Biochemical characterization,cytotoxic, antimutagenic,anticancer and molecular docking studies on Tecomella undulata

In this study bioassay-guided screening of Tecomella undulate was performed for its cytotoxic, antimutagenic and anticancer potential. The ariel parts were extracted on a polarity basis (methanol, dichloromethane and hexane). The in vivo toxicity was assessed on Caenorhabditis elegans, and its locomotion was affected by Tecomella undulata hexane (TUAH) the most. Ames test for antimutagenicity showed Tecomella undulata methanol (TUAM) exhibited against mutagen 2AA showed inhibition of 71.03% and 26.32% 2AA in TA98 while in in vitro MTT assay on carcinoma cell lines TUAM showed 68.1% cytotoxicity. Moreover, In resazurin assay on fibroblast cells African green monkey kidney VERO and on the panel of carcinoma cell lines, the most effective extract was TUAM on liver HepG-2 with CC₅₀ value 117.37 ± 4.73 µg/ml followed by on lungs A549 with 142.01 ± 5.3. Furthermore, for the bioassay-guided screening, the selectivity index was calculated for TUAM CC₅₀ ratio on HepG-2 and VERO which showed a decent 2.77 score. After column chromatography, the fraction TU-63 should remarkable cytotoxic effect in dose–response manner assay as (Hep-G2) CC₅₀ value 11. 67 ± 1.37 µg/ml followed by (A549) CC₅₀ value 17.23 ± 0.58 µg/ml. For qualitative analysis of anticancer potential LC-ESI-MS/MS the potential phytochemicals were identified. In silico molecular modelling against selected carcinogenic proteins. The results suggest Tecomella undulate the substantial anticancer potential which supports potential natural anticancer therapeutic drug candidate development for combating cancer.     

Comparative assessment of biological activities of different parts of halophytic plant Tamarix articulata (T. articulata) growing in Saudi Arabia

Owing to extremely high salinity and harsh environmental conditions, T. articulata is one of the most abundant wild plants growing in the deserts of Saudi Arabia. Such plants may contain novel compounds to display promising biological activities. Here, in this study, we evaluate the biological activities of methanolic extracts of fresh leaves, dry leaves, stem, and roots of T. articulata. The antioxidant activity was determined by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and total phenolic and flavonoid content were determined using standard colorimetric methods. Whereas antimicrobial and ant-proliferative activities were determined by standard well-diffusion and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) methods, respectively. Our results demonstrate that all methanolic extracts of T. articulata showed antioxidant activity, however, the methanolic extract of dry leaves exhibits promising antioxidant effect with IC₅₀ value 49.08 ± 1.98, which was strongly supported by total phenolic (409.92 ± 6.03 mg GAE/g DW) and flavonoid (177.71 mg QE/g DW) content. Although, antimicrobial activity was also exhibited by all the methanolic extracts, however, methanolic extract of dry leaves exhibits promising antimicrobial activity in Gram-positive bacteria Staphylococcus epidemidis. Furthermore, MTT assay revealed that all methanolic extracts exhibit antiproliferative activity in MCF-7 (breast cancer) and RKO (colorectal cancer) cells with IC₅₀ values ranges from 219 ± 5.112 µg/ml to 253 ± 5.231 µg/ml and 220 ± 4.330 µg/ml to 325 ± 6.213 µg/ml, respectively. However, the most promising antiproliferative effect was displayed by methanolic extract of dry leaves with IC₅₀ values 219 ± 5.112 µg/ml and 220 ± 4.330 µg/ml, respectively. In summary, these findings provide evidence that T. articulata has promising biological activities and can be used for many pharmaceutical activities in the future.     

