Human Liver Carcinoma Research Articles

Pollen Bee Aqueous Extract-Based Synthesis of Silver Nanoparticles and Evaluation of Their Anti-Cancer and Anti-Bacterial Activities

Bee pollens are rich source of essential amino acids and are often considered as complete food for human beings. Herein, we exploited the potential reducing abilities of Bee pollens extract for the eco-friendly preparation of silver nanoparticles (AgNPs-G). The resulting NPs were characterized using a combination of microscopic and spectroscopic techniques. The analyses confirm the formation of spherical Ag NPs. AgNPs-G obtained from the aqueous extract of bee pollens was used to study their antibacterial properties against Gram-positive and Gram-negative microbes using the Minimum Inhibitory Concentration 50 (MIC50) method. The antibacterial properties of AgNPs-G were compared to the properties of chemically synthesized Ag NPs (AgNPs-C) using sodium borohydride as a reducing agent. The green synthesized nanoparticles (AgNPs-G) exhibited a better antibacterial activity against most of the studied strains when compared to the chemically synthesized Ag NPs (AgNPs-C). In addition, the anti-cancer activity of Ag NPs was also studied against human liver and breast carcinoma cell lines by applying MTT-assay. The Ag NPs demonstrated considerable anticancer activity against the studied cell lines and exhibited high IC50 values in both MCF-7 and HepG2 cell lines.

Synthesis and characterization of Mannich bases of lawsone and their anticancer activity

Natural and synthetic naphthoquinones are known for a large number of biological activities. Lawsone (2-hydroxy-1, 4-naphthoquinone) is a simplest naturally occurring compound obtained from dried henna (Lawsonia inermis) leaves. In literature, some lawsone derivatives have been reported to exhibit anticancer activity. Hence, a clean and facile one-pot protocol was developed for the synthesis of new aminonaphthoquinones derived from lawsone by three-component Mannich reaction, at room temperature for potential anti-cancer application. Herein we present a small library of Mannich bases with different amines and aromatic aldehydes with moderate to high yield. Synthesized compounds were characterized using various spectroscopic techniques. The anticancer activity (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay) along with nuclear morphology assessment (4′,6-diamidino-2-phenylindole or DAPI staining), apoptosis assessment (acridine orange/ ethidium bromide staining), hemolysis and DNA ladder assay evaluated on human liver carcinoma cell line HepG2 are presented.

DFT calculations and POM analyses of cytotoxicity of some flavonoids from aerial parts of Cupressus sempervirens: Docking and identification of pharmacophore sites.

Two known polyphenols named apigenin 7-O-β-d-glucopyranoside (S1) and querctine-3-O-glucoside (S2), along with another two new compounds apigenin 4'-geranyl-8-glucopyranosyl-7-O-α-glucopyranoside (S3) and apigenin 4'-pernyl-8-glucopyranosyl -7-O-α-glucopyranoside (S4), were isolated from the leaves of Cupressus sempervirens. Structure elucidation of the isolated polyphenols was established on the basis of detailed spectroscopic analysis like 1D and 2D NMR analyses including 1H NMR, 13C NMR, COSY, DEPT, HMQC, UV, and Electron Spray Ionization Mass Spectroscopy (ESI-MS). Density Functional Theory (DFT) of computational, Petra/Osiris/Molinspiration (POM), and docking analyses methods were applied in the structural validation of new isolated compounds. The isolated compounds S1-S4 showed significant cytotoxicity against human hepatocellular liver carcinoma HepG2 cells, MCF-7, HC116 and A549.

Cystathionine gamma-lyase/H2S system suppresses hepatic acetyl-CoA accumulation and nonalcoholic fatty liver disease in mice

