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Purpose: To examine the efficacy of Celastrus orbiculatus extract (COE) on the chemosensitivity of liver cancer (LC) cells and its mechanism of action.Methods: Hep G2/ADM cells in the logarithmic growth phase were assigned to a control group (no treatment for cell culture medium only) and a study group (120 μg/ml COE added to the culture medium). After 48 h of incubation, the biological responses were compared. The study group wasdivided into groups A and B, while control group was divided into groups C and D, with 1 μmol/L XAV939 added in groups A and C. Cell proliferation, cell invasion, cell apoptosis rate, and apoptosis protein in the four groups were evaluated.Results: The study group showed significantly lower values in terms of cell proliferation and cell invasiveness (p < 0.05) and a higher apoptotic rate than the control group (p < 0.05)). The study group also demonstrated an elevated pro-apoptotic protein Bax level and a declined anti-apoptotic protein Bcl-2 level. In contrast to group B, the proliferation and invasiveness of Hep G2/ADM cells in group A treated with the inhibitor, XAV939, were significantly lower (p < 0.05), while the apoptotic rate exhibited a significant increase (p < 0.05). There was a rise in the level of pro-apoptotic protein, Bax, and a fall in the anti-apoptotic protein Bcl-2 level in group A. Lower levels of β-catenin, c-Myc, and cyclin D1 protein were observed in the study group compared with the control group (p < 0.05). Compared with other groups, the multiplication capacity and invasiveness of cells in group A treated with COE and inhibitor XAV939 significantly declined, while the apoptotic rate increased (p < 0.05).Conclusion: COE reverses drug resistance in chemotherapy by inhibiting the expression of Wnt/β-catenin pathway in LC cells. Therefore, COE has potentials for use along with chemotherapeutic agents in the management of liver cancer.

Background/objective: Cancer is a complex genetic disease that occurs due to mutation in genes that control apoptosis and cell growth. Uncontrolled cell growth leads to the formation of tumors. Free radical causes mutation in genes and DNA sequence, however antioxidants can stabilize these harmful effects. Citrus fruits are the rich source of antioxidants. owing to this property this study was planned to evaluate the potential of the citrus fruits for the treatment of the cancer. Aim: This study aimed to evaluate antioxidant as well anticancer potential of five different citrus strains (Citrus deliciosa, Citrus maxima, Citrus limetta, Citrus sinensis and Citrus reticulata). Methods: Peel of all the citrus fruits were collected, grinded and ethanolic extracts were prepared separately, to evaluate radical scavenging ability by employing DPPH method followed by MTT assay of the cancer cell lines to explore the anticancer potential of the extracts. Results: It was observed that citrus peels exhibited good radical scavenging activity and inhibited tumor growth. Maximum effect was produced by Citrus reticulata, and least results were obtained with Citrus sinensis. Conclusion: It was concluded that antioxidant and anti-cancer effects of citrus peels may be due to be owing to the presence of antioxidants (ascorbic acid, flavonoids, phenols, limonene). This research might open new horizon in the treatment of cancer chemotherapy.

A series of 1, 2, 3- triazole hybrids (9a-9n) were synthesised from major phenolic constituent, 4-methoxy ethyl cinnamate (5) isolated from rhizomes of Hedychium spicatum (Sm), a traditional medicinal plant used in variety of disease conditions. All the synthesised analogues were tested for their in vitro antiproliferative potential against HCT 116 (colon cancer), A549 (lung cancer), DU-145 (prostate cancer), Hep G2 (hepatoma) and HEK-293 (normal) cell lines. Among the compounds tested, compounds 9i and 9k potently arrested proliferation of DU-145 (prostate cancer) cell line. Compound 9i displayed 20 times better antiproliferative potential than parent compound and almost identical inhibitory activity to that of the standard drug, doxorubicin. The flow cytometric analysis revealed that 9i arrested cells in G2/M phase of cell cycle and induced apoptosis. Overall, the hybrid derivative 9i was found to be a potential antiproliferative lead against prostate cancer.

