Structural and Property Characterizations of Dual-Responsive Core-Shell Tecto Dendrimers for Tumor Penetration and Gene Delivery Applications.

Core-shell tecto dendrimers (CSTDs) with excellent physicochemical properties and good tumor penetration and gene transfection efficiency have been demonstrated to have the potential to replace high-generation dendrimers in biomedical applications. However, their characterization and related biological properties of CSTDs for enhanced tumor penetration and gene delivery still lack in-depth investigation. Herein, three types of dual-responsive CSTDs are designed for thorough physicochemical characterization and investigation of their tumor penetration and gene delivery efficiency. Three types of CSTDs are prepared through phenylborate ester bonds of phenylboronic acid (PBA)-decorated generation 5 (G5) poly(amidoamine) (PAMAM) dendrimers as cores and monose (galactose, glucose, or mannose)-conjugated G3 PAMAM dendrimers as shells and thoroughly characterized via NMR and other techniques. It is shown that the produced CSTDs display strong correlation signals between the PBA and monose protons, similar hydrodynamic diameters, and dual reactive oxygen species- and pH-responsivenesses. The dual-responsive CSTDs are proven to have structure-dependent tumor penetration property and gene delivery efficiency in terms of small interference RNA for gene silencing and plasmid DNA for gene editing, thus revealing a great potential for different biomedical applications.

NMR Study on Laccase Polymerization of Kraft Lignin Using Different Enzymes Source.

The usage of laccases is a sustainable and environmentally friendly approach to modifying the Kraft lignin structure for use in certain applications. However, the inherent structure of Kraft lignin, as well as that resulting from laccase modification, still presents challenges for fundamental comprehension and successful lignin valorization. In this study, bacterial and fungal laccases were employed to modify eucalypt Kraft lignin. To evaluate the type and range of the chemical and structural changes of laccase-treated lignins, different NMR techniques, including solution 1H and 2D NMR (heteronuclear single quantum correlation (HSQC)), and solid-state 13C NMR, were applied. Size exclusion chromatography and infrared spectroscopy were also used. Interestingly, HSQC analysis showed substantial changes in the oxygenated aliphatic region of lignins, showing an almost complete absence of signals corresponding to side-chains due to laccase depolymerization. Simultaneously, a significant loss of aromatic signals was observed by HSQC and 1H NMR, which was attributed to a deprotonation of the lignin benzenic rings due to polymerization/condensation by laccase reactions. Then, condensed structures, such as α-5', 5-5', and 4-O-5', were detected by HSQC and 13C NMR, supporting the increment in molecular weight, as well as the phenolic content reduction determined in lignins.

Fast and simplified determination of PCA and aromatic carbon content of treated distilled aromatic extract (TDAE) by NMR.

Aromatic oils obtained during lubricant production (DAE) have high value as rubber extenders in tire manufacturing, but they have high carcinogenic potential due to the content of polycyclic aromatic compounds (PCAs). Legislation on PCA content requires additional treatment to reach treated oils (TDAE) with a PCA content lower than 3% according to the IP 346 method. IP 346 is a highly time-consuming and high uncertainty method, and several proposals have tried to replace it, but nowadays, there is no standard alternative. In this work, an extensive collection of samples covering a broad PCA content were obtained and characterized by physical properties, NMR, and aromatic and PCA content. Several correlations were tested to establish an optimum procedure to estimate the aromatic and the PCA content according to the requirement of high accuracy and low time and effort. The combination of several properties does not improve the accuracy of the correlation, and simpler equations were preferred. Integrated spectra appear as an acceptable characterization method as NMR percent of the total aromatic proton and polycyclic aromatic proton correlates satisfactory with the number of aromatic carbons and PCA content, respectively. The refractive index yields the best results for the correlation to PCA content. Obtained deviations compare favorably with methods previously described in the literature and with the uncertainty involved in the experimental method. They can be considered adequate methods to analyze such magnitudes routinely.

Bioactive Potential of Extracts of Labrenzia aggregata Strain USBA 371, a Halophilic Bacterium Isolated from a Terrestrial Source.