AimsHydrogen sulfide (H2S) as a novel gasotransmitter can be endogenously produced in liver by cystathionine gamma-lyase (CSE). The dysfunctions of CSE/H2S system have been linked to various liver diseases. Acetyl-CoA is the key intermediate from the metabolism of lipid. This study examined the roles of H2S in hepatic acetyl-CoA and lipid metabolism. Materials and methodsBoth in vitro cell model and in vivo animal model of lipid accumulation were used in this study. Western blotting and real-time PCR were used for analysis of protein and mRNA expression. Acetyl-CoA was analyzed by a coupled enzyme assay, and lipid accumulation was observed with Oil Red O staining. Key findingsIncubation of human liver carcinoma (HepG2) cells with a mixture of free fatty acids (FFAs) or high glucose reduced CSE expression and H2S production, promoted intracellular accumulation of acetyl-CoA and lipid. Supply of exogenous NaHS or cysteine reduced acetyl-CoA contents and lipid accumulation, while blockage of CSE activity promoted intracellular lipid accumulation. Furthermore, H2S blocked FFAs-induced transcriptions of de novo lipogenesis, inflammation, and fibrosis-related genes. In vivo, knockout of CSE gene stimulated more hepatic acetyl-CoA and lipid accumulation in mice induced by high-fat choline-deficient diet. The expressions of lipogenesis, inflammation, and fibrosis-related genes were significantly higher in liver tissues from CSE knockout mice when compared with wild-type mice. SignificanceCSE/H2S system is indispensable for maintaining the homeostasis of acetyl-CoA and lipid accumulation and protecting from the development of inflammation and fibrosis in liver under excessive caloric ingestion.

Cellular Toxicity Study of Silicon Nanowires.

The objective of this study was to achieve the practical bioapplications of silicon nanowires (SiNWs). In this study, the tumor and normal cell lines were used as models to systematically investigate the cytotoxicity of SiNWs synthesized by HF-assisted etching methods. Morphology observation, Cell Counting Kit 8, real-time polymerase chain reaction, and flow cytometry analysis were used to elucidate the cytotoxicity of SiNWs. The results showed that the cytotoxicity of SiNWs is greatly dependent on cell lines, SiNWs concentration, and incubation time. Particularly, SiNWs show better biocompatibility with tumor cell lines (eg, human epithelial cervical cancer [Hela] cells and human hepatocellular liver carcinoma [HepG2] cells) than normal cell lines (eg, human normal liver [HL-7702] cells and human embryonic kidney [HEK293T] cells). The reasons may be that SiNWs could tightly attach to the cell membrane in the cell medium, which obviously affects cell adhesion and inhibits their cell viability, especially for normal cell lines. From systematical analysis and comparison, we obtain the concentration limits of SiNWs, which may advance SiNWs applications and its toxicological study in vitro.

Synthesis and Biological Activities of Some New Benzotriazinone Derivatives Based on Molecular Docking; Promising HepG2 Liver Carcinoma Inhibitors.

In one-pot strategy, diazotization of methyl anthranilate 5 followed by addition of amino acid ester hydrochloride, we have prepared methyl-2-(4-oxobenzotriazin-3(4H)-yl)alkanoates 6a–c. Starting with hydrazides 7a,b, N-alkyl-2-(4-oxobenzotriazin-3(4H)-yl)alkanamides 9–10(a–h) and methyl-2-(2-(4-oxobenzotriazin-3(4H)-yl)alkanamido)alkanoates 11–12(a–e) were prepared via azide coupling. Hydrazones 13–15 were prepared via condensation of hydrazides 7a,b with 4-methoxybenzaldehyde, 4-dimethylaminobenzaldehyde, and/or arabinose. Molecular docking was done for synthesized compounds using MOE 2008-10 software. The compounds 9a, 12a, 12c, 13a, 13b, and 14b have the most pronounced strong binding affinities toward the target E. coli Fab-H receptor, whereas compounds 3, 11e, 12e, and 13a have the most pronounced strong binding affinities toward the target vitamin D receptor. The in vitro antibacterial activities of the highest binding affinity docked compounds were tested against E. coli, Staphylococcus aureus, and Salmonella spp. Majority of the tested compounds showed effective positive results against E. coli, while they were almost inactive against Staphylococcus aureus and Salmonella spp. The in vitro cytotoxic activities of the highest binding affinity-docked compounds were tested against the human liver carcinoma cell line (HepG2). Some compounds showed potent cytotoxic activity with low IC50 values, especially for 3 (6.525 μM) and 13a (10.97 μM) than that for standard drug doxorubicin (2.06 μM).

First Synthesis for Bis-Spirothiazolidine Derivatives as a Novel Heterocyclic Framework and Their Biological Activity.