Recently, supramolecular self-assembled core–shell nanostructures have emerged as advanced and notable drug delivery vehicles in biomedical arena for human health. Here, we have modified curcumin via Michael addition reaction with 3-mercaptopropionic acid followed by preparation of an amphiphatic conjugate employing hydrophilic polyethylene glycol monomethyl ether (mPEG). The synthesized compounds, curcumin-S-propionic acid (Cur-S) and curcumin-S-propionoyl-mPEG (Cur-S-mPEG), were spectroscopically characterized. Self-assembly of Cur-S-mPEG into micellar nanostructures was monitored by dynamic light scattering, which revealed the size of these nanostructures in the range of ~ 104 nm. Transmission electron microscopic analysis showed the size of these nanostructures ~ 26 nm. These micelles with hydrophobic pockets were then demonstrated to entrap hydrophobic therapeutics, ornidazole (Oz) and sulfasalazine (Sz), successfully with high efficiency. Drug-loaded formulations, Cur-S-mPEG(Oz) and Cur-S-mPEG(Sz), showed sustained release of drugs over a longer duration, particularly, a higher release at neutral pH 7.2 displaying the usefulness of the nanocarrier for colonic delivery. MTT assay performed on HEK 293 and Hep G2 cells displayed the non-toxic nature of the nanocarrier on normal cells (HEK 293 cells) while toxic on cancer cells (Hep G2 cells).

In this study, new amino heterocyclic cellulose derivatives were prepared. Dialdehyde cellulose was functionalized by Schiff base reaction with (E)-2-(4-(dimethylamino) benzylidene)-4-oxo-4-phenylbutanehydrazide, (E)-2-((1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-4-phenylbutane hydrazide, and thiophene-2-carbohydrazide. The prepared derivatives were characterized and confirmed by Fourier-transform infrared spectroscopy, scanning electron microscopy, energy-dispersive X-ray, and Thermo gravimetric analysis. Additionally, antimicrobial activity of all derivatives was assessed as well as antitumor activity. Results revealed that, all derivatives have potential antimicrobial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, Candida albicans, Cryptococcus neoformance, Aspergillus niger, A. fumigatus. Additionally, (E)-2-(4-(dimethylamino) benzylidene)-4-oxo-4-phenylbutanehydrazide and (E)-2-((1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-4-phenylbutanehydrazide cellulose compounds have good antitumor activities against Hep G2 and MCF7 cancerous cell lines without any effects on Wi38 normal cell line. Molecular dynamics study revealed that (E)-2-(4-(dimethylamino) benzylidene)-4-oxo-4-phenylbutanehydrazide and (E)-2-((1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-4-phenylbutanehydrazide cellulose derivatives have selectively target the ATP binding pocket residues. Identification of these ATP binding site residues and their crucial roles could provide the structure basis for understanding c-Kit kinase auto-inhibition

Nickel oxide nanoparticles (NiO NPs) were synthesized via the facile sol–gel method. The synthesized NiO NPs were characterized using X-ray diffraction (XRD), Field-Emission Scanning Electron Microscopy (FESEM), Transmission Electron Microscopy (TEM), Raman and Fourier Transform Infrared (FT-IR) techniques. The effect of particle size was analyzed on structural alterations, electrochemical behaviors, and cytotoxic effect of synthesized NiO NPs. According to TEM results, the particle sizes of synthesized NiO NPs were 8.2, 15.4, and 21.7 nm at 300, 400, and 500 °C, respectively. Electrochemical behaviors of synthesized NiO NPs were assessed through the cyclic voltammetry (CV) technique. The results showed that the magnitude of the current density was decreased in treated samples exposed to higher temperature values. The cytotoxic activity of synthesized nanoparticles was investigated against human liver cancer cell (Hep-G2), breast cancer cell (MCF-7), and colon cancer cell (HT-29) lines using the MTT assay. The results demonstrated that synthesized NiO NPs had higher cytotoxicity at 300 °C than at 400 and 500 °C, because of their small particle size. Thus, synthesized NiO NPs exhibit acceptable cytotoxic effects against Hep-G2, MCF-7, and HT-29 cancer cell lines so that they could be a good choice for cancer treatment.

