four and five coordinated geometries in solution and solid form, respectively. These compounds were screened for a range of biological activities. Antibacterial activities were determined against six pathogenic bacterial strains, three Gram-positive and three Gram-negative; the activities were measured in terms of inhibition zones (mm). Antifungal activities were determined against six pathogenic fungal strains, cytotoxicity by the brine shrimp lethality assay, and antitumor activities by the crown gall tumor inhibition (potato disc) assay.

Optimization of soya lecithin and Tween 80 based novel vitamin D nanoemulsions prepared by ultrasonication using response surface methodology.

Vitamin D nanoemulsions were fabricated using ultrasonic homogenization approach. Response surface methodology (RSM) was used to optimize the preparation conditions for mixed surfactants (Soya lecithin and Tween 80; 2:3) based nanoemulsions. The effects of homogenization time (3.5-6.5 min), surfactant to oil ratio (0.43-0.78) and disperse phase volume (7-9%) on response variables were studied. Response Surface Methodology analysis results depicted that the polynomial model (second-order) can be used to predict response values. The coefficients of determinations were more than 0.90 for each response. The optimum emulsifying conditions for vitamin D nanoemulsions were 4.35 min homogenization time, 0.62 surfactant to oil ratio (S/O) and 7% disperse phase volume (DPV). Whereas, the experimental values for droplet size, droplet growth ratio (DGR) and vitamin D retention were 112.36 ±â€¯3.6 nm, 0.141 ±â€¯0.07 and 76.65 ±â€¯1.7% respectively. This research will be useful for the food and pharmaceutical industry to develop soya lecithin and Tween 80 based vitamin D delivery system for food additives and nutraceutical components.

Optimization of mixed surfactants-based ß-carotene nanoemulsions using response surface methodology: An ultrasonic homogenization approach.

In the present study, food grade mixed surfactant-based ß-carotene nanoemulsions were prepared without using any co-surfactant. Response surface methodology (RSM) along with central composite design (CCD) was used to investigate the effect of independent variables (surfactant concentration, ultrasonic homogenization time and oil content) on response variables. RSM analysis results revealed that experimental results were best fitted into a quadratic polynomial model with regression coefficient values of more than 0.900 for all responses. Optimized preparation conditions for ß-carotene nanoemulsions were 5.82% surfactant concentration, 4 min ultrasonic homogenization time and 6.50% oil content. The experimental values at optimized preparation conditions were 119.33 nm droplet size, 2.67p-Anisidine value and 85.63% ß-carotene retention. This study will be helpful for the fortification of aqueous products with ß-carotene.

Effect of silver nanoparticles and silver nitrate on growth of rice under biotic stress.

This study was organised to check the effect of silver nanoparticles and silver nitrate on rice growth against biotic stress. Silver nanoparticles were synthesised by using plant extract as reducing agent, followed by characterisation through UV Vis spectroscopy, XRD, EDS and SEM. Aspergillus application significantly reduced rice plant fresh mass (0.9%), dry mass (0.21%), root length (2.3%), shoot length (5.2%) and root number (1%) in comparison to control. Similarly, leaf area, leaf fresh mass, dry mass and leaf number were also reduced by 23.1, 0.02, 0.11 and 0.9%, respectively. AgNPs and AgNO3 treatments increased the root length (16.2 & 12.8%), shoot length (21 & 20%), root number (8.1 & 6.8%), plant fresh weight (6.4 & 5%) and plant dry weight (4.6 & 3.5%) in 75mg/l treatment of AgNPs and AgNO3 respectively. Similarly, AgNPs and AgNO3 treatment (75 mg/l concentrations) reflected remarkable increase in leaf area (58.8 & 57.2 %), leaf number (4.3 & 3.7 %), leaf fresh weight (1.7 & 1.4 %) and leaf dry weight (0.9 & 0.8 %). Overall AgNPs showed more significant results as compared to AgNO3. The quantity of aflatoxins ranged from 3.1 to 7.7 µg/kg against tolerable limit (4 µg/kg). Overall AgNPs and AgNO3 treatments showed significant results and it could be considered as a strategy for aflatoxin management in rice plants.

Natural Agents-Mediated Targeting of Histone Deacetylases.