Spirothiazolidines are versatile synthetic scaffold possessing wide spectrum of biological interests involving potential anticancer activity. To report the first synthesis of Bis Spiro-thiazolidine as a novel heterocyclic ring system. One-pot three-component reaction including condensation of p-phenyllene diamine; cyclohexanone and thioglycolic acid produced Spiro-thiazolidine 4, which underwent further condensation with cyclohexanone and thioglycolic acid with equimolar ratio to introduce Bis-Spiothiazolidine 5 as the first synthesis. Also, bis spiro-thiazolidine arylidene derivatives 6-13 were synthesized by the reaction of Bis-Spiothiazolidine 5 with different aromatic benzaldehydes. Four compounds 13, 12, 9 and 11 have shown highly significant anticancer activity compared to Doxorubicin® (positive control) against Human liver carcinoma (HepG2) and Human Normal Retina pigmented epithelium (RPE-1) cell lines. The novel bis-spirothiazolidine deriviatives have been synthesized for the first time and showed excellent anticancer activities compare with the corresponding spirothiazolidine derivatives.

Cytotoxic Evaluation and Anti-Angiogenic Effects of Two Furano-Sesquiterpenoids from Commiphora myrrh Resin.

Commiphora myrrh resin (Myrrh) has been used in traditional Arabic medicine to treat various inflammatory diseases. Two furano-sesquiterpenoids, 2-methoxyfuranodiene (CM1) and 2-acetoxyfuranodiene (CM2), were isolated from the chloroform fraction of the ethanolic extract of Arabic Commiphora myrrh resin. The cytotoxicity of the compounds was evaluated using human liver carcinoma, breast cancer cells (HepG2 and MCF-7, respectively) and normal human umbilical vein endothelial cells (HUVECs) cell lines. The development toxicity and anti-angiogenic activity of both compounds were also evaluated using zebrafish embryos. Cell survival assays demonstrated that both compounds were highly cytotoxic in HepG2 and MCF7 cells, with IC50 values of 3.6 and 4.4 µM, respectively. Both compounds induced apoptosis and caused cell cycle arrest in treated HepG2 cells, which was observed using flow cytometric analysis. The development toxicity in zebrafish embryos showed the chronic toxicity of both compounds. The toxicity was only seen when the embryos remained exposed to the compounds for more than three days. The compound CM2 showed a significant level of anti-angiogenic activity in transgenic zebrafish embryos at sublethal doses. Thus, we demonstrated the cytotoxic properties of both compounds, suggesting that the molecular mechanism of these compounds should be further assessed.

HP1s modulate the S-Adenosyl Methionine synthesis pathway in liver cancer cells.

Hepatocellular carcinoma (HCC) is the most frequent primary liver cancer in adults. Among the altered pathways leading to HCC, an increasing role is attributed to abnormal epigenetic regulation. Members of the Heterochromatin Protein (HP1) 1 family are key players in chromatin organisation, acting as docking sites for chromatin modifiers. Here, we inactivated HP1α in HepG2 human liver carcinoma cells and showed that HP1α participated in cell proliferation. HP1α-depleted cells have a global decrease in DNA methylation and consequently a perturbed chromatin organisation, as exemplified by the reactivation of transcription at centromeric and pericentromeric regions, eventhough the protein levels of chromatin writers depositing methylation marks, such as EZH2, SETDB1, SUV39H1, G9A and DNMT3A remained unaltered. This decrease was attributed mainly to a low S-Adenosyl Methionine (SAM) level, a cofactor involved in methylation processes. Furthermore, we showed that this decrease was due to a modification in the Methionine adenosyl transferase 2A RNA (MAT2A) level, which modifies the ratio of MAT1A/MAT2A, two enzymes that generate SAM. Importantly, HP1α reintroduction into HP1α-depleted cells restored the MAT2A protein to its initial level. Finally, we demonstrated that this transcriptional deregulation of MAT2A in HP1α-depleted cells relied on a lack of recruitment of HP1β and HP1γ to MAT2A promoter where an improper non-CpG methylation site was promoted in the vicinity of the transcription start site where HP1β and HP1γ bound. Altogether, these results highlight an unanticipated link between HP1 and the SAM synthesis pathway, and emphasise emerging functions of HP1s as sensors of some aspects of liver cell metabolism.