Previous studies revealed the potential of Labrenzia aggregata USBA 371 to produce cytotoxic metabolites. This study explores its metabolic diversity and compounds involved in its cytotoxic activity. Extracts from the extracellular fraction of strain USBA 371 showed high levels of cytotoxic activity associated with the production of diketopiperazines (DKPs). We purified two compounds and a mixture of two other compounds from this fraction. Their structures were characterized by 1D and 2D nuclear magnetic resonance (NMR). The purified compounds were evaluated for additional cytotoxic activities. Compound 1 (cyclo (l-Pro-l-Tyr)) showed cytotoxicity to the following cancer cell lines: breast cancer 4T1 (IC50 57.09 ± 2.11 µM), 4T1H17 (IC50 40.38 ± 1.94), MCF-7 (IC50 87.74 ± 2.32 µM), murine melanoma B16 (IC50 80.87 ± 3.67), human uterus sarcoma MES-SA/Dx5 P-pg (-) (IC50 291.32 ± 5.64) and MES-SA/Dx5 P-pg (+) (IC50 225.28 ± 1.23), and murine colon MCA 38 (IC50 29.85 ± 1.55). In order to elucidate the biosynthetic route of the production of DKPs and other secondary metabolites, we sequenced the genome of L. aggregata USBA 371. We found no evidence for biosynthetic pathways associated with cyclodipeptide synthases (CDPSs) or non-ribosomal peptides (NRPS), but based on proteogenomic analysis we suggest that they are produced by proteolytic enzymes. This is the first report in which the cytotoxic effect of cyclo (l-Pro-l-Tyr) produced by an organism of the genus Labrenzia has been evaluated against several cancer cell lines.

Discovery of Novel Imidazopyridine GSK-3ß Inhibitors Supported by Computational Approaches.

The interest of research groups and pharmaceutical companies to discover novel GSK-3ß inhibitors has increased over the years considering the involvement of this enzyme in many pathophysiological processes and diseases. Along this line, we recently reported on 1H-indazole-3-carboxamide (INDZ) derivatives 1-6, showing good GSK-3ß inhibition activity. However, they suffered from generally poor central nervous system (CNS) permeability. Here, we describe the design, synthesis, and in vitro characterization of novel imidazo[1,5-a]pyridine-1-carboxamide (IMID 1) and imidazo[1,5-a]pyridine-3-carboxamide (IMID 2) compounds (7-18) to overcome such liability. In detail, structure-based approaches and fine-tuning of physicochemical properties guided the design of derivatives 7-18 resulting in ameliorated absorption, distribution, metabolism, and excretion (ADME) properties. A crystal structure of 16 in complex with GSK-3ß enzyme (PDB entry 6Y9S) confirmed the in silico models. Despite the nanomolar inhibition activity, the new core compounds showed a reduction in potency with respect to INDZ derivatives 1-6. In this context, Molecular Dynamics (MD) and Quantum Mechanics (QM) based approaches along with NMR investigation helped to rationalize the observed structure activity relationship (SAR). With these findings, the key role of the acidic hydrogen of the central core for a tight interaction within the ATP pocket of the enzyme reflecting in good GSK-3ß affinity was demonstrated.

The influence of sulfur configuration in 1 H NMR chemical shifts of diasteromeric five-membered cyclic sulfites.

The effect of the stereochemistry of the sulfur atom on 1 H chemical shifts of the diasteromeric pair of cyclic sulfites of 4-[methoxy(4-nitrophenyl)methyl]-5-phenyl-1,3,2-dioxathiolan-2-oxide was investigated. The complete 1 H and 13 C NMR spectral assignment was achieved by the use of one-dimensional and two-dimensional NMR techniques in combination with X-ray data. A correlation of experimental data with theoretical calculations of chemical shift tensors using density functional theory and topological theory of atoms in molecules was made. Copyright © 2016 John Wiley & Sons, Ltd.

Characterization of Polyphenolic Content in the Aquatic Plants Ruppia cirrhosa and Ruppia maritima -A Source of Nutritional Natural Products.