Glycosmis stenocarpa is a species of shrub found in the Northern provinces of Vietnam. Its roots contain different carbazolic derivatives, mainly Murrayafoline A (Mu-A), which exhibits valuable biological activities. In this study, we performed an extraction of Mu-A from the roots of G. stenocarpa and optimized this process using response surface methodology (RSM) according to a central composite design, with three independent parameters including extraction time (min), extraction temperature (°C), and solvent/material ratio (mL/g). Two dependent variables were the Mu-A content (mg/g raw materials) and extraction efficiency (%). The optimal conditions to extract Mu-A were found to be as follows: extraction temperature, 67°C; extraction time, 165 min; and solvent/material ratio, 5:1. Under these conditions, the Mu-A content and extraction efficiency were 38.94 ± 1.31 mg/g raw materials and 34.98 ± 1.18%, respectively. Mu-A exhibited antiproliferation and antitumor-promoting activity against the HepG-2 cell line. The present optimization work of Mu-A extraction from G. stenocarpa roots contributed to the attempt of designing a large-scale extraction process for the compound and further exploitation of its potential in vivo applications.

Purpose Physical activity and professional physical activity such as water polo (WP) sport, has numerous beneficial effects to fight metabolism-related disorders through several mechanisms, including the promotion of liver metabolic adaptations, and the modulation of cytokine production. The aim of this study was to investigate the effects of different types of physical activity on AMPKα and ACC, two proteins involved in liver metabolism; therefore, we treated the hepatoma cell line Hep G2 with sera from elite WP athletes and amateur (basket) players. As control, we used serum from both sedentary and obese subjects. Methods Help G2 cells were treated with 5% of human sera from the different subjects; after 24 h and 48 h, HepG2 cell viability was verified through MTT assay and activation status of AMPKα and ACC through western blotting. Cytokine’s serum levels were measured through ELISA assay. Results After 72 h, the treatment of HepG2 cells with sera from the different subjects produced no effect on cell viability. Furthermore, after 48 h of treatment, both AMPKα and ACC phosphorylation statistically increases in HepG2 cells treated with sera from WP athletes. Furthermore, IL-4, IL-6 and IL-10 levels resulted statistically increased in WP athlete’s sera than in sedentary subjects. Conclusion The specific activation of AMPKα and ACC by WP sera confirms that professional sport activity carried out by WP athletes can be considered as a physiological activator of these two proteins also in HepG2 liver cells. In addition, the increase of anti-inflammatory cytokines in WP sera confirms the ample evidence for multiple anti-inflammatory activities carried out by WP discipline.

A novel smartphone-based electrochemical cell sensor was developed to evaluate the toxicity of heavy metal ions, such as cadmium (Cd2+), lead (Pb2+), and mercury (Hg2+) ions on Hep G2 cells. The cell sensor was fabricated with reduced graphene oxide (RGO)/molybdenum sulfide (MoS2) composites to greatly improve the biological adaptability and amplify the electrochemical signals. Differential pulse voltammetry (DPV) was employed to measure the electrical signals induced by the toxicity of heavy metal ions. The results showed that Cd2+, Hg2+, and Pb2+ significantly reduced the viability of Hep G2 cells in a dose-dependent manner. The IC50 values obtained by this method were 49.83, 36.94, and 733.90 μM, respectively. A synergistic effect was observed between Cd2+ and Pb2+ and between Hg2+ and Pb2+, and an antagonistic effect was observed between Cd2+ and Hg2+, and an antagonistic effect at low doses and an additive effect at high doses were found in the ternary mixtures of Cd2+, Hg2+, and Pb2+. These electrochemical results were confirmed via MTT assay, SEM and TEM observation, and flow cytometry. Therefore, this new electrochemical cell sensor provided a more convenient, sensitive, and flexible toxicity assessment strategy than traditional cytotoxicity assessment methods.