ANTIOXIDANT AND CYTOTOXIC ACTIVITY OF A SERIES OF O- AND S-CONTAINING MACROCYCLES

The significant interest in the search and study of antioxidants, both natural and synthetic, is explained by the possibility of preventing these harmful effects of free radicals in the human body. The similarity of macroheterocyclic derivatives to endogenous biomolecules makes them promising for research as antioxidant agents. By the interaction of 1,3-oxoheterocycloalkanes with ethyl 2-diazo-3-oxobutanoate, previously unexplored polyfunctional oxygen and sulfur-containing macroheterocycles are obtained. The relative antioxidant activity of new macroheterocycles in two model systems: generating active forms of oxygen and modulating lipid peroxidation reaction, was revealed active forms of oxygen and described by the method of recording luminol-dependent chemiluminescence lipid peroxidation reaction. The in vitro cytotoxic activity of the studied compounds was studied on Jurkat (human T-lymphoblastic leukemia cells), HepG2 (human liver carcinoma cells), HEK293 (human embryonic kidney cells) cell lines. The data obtained indicate practical significance. So, reagents 1-7 in the active forms of oxygen generating system have anti- and prooxidative properties, and in the system modeling lipid peroxidation reaction, they show only prooxidant activity. The influence of heterocycles 1–7 on the processes of free radical oxidation was determined by the intensity of the maximum flash (Imax, у.е.) and the luminosity of light (S, у.е.). Compounds with maximum anti- (4) and prooxidative (6) properties in the active forms of oxygen generating system and reagent 3 with the highest prooxidant activity in the lipid peroxidation reaction modeling system do not possess cytotoxic activity in vitro on cell lines HEK293 and HepG2 cultured in DMEM medium (Biolot, Russia), Jurkat in RPMI medium (Biolot, Russia) in the presence of 10% fetal calf serum (Invitrogen, USA), 2 mM L-glutamine and 50 μg / ml gentamicin sulfate.

Expeditious Sonochemical Synthesis of New 1,8-Naphthyridine Derivatives and their Inhibitory Activity on HepG2 Cell Line

Abstract: A new series of 2-phenyl-1,8-naphthyridine derivatives were synthesized via traditional heating and under ultrasonic irradiation to run out comparative study and confirm the utility of the green chemistry in organic synthesis. An improvement in the rates and yields were observed upon carrying out the reactions under environmentally benign protocol. The newly produced compounds were scanned in vitro for their adverse activity on HepG2 (Human liver) carcinoma cell lines. Results revealed that the tested compounds possess an inhibitory effect on the growth of HepG2 carcinoma cells. The naphthyridinyl pyridine derivatives 4c and 5c showed significant cytotoxic activity. The oxo-pyridine derivative4c was more potent than the reference drug doxorubicin (DOX), while the imino-pyridine derivative 5c showed slight reduction in the potency. On the other hand, Mannich bases (2a,c,d,e) showed good activity and the styryl derivatives (6b-d) showed moderate activity when compared to (DOX).

Chiral Ru(ii) complexes act as a potential non-viral gene carrier for directional transportation to the nucleus and cytoplasm.

Guanine-rich DNA sequences can spontaneously fold into four-stranded structures called G-quadruplexes (G4s). G4s have been identified extensively in the promoter regions of several proto-oncogenes, including c-myc, as well as telomeres. G4s have attracted an increasing amount of attention in the field of nanotechnology because of their use as versatile building blocks of DNA-based nanostructures. In this study, we report the self-assembly of c-myc G-quadruplex DNA controlled by a pair of chiral ruthenium(ii) complexes coordinated by 2-(4-phenyacetylenephenyl)-1H-imidazo[4,5f][1,10]phenanthroline (PBEPIP), Λ-[Ru(bpy)2(PBEPIP)](ClO4)2 (Λ-RM0627, bpy = bipyridine) and Δ-[Ru(bpy)2(PBEPIP)](ClO4)2 (Δ-RM0627). Λ-RM0627 could promote the high-order self-assembly of c-myc G-quadruplex DNA into a nanowire structure, whereas Δ-RM0627 could induce DNA condensation into G-quadruplex aggregates. Moreover, in vitro studies on human liver carcinoma HepG2 cells showed that the nanowire of c-myc G-quadruplex DNA promoted by Λ-RM0627 could be localized in the nuclei of cells, whereas the nanoparticle of c-myc G-quadruplex DNA generated by Δ-RM0627 was taken up and localized in the cytoplasm. This study provides examples of the enantioselective self-assembly of G4 DNA molecules controlled by chiral ruthenium(ii) complexes and suggests the potential applications of assembled nanostructures as non-viral DNA vectors for gene therapy.