Herein, the polyphenolic content in extracts of Ruppia cirrhosa (Petagna) Grande and Ruppia maritima L.was fully characterized for the first time. High amounts of the main compound chicoric acid (CA) (≤30.2 ± 4.3 mg/g) were found in both Ruppia species. In addition, eight flavonoids, namely the 3-O-glucopyranosides and 3-O-galactopyranosides, as well as malonylated 3-O-glycosides of quercetin and isorhamnetin, were isolated and identified. The antioxidant activity of Ruppia cirrhosa extracts and isolated compounds was investigated spectrophotometrically by a 1,1-diphenyl-2-picrylhydrazyl (DPPH·) radical scavenging assay. IC50 values were 31.8-175.7 µg/mL for Ruppia cirrhosa extracts and 12.1-88.4 µg/mL for isolated flavonoids. Both individual and total phenolic and flavonoid content were quantified in crude extracts using analytical HPLC. The relative high amount of total flavonoids ranged from 5.9 to 14.7 mg/g in both species, with concentrations of individual flavonoids ranging from 0.4 to 2.9 mg/g dry weight. The content of chicoric acid was twofold more in Ruppia maritima than in Ruppia cirrhosa. Seasonal variation of the quantitative content in Ruppia cirrhosa was examined. Total flavonoid content ranged from 8.4 mg/g in October to 14.7 mg/g in August, whereas the highest concentration of chicoric acid was observed in March (29.2 mg/g).

Solid-state 13 C, 15 N and 29 Si NMR characterization of block copolymers with CO2 capture properties.

Natural abundance solid-state multinuclear (13 C, 15 N and 29 Si) cross-polarization magic-angle-spinning NMR was used to study structures of three block copolymers based on polyamide and dimethylsiloxane and two polyamides, one of which including ferrocene in its structure. Assignment of most of the resonance lines in 13 C, 15 N and 29 Si cross-polarization magic-angle-spinning NMR spectra were suggested. A comparative analysis of 13 C isotropic chemical shifts of polyamides with and without ferrocene has revealed a systematic shift towards higher δ -values (de-shielding) explained as the incorporation of paramagnetic ferrocene into the polyamide backbone. In addition, the 13 C NMR resonance lines for ferrocene-based polyamide were significantly broadened, because of paramagnetic effects from ferrocene incorporated in the structure of this polyamide polymer. Single resonance lines with chemical shifts ranging from 88.1 to 91.5 ppm were observed for 15 N sites in all of studied polyamide samples. 29 Si chemical shifts were found to be around -22.4 ppm in polydimethylsiloxane samples that falls in the range of chemical shifts for alkylsiloxane compounds. The CO2 capture performance of polyamide-dimethylsiloxane-based block copolymers was measured as a function of temperature and pressure. The data revealed that these polymeric materials have potential to uptake CO2 (up to 9.6 cm3 g-1 ) at ambient pressures and in the temperature interval 30-40 °C. Copyright © 2016 John Wiley & Sons, Ltd.

Strecker degradation of amino acids promoted by a camphor-derived sulfonamide.

A camphor-derived sulfonimine with a conjugated carbonyl group, oxoimine 1 (O2SNC10H13O), reacts with amino acids (glycine, L-alanine, L-phenylalanine, L-leucine) to form a compound O2SNC10H13NC10H14NSO2 (2) which was characterized by spectroscopic means (MS and NMR) and supported by DFT calculations. The product, a single diastereoisomer, contains two oxoimine units connected by a -N= bridge, and thus has a structural analogy to the colored product Ruhemann´s purple obtained by the ninhydrin reaction with amino acids. A plausible reaction mechanism that involves zwitterions, a Strecker degradation of an intermediate imine and water-catalyzed tautomerizations was developed by means of DFT calculations on potential transition states.

A Characterization of Biological Activities and Bioactive Phenolics from the Non-Volatile Fraction of the Edible and Medicinal Halophyte Sea Fennel (Crithmum maritimum L.).

Although the biochemical composition and biological properties of the volatile fraction of the halophyte sea fennel (Crithmum maritimum L.) have been largely described, little is known about its polar constituents and bioactivities. Here, a hydromethanolic extract of Crithmum maritimum (L.) leaves was fractionated, and the fractions were evaluated in vitro for antioxidant (using DPPH, ABTS, and FRAP bioassays), anti-inflammatory (inhibition of NO production in RAW 264.7 macrophages), antidiabetic (alpha-glucosidase inhibition), neuroprotective (inhibition of acetylcholinesterase), and skin-protective (tyrosinase and melanogenesis inhibitions) activities. Polar fractions of the extract were rich in phenolics and, correlatively, displayed a strong antioxidant power. Moreover, fractions eluted with MeOH20 and MeOH80 exhibited a marked inhibition of alpha-glucosidase (IC50 = 0.02 and 0.04 mg/mL, respectively), MeOH60 fractions showed a strong capacity to reduce NO production in macrophages (IC50 = 6.4 µg/mL), and MeOH80 and MeOH100 fractions had strong anti-tyrosinase activities (630 mgKAE/gDW). NMR analyses revealed the predominance of chlorogenic acid in MeOH20 fractions, 3,5-dicaffeoylquinic acid in MeOH40 fractions, and 3-O-rutinoside, 3-O-glucoside, 3-O-galactoside, and 3-O-robinobioside derivatives of quercetin in MeOH60 fractions. These compounds likely account for the strong antidiabetic, antioxidant, and anti-inflammatory properties of sea-fennel polar extract, respectively. Overall, our results make sea fennel a valuable source of medicinal or nutraceutical agents to prevent diabetes, inflammation processes, and oxidative damage.