Turnera subulata are bright common garden flowers that are grown in Asian regions. Mostly flowers of several kinds have medicinal properties and applications. This is as one of a kind that contains compounds that has medicinal application. The present studies are targeted to investigate the phytochemical composition through GC-MS technique, antimicrobial activity and antitumor activity via MTT assay against Hep G2 (or HepG2), a human liver cancer cell line. Ethanol (EtOH) extracts has reasonable antitumor activity against Hep G2 for period of 24 h and 48 h and the aqueous part was non-reactive. From gas chromatography‑mass spectrometry (GC-MS), a sum of 27 identified natural compounds exhibiting against cancer cell. Some traces of flavouring agents and antifungal agent with very low GC-MS peak lengths are too observed furaneol (2,4-Dihydroxy-2,5-dimethyl-3(2H)-furan-3-one), benzeneacetaldehyde, benzoic acid and undecanoic acid. Hence, the result that indicates the flavouring agents including flavonoids along with phenolic and other acidic compounds have important characteristic property in reducing and treating against cancer cells.

A set of 12 maslinic acid−coumarin conjugates was synthesized, with 9 being maslinic acid−diamine−coumarin conjugates at the C-28 carboxylic acid group of triterpene acid and the other three being maslinic acid−coumarin conjugates at C- 2/C-3 and/or C-28 of the triterpene skeleton. The cytotoxic effects of these 12 triterpene conjugates were evaluated in three cancer cell lines (B16-F10, HT29, and Hep G2) and compared, respectively, with three nontumor cell lines from the same or similar tissue (HPF, IEC-18, and WRL68). The most potent cytotoxic results were achieved by a conjugate with two molecules of coumarin-3-carboxylic acid coupled through the C-2 and C-3 hydroxy groups of maslinic acid. This conjugate showed submicromolar IC50 values in two of the three cancer cell lines tested (0.6, 1.1, and 0.9 μM), being between 110- and 30-fold more effective than its corresponding precursor. Furthermore, this conjugate (10) showed percentages of cell viability for the three nontumor lines of 90%. Four maslinic acid−coumarin conjugates displayed apoptotic effects in the treated cells, with total apoptosis rates of between 40 and 85%, relative to the control. Almost all the compounds assayed caused cell-cycle arrest in all cancer cell lines, increasing the number of these cells in the G0/G1 phase., Junta de Andalucia B1-FQM-217-UGR18 B1-BIO-281-UGR18