Synthesis and anticancer activity of new tetrahydroquinoline hybrid derivatives tethered to isoxazoline moiety

A new series of tetrahydroquinoline-isoxazoline hybrid derivatives (3a–p) were efficiently synthesized involving 1,3-dipolar cycloaddition reaction according to click chemistry approach, from the corresponding N-allyl-4-(2-oxopyrrolinidyl-1)-tetrahydroquinolines preformed, with moderate to good yields (63–77%). To establish new candidates with anticancer activity, the antiproliferative effect of these compounds was measured by the MTT assay on different cancer cell lines such as human breast adenocarcinoma (MCF-7), human liver carcinoma (HepG2), human lung adenocarcinoma (A549), cervical cancer (HeLa), and murine melanoma (B16F10). Compounds 3a (CC50 = 11.37 μM, SI = 5.1) and 3i (CC50 = 25.59 μM, SI > 4.6) showed the best anticancer activities against murine melanoma cells with considerable selectivity compared with VERO cells. Compound 3h showed the best anticancer activity on cervical cancer (HeLa) cells (CC50 = 10.21 μM, SI = 4.1), and it was also slightly more active than the reference drug oxaliplatin. In addition, the compounds 3a and 3m decrease the mitochondrial membrane potential and induce apoptosis, suggesting that their cytotoxic effects may be based on mitochondrial parameter modulation.

Phytoconstituents and bioactivities of the Bark of Pleiogynium timorense (DC.) Leenh (Anacardiaceae)

Introduction: The purpose of this study was to evaluate the phytoconstituents and various bioactivities of Pleiogynium timorense bark as a step towards the production of a new drug from natural origin to overcome the complications of the synthetic drugs. Methods: The phenolic compounds were isolated and identified by chromatographic and spectroscopic methods as ultraviolet (UV) and nuclear magnetic resonance (NMR) spectra. The isolated compounds, as well as 70% methanol extract of P. timorense bark were tested for cytotoxicity against human colon carcinoma (HCT 116), human hepatocellular liver carcinoma (HepG2), normal melanocytes (HFB-4) and human breast carcinoma (MCF-7) cell lines. In addition, the methanol extract was evaluated for renal protective, hepatoprotective, antioxidant and antihyperglycaemic activities. Results: Seven phenolic compounds were isolated from the bark of the plant for the first time which were identified as; pyrogallol, catechin, gallic acid, kaempferol, quercetin, rutin and quercetrin. Moreover, the methanol extract of the bark showed a promising cytotoxic effect against HepG2 cell line more than that of the isolated compounds comparing with doxorubicin (a positive control), where catechin and gallic acid showed moderate effects. In addition, the methanol extract showed potent antioxidant, hepatorenal protective and antihyperglycaemic effects. Conclusion: Pleiogynium timorense extract possesses a potent cytotoxic effect against HepG2 cell line and significant antioxidant, hepatorenal protective and antihyperglycaemic effects.

Cytotoxicity of photoactivatable bromo tricarbonyl manganese(i) compounds against human liver carcinoma cells.

Two series of photoinduced tricarbonyl manganese(i) compounds were prepared from the reaction of [MnBr(CO)3(2-C(H)[double bond, length as m-dash]O)] (2-C(H)[double bond, length as m-dash]O: quinoline-2-carboxaldehyde and pyridine-2-carboxaldehyde) and para-substituted aniline derivatives (X = OH, OCH3, Cl and NO2). Different electron-donating and electron-withdrawing substituents were introduced in the para-position of the phenyl ring to investigate their influence on the stability of the compounds in the dark and the photophysical properties upon illumination at 525 nm. When kept in the dark, the aerated solutions of the complexes in dimethyl sulfoxide (DMSO) and CH2Cl2 were stable. In the solution, the complexes bearing electron-withdrawing substituents, exchange their bromo ligands with DMSO solvent molecules, as evidenced from infrared and UV/Vis studies as well as time-dependent density functional theory (TDDFT) calculations. The complexes were assessed for their cytotoxicity, both in the dark and upon exposure to a 525 nm LED, against the human hepatocarcinoma cell line (HepG2). A marked reduction in the viability of HepG2 cells treated with the complex functionalized with quinoline and methoxy substituent was observed after illumination in a dose-dependent manner, with an IC50 value of 7.1 μM, making it the most phototoxic compound in our study.