Synthesis, NMR characterization and cytotoxic activity of hybrid spirostanic sapogenins-estradiol dimers.

Four hybrid steroid dimers were obtained by BF3·Et2O-catalyzed aldol condensation of acetylated steroid sapogenins with 2-formyl-estradiol diacetate. The structures of the obtained dimers were unambiguously established by NMR. The hybrid dimers 9a (IC50 18.37 µM) and 9c (IC50 9.4 µM) with the 5α configuration at the A/B rings junction showed the higher cytotoxicity against HeLa, with selectivity index of 4.36 and 11.8 respectively. The presence of a carbonyl function at position C-12 produced the highest cytotoxic effect, which is in line with our previous reports.

Synthesis and characterization of a fluorescent steroid dimer linked through C-19 by a 1,4-Bis(phenylethynyl)phenylene fragment.

The synthesis and characterization of a dimer in which two nuclei of 3ß-acetoxy-19-hydroxyandrost-5-en-17-one are linked by the fluorescent 1,4-bis(phenylethynyl)phenylene bridge attached to the oxygenated functions at positions C-19 of each steroid fragment is described. The compound was obtained in five steps and 23 % overall yield and showed a strong blue emission with a quantum yield of 0.66.

Synthesis Characterization and Highly Protective Efficiency of Tetraglycidyloxy Pentanal Epoxy Prepolymer as a Potential Corrosion Inhibitor for Mild Steel in 1 M HCl Medium.

Anticorrosive protection efficiency of novel tetrafunctional epoxy prepolymer, namely 2,3,4,5-tetraglycidyloxy pentanal (TGP), for mild steel in 1 M HCl medium was assessed through potentiodynamic polarization (PDP), electrochemical impedance spectroscopy (EIS), scanning electron microscope (SEM), energy dispersive X-ray spectroscopy (EDS), contact angle (CA), adsorption isotherm model, temperature effect and thermodynamic parameters. The synthesized TGP was characterized and confirmed by Fourier transform infrared (FTIR) spectroscopy and nuclear magnetic resonance (NMR). The inhibitory efficiencies found at lower concentration of the prepolymer TGP were85% (PDP) and 87.17% (EIS). PDP measurement illustrated that the TGP behaved as a mixed-type inhibitor in the realized solution. SEM and EDS analysis showeda significant decrease in the corrosion of the MS surface in the presence of the inhibitory prepolymer compared with the blank (1 M HCl). Langmuir adsorption isotherm is the most acceptable modelto describe the TGP epoxy prepolymer on the MS area.

Alternative modification by grafting in bamboo cellulose nanofibrils: A potential option to improve compatibility and tunable surface energy in bionanocomposites.

Chemical modification in surface of cellulose nanofibrils CNFs (20 nm) from an endemic and non-significant value-added, Argentine bamboo, was developed. The modification in the CNFs was carried out with three simple routes using a low molecular weight polylactic acid synthesized in our laboratory (PLA1). The first step comprises of protection of the hydroxyl groups of PLA1 through a benzoylation (PLA1Bz). The next step consisted of the activation of carboxyl groups using thionyl chloride and the last reaction was the grafting of the modified PLA onto the CNFs (PLA1Bz-g-CNF). The covalently functionalization is confirmed by spectroscopically techniques as well as PLA1Bz-g-CNFs were characterized by thermal analyses. The PLA1Bz-g-CNFs were taken up such as nanocharges to improve properties of compatibilization and changing surface properties in films based on PLA. The comparison between the films with PLA1Bz-g-CNFs with respect to the physic mixture of the components (PLA1Bz/CNF), shows an improvement in the thermal, mechanical, and surface properties of the material, particularly when 5% of PLA1Bz-g-CNFs was added. The dispersive (γS D) component of film is increased in 36.1 mN/m respect to 29.3 mN/m from the films obtained with the physic mixture nanofibrils without modification and a plasticizing effect was noticed in the final material.