Phytochemical profiling,antioxidant and antibacterial efficacy of a native Himalayan Fern: Woodwardia unigemmata (Makino) Nakai

Present work elucidates the antioxidant and antibacterial activity of Woodwardia unigemmata (Makino) Nakai along with chemical characterization using its aqueous (AEW), methanol (MEW), and hexane (HEW) extracts. Chemical profile of different extracts was illustrated by using Gas chromatography and mass spectrometry (GC-MS) analysis. Antioxidant activities were tested using DPPH and FRAP assays, total phenolic and flavonoid content by Folin-Ciocalteu and aluminum chloride method, respectively. Further, antibacterial activity against six plant and four animal pathogenic bacteria was analyzed by employing the disc diffusion assay. GC-MS analysis revealed the presence of catechol (21.96%), glycerol (20.22%), n-pentadecanoic acid (6.95%), glyceryl monoacetate (6.35 %), ethyl acetimidate (5.39 %) and 3-hydroxy-2,3-dihydromaltol (5.36%) in AEW; β-sitosterol (17.39%), pentadecanoic acid (9.81%), vitamin E (7.82%) and glycerol (7.05%) in MEW; γ-sitosterol (33.45%), vitamin E (10.04%) and campesterol (7.32%) in HEW as major constituents. Maximum phenolics (873 ± 6.01 mgGAE/g dry extract) as well as flavonoids (151 ± 11.44 mgQE/g dry extract) content was found in MEW, which also showed remarkable antioxidant potential (IC₅₀ 6.07 ± 1.4 µg/ml for DPPH and 768 ± 10.4 mg AAE/g dry extract for FRAP assay. In antibacterial activity, maximum inhibition (15 ± 0.9 mm) was observed for HEW against R. solanacearum, followed by AEW against A. tumefaciens and X. phaseoli (11 ± 0.3 mm each). MEW was found positive only against A. tumefaciens. Significant minimum inhibitory concentration (MIC) value observed for AEW against L. monocytogenes (10 mg/ml). Polar extracts had remarkable antioxidant potential, while non-polar extract did show significant antibacterial activity. Further, GC- MS reports indicated that this traditionally useful fern species can be an excellent source of biologically active compounds.     

Antiproliferative and antioxidant properties of nematocysts crude venom from jellyfish Acromitus flagellatus against human cancer cell lines

This study aimed to investigate the antiproliferative and antioxidant properties of crude venom from the nematocyst of Jellyfish Acromitus flagellates on human lung cancer (A549) and liver cancer (HepG2) cell lines. The prepared crude venom was subjected to analyses of the biochemical constituents, protein profiles, antioxidant and anticancer activities by standard methods. The extracted venom was pale-yellow in color and viscous/sticky. The biochemical composition such as, protein (1.547 mg/ml), lipid (0.039 mg/ml) and carbohydrate (0.028 mg/ml) was estimated. Protein profiles were determined by SDS PAGE, the result revealed that the molecular weight range from 205 ? 3.5 kDa. The free radical scavenging activity was analyzed by the reducing potential (56.36%), DPPH (72.47%), hydroxyl (68.50%), superoxide anion (65.75%), and nitric oxide (33.04%). The cell viability was observed by using different concentrations (20 to 100 µg/ml) of crude venom on A549 and HepG2 cancer cell lines and the IC₅₀ values were recorded in (60 μg/ml and 40 μg/ml) respectively, while it had none cytotoxic effects on Vero cell line up to the concentration of 90 μg/ml. These results suggest that crude venom from nematocyst of A. flagellatus possesses anti-cancer activity and able to develop novel drugs on marine-derived compounds.     