Bioactive phospho-therapy with black phosphorus for in vivo tumor suppression.

Background and Purpose: Although inorganic nanomaterials have been widely used in multimodal cancer therapies, the intrinsic contributions of the materials are not well understood and sometimes underestimated. In this work, bioactive phospho-therapy with black phosphorus nanosheets (BPs) for in vivo tumor suppression is studied.Methods: Orthotopic liver tumor and acute myeloid leukemia are chosen as the models for the solid tumor and hematological tumor, respectively. BPs are injected into mice through the tail vein and tumor growth is monitored by IVIS bioluminescence imaging. Tumor tissues and serum samples are collected to determine the suppression effect and biosafety of BPs after treatment.Results: The in vitro studies show that BPs with high intracellular uptake produce apoptosis- and autophagy-mediated programmed cell death of human liver carcinoma cells but do not affect normal cells. BPs passively accumulate in the tumor site at a high concentration and inhibit tumor growth. The tumor weight is much less than that observed from the doxorubicin (DOX)-treated group. The average survival time is extended by at least two months and the survival rate is 100% after 120 days. Western bolt analysis confirms that BPs suppress carcinoma growth via the apoptosis and autophagy pathways. In addition, administration of BPs into mice suffering from leukemia results in tumor suppression and long survival.Conclusions: This study reveals that BPs constitute a type of bioactive anti-cancer agents and provides insights into the application of inorganic nanomaterials to cancer therapy.

Study on the Mechanism of Shugan Xiaozhi Fang on Cells with Non-alcoholic Fatty Liver Disease

AbstractCells with non-alcoholic fatty liver disease (NAFLD) were studied to determine the mechanism of liver deficiency via the AdipoR2-PPARa pathway. NAFLD cells were randomly divided into a normal control group, blank control group, model group, low dose group, medium dose group, and high dose group. The NAFLD models were established by incubating the cells with linoleic acid (LA) and palmitic acid (PA) (2:1) for 24 h. The test groups were incubated with different doses of Shugan Xiaozhi Fang extract. The pathological changes in cells that accumulated lipids were detected by Oil Red O staining. Malondialdehyde (MDA) and triglyceride (TG) levels were measured. The apoptosis of cells was evaluated by flow cytometry. The levels of AdipoR2, PPARa, CD36, acyl-CoA mRNA, and protein were confirmed by RT- PCR and Western blot. The results of the Oil Red O staining demonstrated that the NAFLD cell model was successfully established. Compared with the model group, the levels of TG and MDA in the groups that received low, medium, and high doses of Shugan Xiaozhi were significantly lower (P<0.01), and a dose effect was evident. In addition, the expression of AdipoR2, PPARa, CD36, acyl-CoA protein, and mRNA in the Shugan Xiaozhi-treated groups was upregulated. Furthermore, the levels of AdipoR2, PPAR, CD36, acyl-CoA protein, and mRNA in all drug treatment groups that were extracted from L-O2 normal human hepatocytes were significantly upregulated (P<0.01). Moreover, the factor pattern of HepG2 human liver carcinoma cells was similar to that of L-O2. The levels of AdipoR, CD36, acyl-CoA, and AdipoR mRNA in the HepG2 low group were increased (P<0.05). AdipoR, PPAR, CD36, and acyl-CoA protein levels and AdipoR mRNA expression were significantly increased in the intermediate dose group and high dose group (P<0.01). Shugan Xiaozhi Fang attenuates hepatic lipid deposition in NAFLD induced by incubating with LA and PA for 24 h, which is associated with the activation of the AdipoR2-PPARα pathway.

A Novel Approach towards Synthesis and Characterization of Non-Cytotoxic Gold Nanoparticles Using Taurine as Capping Agent.