Reductive desymmetrization of steroid dimers.

NaBH3CN reduction of symmetric dimers in which two steroid units are linked by a 1,4-dimethylidenebenzene moiety followed two different courses: (a) hydrogenation of the benzylic double bond and (b) reductive F ring opening of the side chain. While courses a and b led to symmetrical dimers, the combination of both pathways produced an unsymmetrical dimer that bears different side chains in each half. The exhaustive NMR characterization of all obtained compounds is presented.

Dual stimuli-responsive polyurethane-based hydrogels as smart drug delivery carriers for the advanced treatment of chronic skin wounds.

The design of multi-stimuli-responsive vehicles for the controlled and localized release of drugs is a challenging issue increasingly catching the attention of many research groups working on the advanced treatment of hard-to-close wounds. In this work, a thermo- and pH-responsive hydrogel (P-CHP407) was prepared from an ad hoc synthesized amphiphilic poly(ether urethane) (CHP407) exposing a significant amount of -COOH groups (8.8 ± 0.9 nmol/gpolymer). The exposure of acid moieties in P-CHP407 hydrogel led to slightly lower initial gelation temperature (12.1 °C vs. 14.6 °C, respectively) and gelation rate than CHP407 hydrogel, as rheologically assessed. Nanoscale hydrogel characterization by Low Field NMR (LF-NMR) spectroscopy suggested that the presence of carboxylic groups in P-CHP407 caused the formation of bigger micelles with a thicker hydrated shell than CHP407 hydrogels, as further proved by Dynamic Light Scattering analyses. In addition, P-CHP407 hydrogel showed improved capability to change its internal pH compared to CHP407 one when incubated with an alkaline buffer (pH 8) (e.g., pHchange_5min = 3.76 and 1.32, respectively). Moreover, LF-NMR characterization suggested a stronger alkaline-pH-induced interaction of water molecules with micelles exposing -COOH groups. Lastly, the hydrogels were found biocompatible according to ISO 10993 and able to load and release Ibuprofen: delivery kinetics of Ibuprofen was enhanced by P-CHP407 hydrogels at alkaline pH, suggesting their potential use as smart delivery systems in the treatment of chronic infected wounds.

Deep eutectic solvent combined with ultrasound-assisted extraction as high efficient extractive media for extraction and quality evaluation of Herba Epimedii.

Deep eutectic solvent (DES) combined with ultrasound-assisted extraction (UAE) was successfully developed and fully validated to simultaneously determine Icarrin, IcarisidⅡ, Epimcdin A, Epimcdin B and Epimcdin C for the quality evaluation of Herba Epimedii. Twelve kinds of DESs were initially screened, and then the effective extraction was achieved by the tailor-made DES consisting of the mixture of l-proline and ethylene glycol with the molar ratio of 1:4 in this study. The optimal conditions were further optimized by the orthogonal experimental design (OED). 0.2 g sample powder was ultrasonic extracted by using 4.00 mL of aqueous solution containing 70 % (v/v) the above DES for 45 min, resulting to the optimum extraction efficiency. The FT-IR and NMR spectra showed the chemical structural characteristic correlation between l-proline and ethylene glycol, and could infer the formation of hydrogen bonds between the hydroxyl group of ethylene glycol and the nitrogen atom of l-proline. The hierarchical cluster analysis (HCA) was further processed for the quality evaluation of Herba Epimedii. Finally, DES could be used to distinguish different origins and different kinds of Herba Epimedii, and to evaluate the quality of Herba Epimedii. This method provided good linearity, precision and accuracy. The recoveries of the five main bioactive flavonoids in Herba Epimedii were within the range of 88.5-107.7 % (RSD less than 3.4 %). Compared to the traditional extraction method of Icarin in the Chinese Pharmacopoeia (2015 edition), the solvent consumption was decreased by 80 % and the extraction time was shortened by 25 %, leading to more efficient and more convenient of this DES-UAE method. This work indicated that DES would be a promising high effective solvent for the analytical sample preparations of plant herbs, and it might have a broad application in the quality control of traditional Chinese medicines.