Platinum-based complexes are one of the most successful chemotherapeutic agents having a significant ground in cancer chemotherapy despite their side effects. During the past few decades, Ru(II) complexes have been emerging as efficient alternatives owing to their promising activities against platinum-resistant cancer. The pathway of action, lipophilicity, and cytotoxicity of a Pt or Ru complex may be tuned by varying the attached ligands, the coordination mode, and the leaving group. In this work, we report a family of Pt(II) and Ru(II) complexes (1-5) of three N,O and N,N donor-based trimethoxyanilines containing Schiff bases with the general formula [PtII(L)(DMSO)Cl], [RuII(L)(p-cymene)Cl], [RuII(L)(p-cymene)Cl]+, and [PtII(L)Cl2]. All of the complexes are characterized by different analytical techniques. 1H NMR and electrospray ionization mass spectrometry (ESI-MS) data suggest that the N,O-coordinated Pt(II) complexes undergo slower aquation compared to the Ru(II) analogues. The change of the coordination mode to N,N causes the Ru complexes to be more inert to aquation. The N,O-coordinating complexes show superiority over N,N-coordinating complexes by displaying excellent in vitro antiproliferative activity against different aggressive cancer cells, viz., triple-negative human metastatic breast adenocarcinoma MDA-MB-231, human pancreatic carcinoma MIA PaCa-2, and hepatocellular carcinoma Hep G2. In vitro cytotoxicity studies suggest that Pt(II) complexes are more effective than their corresponding Ru(II) analogues, and the most cytotoxic complex 3 is 10-15 times more toxic than the clinical drugs cisplatin and oxaliplatin against MDA-MB-231 cells. Cellular studies show that all of the N,O-coordinated complexes (1-3) initiate disruption of the microtubule network in MDA-MB-231 cells in a dose-dependent manner within 6 h of incubation and finally lead to the arrest of the cell cycle in the G2/M phase and render apoptotic cell death. The disruption of the microtubule network affects the agility of the cytoskeleton rendering inhibition of tyrosine phosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), a key step in angiogenesis. Complexes 1 and 2 inhibit VEGFR2 phosphorylation in a dose-dependent fashion. Among the Pt(II) and Ru(II) complexes, the former displays higher cytotoxicity, a stronger effect on the cytoskeleton, better VEGFR2 inhibition, and strong interaction with the model nucleobase 9-ethylguanine (9-EtG).

Although Pakistan is stacked with enormous varieties of medicinal plants, only a little proportion of these plants has been evaluated for their medicinal and therapeutic properties. Herein, four indigenous medicinal plants Citrus sinenesis, Citrus paradiasii, Moringa olifera, and Hibiscus rosa-sinenesis were collected and subjected to phytochemical analyses to scrutinize the presence of secondary metabolites. Qualitative analy�sis showed the presence of an array of secondary metabolites in the selected plants, which were further corroborated by high-performance liquid chromatography. Results revealed the presence of 33.24, 21.04, 15.2 ppm gallic acid in methanol, ethyl acetate and n-hexane fraction of C. sinensis peels extract, respectively. C. paradaissi peels consist of 24.06, and 18.24 ppm of gallic acid and caffeic acid, respectively, in methanol and chloroform fractions, whereas its methanolic seeds extract contain caffeic acid as a major component (10.63 ppm). H. rosa-sinenesis has shown p-coumaric acid, caffeic acid, and gallic acid at 35.26, 15.04, and 11.4 ppm, respectively. M. olifera contained 3.24 ppm gallic acid in pods extract while stems and leaves extract contain a very low amount. Anticancer profile evinced that Citrus sinensis extract showed the highest percent inhibition (142.746%) of human liver cancer (Hep G2) cell lines followed by H. rosa-sinensis (132.49%), C. paradaisii (82.39%) and M. olifera (68.0%). The determined IC50 values for antioxidant activity were C. sinenesis (IC50=0.49 mM), C. paradaisii (IC50=0.43 mM), M. olifera (IC50=0.42 mM) and H. rosa-sinensis (IC50=0.41 mM). Conclusively, the selected plants could be an effective alternative and deliverable chemical therapeutic to the pharmaceutical industry due to their excellent biological effects.

Endophytic fungi isolated from desert plants are among the less known organisms with potentially valuable applications. The bioactivities of an endophytic fungus isolated from Aloe vera, a plant found in central regions of Asir desert, Saudi Arabia. Based on primary phytochemical screening, an efficient isolate was selected and identified according to the sequence analysis of the internal spacer regions ITS1, ITS4 and the 5.8S region as Preussia africana belonging to the family Sporormiaceae. The crude extract of this fungus was evaluated for its bioactivities. Under static conditions, the crude extract at a concentration of 500 μg/mL had a strong 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging rate of 87%, whereas a higher concentration (100 μg/mL) had an astounding wound healing effect (42.6% at 48 h) when compared to positive control. Moreover, the crude extract with a concentration of 50 μg/mL was active against almost all cancer cell lines such as HeLa (cervical cancer), Hep G2 (liver cancer), MCF-7 (breast cancer), A549 (lung cancer), LN-229 (glioblastoma), A-431 (skin cancer), and kidney cell line (HEK 293T). The results suggest that the endophytic fungus P. africana from A. vera has wide therapeutic applications against severe disease conditions.