Metal gold nanoparticles are of great interest due to their unique physico-chemical properties and their potential to be used as nano-probes in biosensors, drug delivery, and therapeutic applications. Currently, many capping agents are used for metal gold nanoparticles, such as cetyltrimethylammonium bromide (CTAB) and tri-sodium citrate that have been reported to be toxic and hinders biological applications. To address this issue, we report, for the first time, the use of taurine as a stable non-cytotoxic capping agent for synthesizing gold nanoparticles by using an in situ wet-chemical method. This facile method resulted in monodisperse gold nanospheres with a high yield and stability. Monodisperse gold nanospheres with average diameters of 6.9 nm and 46 nm were synthesized at a high yield with controlled morphology. Temperature played a critical role in determining the size of the taurine-capped gold nanoparticles. The subtle changes in the reaction parameters had a tremendous effect on the final size of nanoparticles and their stability. The synthesized nanoparticles were characterized by using optical spectroscopy, a ZetaSizer, a NanoSight, Fourier Transform Infrared (FTIR) spectroscopy, X-ray Diffraction (XRD), X-ray Photon Spectroscopy (XPS) and Electron Microscopy to understand their physico-chemical properties. Taurine was explored as a capping and stabilizing agent for gold nanospheres, which were evaluated for their toxicity responses towards human liver carcinoma cells (HepG2) via MTT assay.

Synthesis and characterization studies of 3‐formyl chromone Schiff base complexes and their application as antitumor, antioxidant and antimicrobial

A novel Schiff base namely (E)‐3‐((2,6‐dihydroxypyrimidin‐4‐ylimino)methyl)‐4H‐chromen‐4‐one and its Co (II), N (II)i, Cu (II) and Cd (II) complexes have been synthesized and proved by elemental analysis, molar conductance, thermal analysis (TGA), Inductive Coupled plasma (ICP), magnetic moment measurements, X‐ray powder diffraction, IR, EI‐mass,1H NMR, 13C NMR,UV–Vis. and ESR spectral studies. On the basis of these data, it is evident that the Schiff base acts as bidentate via oxygen atom of carbonyl group and azomethine nitrogen atom for Co (II) complex; monobasic bidentate ligand for Ni (II), Cu (II) and Cd (II) complexes via oxygen atom of hydroxyl group and nitrogen atom of pyrimidine ring. The results showed all complexes have octahedral geometry. The average particle size of the ligand and its complexes were found to be 1.010–0.343 nm. The pharmacological action (antioxidant, antimicrobial and anticancer) of the prepared compounds is studied. The antitumor activity of the ligand and its metal complexes is evaluated against human liver carcinoma (HEPG2) cell. The data displayed the Co (II) complexes strong cytotoxicity where IC50 values of Co (II) complex and 5‐fluorouracil (stander drug) are 9.33 and 7.86 μg/ml respectively. The Co (II) and Cd (II) complexes have antibacterial activity more than ampicillin (stander drug). The interaction of the synthesized compounds with calf‐thymus DNA (CT‐DNA) has been performed via absorption spectra and viscosity technique. The DNA‐ binding constants have been determined.

PH-sensitive, dynamic graft polymer micelles via simple synthesis for enhanced chemotherapeutic efficacy.

To promote chemotherapeutic efficacy and easier clinical transformation, a series of pH-sensitive and dynamic drug delivery systems with facile two-step synthesis and simple structure have been successfully constructed by the tunable grafting reaction between pH-sensitive ortho ester and poly(vinyl alcohol). The amphipathic graft macromolecules (PVA- g-OE x, x represents the percentage of feed between ortho esters and hydroxyl groups of polyvinyl alcohol) could self-assemble into micelles and doxorubicin was embedded. These micelles exhibited pH-sensitivity to both extracellular and intracellular pH and demonstrated the following characteristics: (i) maintaining long-term storage and blood circulation stability at pH 7.4; (ii) responding to tumoral extracellular pH value following gradually larger nanoparticles for improved drug accumulation and retention; (iii) being sensitive to tumoral intracellular pH value following disintegration for rapid drug release to improve toxicity to tumor cells. Moreover, the doxorubicin-loaded micelle (PVA- g-OE30-DOX) showed similar cytotoxicity to free doxorubicin in vitro, but stronger tumor penetration and inhibition ability in vitro human liver carcinoma cell line multicellular tumor spheroids. In vivo biodistribution and tumor inhibition examinations demonstrated that PVA- g-OE30-DOX had more superior efficacy in significantly enhancing drug accumulation in tumor, restraining tumor growth while decreasing drug concentration in normal tissues. The pH-sensitive, dynamic graft polymer micelles via simple synthesis could be considered as a promising and effective drug carrier in tumor therapy.