Gemcitabine-vitamin E conjugates: Synthesis, characterization, entrapment into nanoemulsions, and in-vitro deamination and antitumor activity.

Gemcitabine is the first line therapy for pancreatic cancer. It is, however, extensively metabolized to the inactive form by deamination enzymatic reaction. Conjugation of gemcitabine with fatty acids on its 4-amino group was found to protect it from deamination deactivation reaction. The objective of the present study was to test the in-vitro anticancer activity of gemcitabine conjugated to the γ-tocotrienol isomer of vitamin E against pancreatic tumor cells. This objective was based on reported studies in which it was demonstrated that free tocotrienol isomers of vitamin E can potentiate the anticancer activity of gemcitabine. To accomplish this objective, a full synthesis scheme for gemcitabine conjugation to fatty acids (stearic and linoleic) and the tocopherol and tocotrienol isomers of vitamin E (α-T and γ-T3) was presented. The conjugates were characterized by 1H NMR and mass spectrometry analysis and tested for their susceptibility to deamination. Also discussed is the impact of entrapping the conjugates into nanoemulsions on the physiochemical properties of the delivery system and the in vitro anticancer activity of gemcitabine against Bx-PC-3 and PNAC-1 pancreatic cancer cells. In-vitro enzymatic deamination study showed that the γ-T3 conjugate of gemcitabine was least affected by deamination deactivation reaction when compared with the free and conjugated gemcitabine in solution. Furthermore, in-vitro cytotoxicity study demonstrated that entrapment of gemcitabine-lipid conjugates into nanoemulsions significantly enhanced their anticancer activity when compared to the free drug. It was concluded that conjugation to the γ-T3 isomer is a viable option for gemcitabine delivery and is worthy of further investigation.

Comparison for the compositions of fast and slow pyrolysis oils by NMR characterization.

The pyrolysis of softwood (SW) kraft lignin and pine wood in different pyrolysis systems were examined at 400, 500 and 600 °C. NMR including quantitative (13)C and Heteronuclear Single-Quantum Correlation (HSQC)-NMR, and Gel Permeation Chromatography (GPC) were used to characterize various pyrolysis oils. The content of methoxyl groups decreased by 76% for pine wood and 70% for lignin when using fast pyrolysis system. The carbonyl groups also decreased by 76% and nearly completely eliminated in 600 °C pine wood fast pyrolysis oil. Compared to the slow pyrolysis process, fast pyrolysis process was found to improve the cleavage of methoxyl groups, aliphatic CC bonds and carbonyl groups and produce more polyaromatic hydrocarbons (PAH) from lignin and aliphatic CO bonds from carbohydrates. Another remarkable difference between fast and slow pyrolysis oils was the molecular weight of fast pyrolysis oils increased by 85-112% for pine wood and 104-112% for lignin.

Antioxidant activity, antibacterial potential and characterization of active fraction of Dioscorea pentaphylla L. tuber extract collected from Similipal Biosphere Reserve, Odisha, India

ABSTRACT Dioscorea pentaphylla L., a wild tuber is used both as food and medicines among different ethnic groups of Similipal Biosphere Reserve, India. Tubers are used against skin infections. In order to establish and confirm tribal claims, methanol extract was subjected to fractionation. The active fraction (DP1) was subsequently used for further purification and NMR (Nuclear magnetic resonance) characterization. The phytochemical analysis revealed the presence of saponin groups. The antibacterial activity of DP1 was done against selected bacterial strains (Salmonella typhi, Shigella flexneri, Streptococcus pyogenes, Streptococcus mutans and Vibrio cholerae) using DD (disc diffusion), AWD (agar well diffusion) and broth dilution assay. The activity was compared with antibiotics Penicillin and Kanamycin. It was observed that DP1 showed significant inhibitory activity against the tested bacteria. The characterization of DP1 through NMR analysis and presence of proton in carbon position at C-3, C-19, C-18, C-21 and C-27 was same as the known compound "Diosgenin". Therefore, isolated compound was confirmed to be Diosgenin. The study for the first time showed that, diosgenin present in D. pentaphylla tuber was responsible for antibacterial and antioxidant potential. Present study highlights the importance of Dioscorea species as sources of diverse secondary metabolites for the isolation of active compound(s).