In recent years, metal oxides have been studied as an encapsulating matrix nevertheless, few studies the effect that can exist between different precursors to form this type of nanomaterials; In this paper, we compare its ability as a mangiferin (MG) nanoencapsulated. Phytochemical that has been studied for its generous biological properties like anti-inflammatory, antiproliferative, and others; the nanoparticles (NP’s) be synthesized with zinc nitrate and zinc acetate. The results showed modifications in the morphology of the ZnO associated with the precursor but, there is no significant difference between any treatment that is associated with antitopoisomerase activity however, ZnOA-MG is statistically the best treatment by reducing in greater proportion the production of COX-II prostaglandins (97.38 ± 7.09%) with a significant difference (p

New chelates derived from the novel ligand, (Z)-3-amino-N-(3-amino pyrazine-2-carbonyl)pyrazine-2-carbohydrazonic acid (APA, L), with Cu2+, Co2+, Pt4+ and Pd2+ salts were investigated. The results suggest that APA acts as mononegative tridentate in the case of Cu2+, binegative tetradentate in the case of Co2+ and as mononegative bidentate towards Pt4+ and Pd2+ chelates. The results of the corrected μeff. and spectral suggest the structures of the isolated chelates. The results of the corrected μeff. and spectral suggest the geometries of the isolated chelates. Molecular modeling is deduced and chemical reactivity, energy components for chelates and also MEP for APA is illustrated. In Vitro, the SOD and radical scavengers like activity of the synthesized compounds Hep G2 liver cancer cells and cytotoxic activity were checked. Metal chelates show potent anti-oxidative activity. The results of cytotoxic activity assay against hepatocellular carcinoma cell line Hep G2 confirmed that Pt4+ complex has the highest value, while APA, Cu2+, Co2+ and Pd2+ chelates have no significant cytotoxic activity.

Resveratrol (RES) (trans-3, 5,-4′-trihydroxystilebene) is a multi-biofunctional compound found in a variety of plants such as grapes and mulberries. Studies of nanoencapsulated resveratrol have ind...

A series of binary metal complexes (halo, hydroxyl and methoxy substituted bis(2-(E)acryloyl)naphthalen-1-yl)oxy)Cu(II) and Zn(II) (C1? ?C10)) of Cu2+ and Zn2+ ions derived from bi-coordinated hydroxylated 1,3- -diaryl-2-propene-1-ones were synthesized. The newly synthesized metal complexes were structurally determined by FT-IR, 1H-NMR, 13C-NMR, ESR spectral, XRD and TGA analyses. The FT-IR and ESR studies demonstrated that interactions between metal ions with ligands occur through carbonyl oxygen and deprotonated hydroxyl oxygen and correspond to square-planar geometry for all complexes. The metal complexes were screened in-vitro and evaluated for their antimicrobial and cytotoxic activities. The complexes C1 and C4 showed significant antimicrobial activity while the remaining complexes showed moderate antimicrobial activity against the tested pathogens. The complexes were evaluated for cytotoxic activity against the organism Artemia salina. Complexes C2?C5 exhibited LC50 values of 630.45, 969.99, 921.94 and 918.41 ?M mL-1, respectively. Furthermore, the complexes were evaluated for their anticancer activity against the liver cancer cell line Hep G2 in comparison with the 5-fluorouracil standard. Complex C5 showed a significant IC50 value of 58.94 ?g mL-1. Therefore, the present study is useful for the development of a new class of antimicrobial and anticancer agents.