In the past few years, basic and clinical scientists have witnessed landmark achievements in many research projects, such as those conducted by the US National Institutes of Health Roadmap Epigenomics Mapping Consortium, the International Human Epigenome Consortium, The Cancer Genome Atlas Network and the International Cancer Genome Consortium, which have provided near-complete resolution of epigenetic landscape in different diseases. Furthermore, genome sequencing of tumors has provided compelling evidence related to frequent existence of mutations in readers, erasers and writers of epigenome in different cancers. Histone acetylation is an intricate mechanism modulated by two opposing sets of enzymes and deeply studied as a key biological phenomenon in 1964 by Vincent Allfrey and colleagues. The research group suggested that this protein modification contributed substantially in transcriptional regulation. Subsequently, histone deacetylases (HDACs), histone acetyltransferases and acetyl-Lys-binding proteins were identified as transcriptional mediators, which further deepened our comprehension regarding biochemical modifications. Overwhelmingly increasing high-impact research is improving our understanding of this molecularly controlled mechanism; moreover, quantification and identification of lysine acetylation by mass spectrometry has added new layers of information. We partition this multi-component review into how both activity and expression of HDAC are targeted using natural agents. We also set spotlight on how oncogenic fusion proteins tactfully utilize HDAC-associated nano-machinery to modulate expression of different genes and how HDAC inhibitors regulate TRAIL-induced apoptosis in cancer cells. HDAC inhibitors have been reported to upregulate expression of TRAIL receptors and protect TRAIL from proteasomal degradation. Deeper understanding of HDAC biology will be useful for stratification and selection of patients who are responders, non-responders and poor-responders for HDACi therapy, and for the rational design of combination studies using HDACi.

Synthesis, chemical characterization and biological screening for cytotoxicity and antitumor activity of organotin (IV) derivatives of 3,4-methylenedioxy 6-nitrophenylpropenoic acid.

A series of mono-, di- and triorganotin compounds with general formulae [RSnL(2)Cl], R = Bu (compound 3), [R(2)SnL(2)], where R = Me, Et, Bu, Oct (compounds 1, 2, 4 and 6) and [R(3)SnL], where R = Bu, Cy and Ph (compounds 5, 7 and 8) and where L = 3,4-methylenedioxy-6-nitrophenylpropenoic acid have been prepared and characterized by elemental analysis, multinuclear ((1)H-, (13)C- and (119)Sn-) NMR and mass spectrometry. The ligand and its respective organotin complexes were screened for cytotoxicity using the brine shrimp lethality assay and for antitumor activity using the crown gall tumor inhibition (potato disc) assay. The bioassay results support the conclusion that the biological activities of these synthetic compounds are in the following order: [RSnL(2)Cl] < [R(2)SnL(2)] < [R(3)SnL].

Dimethyltin(IV) derivatives of biologically potent substituted phenylacrylic acids: synthesis, chemical characterization and inhibitory effects on Agrobacterium tumefaciens.

Effect of dimethyltin(IV) complexes of different substituted phenyl acrylic acids on the ability of Agrobacterium tumefaciens to cause tumours in plants was studied by using potato discs. The results demonstrated significant inhibition of tumours formation. All the compounds were synthesized and characterized by using analytical techniques, i.e. FTIR, multinuclear NMR ((1)H, (13)C, (19)F and (119)Sn) and mass spectrometry. These studies explain that dimethyltin(IV) derivatives exist in a deformed octahedral environment known as skew trapezoidal geometry with four strong and two weaker bonds.

Di- and triorganotin(IV) esters of 3,4-methylenedioxyphenylpropenoic acid: synthesis, spectroscopic characterization and biological screening for antimicrobial, cytotoxic and antitumor activities.

Nine biologically significant organotin(IV) esters of 3,4-Methylenedioxyphenylpropenoic acid (L) were synthesized with the general formulae [R2SnL2], where R includes Me(1), Et(3), But(4), Oct(5), Ph(8), and [R3SnL], in which R is Me(2), Cy(6), Ph(7), and But(9). The acid and its compounds were characterized by basic analytical techniques comprising elemental analysis, FTIR and mass spectrometry in solid state and by Multinuclear (1H, 13C and 119Sn) NMR in solution form, which provides some important information about the different coordination behaviors of metal in both solid and solution. Methylenedioxy moiety in these compounds enhances the biological activity of these compounds. These compounds were screened for a range of biological activities. Antibacterial activities were determined against six pathogenic bacterial strains, three gram-positive and three gram-negative, the activities were measured in terms of inhibition zones (mm). Results demonstrate that diorganotin derivatives are more active than triorganotin derivatives and ligand acid. Antifungal activity was determined against six pathogenic fungal strains, cytotoxicity by the brine shrimp lethality assay, and antitumor activity by crown gall tumor inhibition (potato disc) assay. Results for antifungal activity, cytotoxicity, and antitumor activity of these compounds demonstrate that triorganotin derivatives are more active than diorganotin derivatives and ligand. Finally, the results were compared with similar reports in the literature.