Monochoria vaginalis commonly known as Neelolpalam belonging to pontederiaceae family have several medicinal properties. The present study deals with the free radical scavenging activity of various extracts of Monochoria vaginalis. It aimed to identify various secondary metabolites present in the active fraction and to investigate the hepatoprotective efficacy against acetaminophen induced toxicity in Hep G2 cell lines. The studies showed that M. vaginalis methanolic extract have a hepatoprotective action at a concentration of 12.5 µg/ml. The study proved that the root stock of plant had antioxidant activity as well as hepatoprotective efficacy due to the combined effect of phytoconstituents like alkaloids, phenolics and flavonoids.

Background: Megakutki® (MK) is a polyherbal preparation of 11 standardized extracts that are individually proven for hepatoprotection scientifically. Aim: Study evaluated MK’s hepatoprotective potential against paracetamol (PCM) in in-vitro on Hep G2 cells using cell viability, cell cycle analysis and apoptotic studies and in in-vivo in Wistar rats using liver function tests, histological and DNA fragmentation study. Materials and Methods: In in-vitro studies, IC50 (50% inhibition in viability) values of silymarin, MK and PCM were found out by MTT assay. In-vitro hepatoprotection was found out by pretreating the cells with below-IC50 concentrations of MK and silymarin for 24h followed by PCM (at IC50 concentration) challenge for next 24h and % viability was evaluated using MTT assay. Same treatment protocol was followed for cell cycle analysis and apoptotic studies (100 and 200 µg/ml for MK and 50 µg/ml for silymarin and 40µM for PCM). In in-vivo study, animals were grouped in six, namely, vehicle, PCM control, silymarin (50 mg/kg, standard), MK (100 and 300 mg/kg) groups. Animals were dosed for 8 days while they were challenged on day 6 (except vehicle group) with PCM (2.75 g/kg p.o). On day 8, blood and livers were collected under anaesthesia and analyzed. Results: In-vitro results showed hepatoprotection by MK and silymarin by inhibition of PCM-induced cell death apoptotic cells percentage. In in-vivo study, MK and silymarin reversed the altered liver function and elevated oxidative stress markers (catalase, SOD, GSH, total thiols and lipid peroxidation) compared to paracetamol alone group. Both MK and silymarin decreased the percentage of DNA fragmentation and histopathological changes in liver tissue compared to the PCM group. Conclusion: The in-vitro and in-vivo studies showed the hepatoprotective effect of MK by the prevention of PCM-induced induction of oxidative stress by its antioxidant potential thereby preventing PCM-induced DNA damage.

β-sitosterol (BS), a phytosterol, exhibits ameliorative effects on hepatocellular carcinoma (HCC) due to its antioxidant activities. However, its poor aqueous solubility and negotiated bioavailability and short elimination half-life is a huge limitation for its therapeutic applications. To overcome these two shortcomings, BS-loaded niosomes were made to via, film hydration method and process parameters were optimized using a three-factor Box-Behnken design. The optimized formulation (BSF) was further surface-modified with polyethylene glycol (PEG). The resulting niosomes (BSMF) have spherical shapes, particle sizes, 219.6 ± 1.98 nm with polydispersity index (PDI) and zeta potential of 0.078 ± 0.04 and -19.54 ± 0.19 mV, respectively. The drug loading, entrapment efficiency, and drug release at 24 h of the BSMF were found to be 16.72 ± 0.09%, 78.04 ± 0.92%, and 75.10 ± 3.06%, respectively. Moreover, BSMF showed significantly greater cytotoxic potentials on Hep G2 cells with an enhanced cellular uptake relative to pure BS and BSF. The BSMF also displayed potentially improved curative property of HCC in albino wistar rat. Thus, the BSMF could be one of the promising therapeutic modalities for HCC treatment in terms of targeting potential resulting in enhanced therapeutic efficacy.

Objective: Aspergillus fungus is a rich source of natural products with broad biological activities. This study was conducted to identify secondary metabolites from the rice culture of Aspergillus species isolated from Melaleuca subulata leaves and evaluated their anticancer activity. Methods: Ethyl acetate extract was fractionated on silica gel and Sephadex columns. Structures of the compounds were established using physical and chemical methods. Cytotoxic activities of the extract and pure compounds against two human cancer cell lines (Mcf-7and Hep G2) were evaluated using microculture tetrazolium assay as well as the mode of the cytotoxicity was evaluated. Molecular docking studies have been performed using the Hsp 90 enzyme as an anticancer target. Results: Methyl linoleate (1), arugosin C (2), ergosterol (3), sterigmatocystin (4), diorcinol (5), alternariol-5-O-methyl ether (6), averufin (7), averufanin (8), and alternariol (9) were identified from ethyl acetate extract. All tested compounds exhibit week activity against MCF-7 and Hep G2 cell lines but a mixture of compounds 7 and 8 is considered to be more active towards both MCF-7 and Hep G 2 in comparison to other compounds. Compound 4 exhibits moderate activity against Hep G2 only as well as the ethyl acetate extract exerts moderate activity against MCF-7 cell line Moreover, compound 4 and a mixture of 7 and 8 caused a decrease in the number of Hep G2 cancer cells due to apoptotic and necrotic processes. Most active anticancer candidates 7 and 8 showed binding to the active site similar to geldanamycin reference ligand. Conclusion: Secondary metabolites identified from Aspergillus sp. and their anticancer activity were evaluated. Molecular docking suggested active candidates as Hsp 90 inhibitors.

In the present study, phytochemical analysis, synthesis and characterization of zinc oxide nanoparticles (NG-ZnO NPs) from neem gum as a capping agent. GC–MS analysis confirms the phytochemical oxadiazol-2yl-benzothiazole-(21.5%) on the synthesized ZnO nanoparticles. Various sophisticated analytical instrumentations characterized the morphological and crystalline behaviour of NG-ZnO NPs. The analytical results confirm the spherical crystals of NG-ZnO NPs in size range of 60–80 nm size. The NG-ZnO NPs shown significantly efficient antibacterial and antibiofilm activity against P. aeruginosa at 100 µg/mL. Further, in vitro study on human liver cancer cell line (Hep G2) indicated significantly inhibited the cell proliferation at 100 µg/mL in 24 h. Also, NG-ZnO NPs have also shown potent mosquito larvicidal activity on C. quinquefasciatus at 100 µg/mL. Based on findings, it is recommended that neem gum capped ZnO NPs is potential nano biomedical agents to be used in new drug formulations.

14-O-[(4,6-Diaminopyrimidine-2-yl)thioacetyl] mutilin (DPTM) is a promising drug candidate with excellent antibacterial activity against Gram-positive bacteria. The present study was designed to characterize its Cytochrome P450 (CYP) enzymes inhibition activities and the genotoxicity with the standard Ames test. We determined the inhibitory effects of DPTM on CYP1A2, CYP2D1/6, CYP2E1, CYP2C11/9 and CYP3A/4 in rat liver microsomes (RLMs) and in human liver microsomes (HLMs). The mRNA expressions of the above CYP isoforms and their transcriptional regulators were also evaluated using the Hep G2 cell model. The results showed DPTM exhibited a moderate inhibitory potential against CYP3A/4 (IC50 values of 10 ± 2 and 8 ± 2 μM, respectively) and weak against the other CYP enzymes based on their IC50 values. Compared to the control, CYP isoforms and their transcriptional regulators mRNA expressions significantly increased when the Hep G2 cells were treated with DPTM for a certain period of time. In the Ames test, Salmonella strains TA97, TA98, TA100, TA102 and TA1535 were treated with or without the metabolic activation (S9). Analysis showed the average number of revertant colonies per plate was less in double in the groups treated with DPTM than that in the negative control plate and showed no dose-related increase.