In vitro antioxidant and cytotoxic activities of polyherbal extracts from Vetiveria zizanioides,Trichosanthes cucumerina,and Mollugo cerviana on HeLa and MCF-7 cell lines

Various metabolites exist in the medicinal plants have lot of potential to cure various diseases and disorders. Plants such as, Vetiveria zizanioides, Trichosanthes cucumerina, and Mollugo cerviana were collected from Western Ghats, Tamilnadu, India. Phytochemicals were extracted from these plants using various organic solvents and tested against Gram-positive and Gram-negative bacteria. The phytochemicals such as, carbohydrate, alkaloids, steroids, saponins, flavonoids and tannin were detected from these medicinal plants. Among the extracts, methanol showed potent activity and this solvent was used to extract polyherbal medicinal plants. Methanol extract of V. zizanioides was found to be highly active against E. coli (27 ± 2 mm), P. mirabilis (19 ± 3 mm) and B. subtilis (18 ± 2 mm). Ethyl acetate extract showed high activity against E. coli (24 ± 2 mm), P. mirabilis (22 ± 3 mm) and B. subtilis (20 ± 1 mm). These three plants were taken at 1:1:1 ratio and extracted with methanol at 1:10 ratio and synergistic activity was tested against bacterial pathogens. Synergistic activity of polyherbal extract was analyzed. The extracted crude herbal medicine was found to be effective against Staphylococcus aureus, E. coli, Enterbacter sp., Pseudomonas aeruginosa, Bacillus subtilis and Proteus mirabilis. The zone of inhibition was 33 ± 3 mm, 17 ± 2 mm, 22 ± 2 mm, 40 ± 2 mm, 33 ± 1 mm and 38 ± 2 mm zone of inhibition against E. coli, S. aureus, P. aeruginosa, P. mirabilis, B. subtilis and Enterobacter sp. Polyherbal extract was found to be highly effective against P. mirabilis and Enterobacter sp. MIC values of polyherbal extract ranged from 29 ± 2.5 µg/ml to 34 ± 2.5 µg/ml. MIC value was found to be less against P. mirabilis and was high against S. aureus. Antioxidant property varied between 49 ± 3% and 95.3 ± 2%. At 20 µg/ml antioxidant activity was reported as 49 ± 3% and it was increased at higher concentrations of polyherbal extract. Two cell lines (HeLa and MCF cell lines) were selected to analyze cytotoxic activity of polyherbal extract. The methanol extract of polyherbal fraction showed cytotoxicity against these two cell lines. The LC50 value was 467 ± 2.9 µg/ml against HeLa cell line and >800 µg/ml against MCF-7 cell lines. The polyherbal extract showed antibacterial, antioxidant and anticancer activities.     

Mn3O4 nanoparticles: Synthesis,characterization and their antimicrobial and anticancer activity against A549 and MCF-7 cell lines

Due to their inexpensive and eco-friendly nature, and existence of manganese in various oxidation states and their natural abundance have attained significant attention for the formation of Mn₃O₄ nanoparticles (Mn₃O₄ NPs). Herein, we report the preparation of Mn₃O₄ nanoparticles using manganese nitrate as a precursor material by utilization of a precipitation technique. The as-prepared Mn₃O₄ nanoparticles (Mn₃O₄ NPs) were characterized by using X-ray powder diffraction (XRD), UV–Visible spectroscopy (UV–Vis), High-Resolution Transmission electron microscopy (HRTEM), Field emission scanning electron microscopy (FESEM), Thermal gravimetric analysis (TGA) and Fourier-transform infrared spectroscopy (FT-IR). The antimicrobial properties of the as-synthesized Mn₃O₄ nanoparticles were investigated against numerous bacterial and fungal strains including S. aureus, E. coli, B. subtilis, P. aeruginosa, A. flavus and C. albicans. The Mn₃O₄ NPs inhibited the growth of S. aureus with a minimum inhibitory concentration (MIC) of 40 μg/ml and C. albicans with a MIC of 15 μg/ml. Furthermore, the Mn₃O₄ NPs anti-cancer activity was examined using MTT essay against A549 lung and MCF-7 breast cancer cell lines. The Mn₃O₄ NPs revealed significant activity against the examined cancer cell lines A549 and MCF-7. The IC₅₀ values of Mn₃O₄ NPs with A549 cell line was found at concentration of 98 µg/mL and MCF-7 cell line was found at concentration of 25 µg/mL.     

Phytochemical profiling,antioxidant and antiproliferation potential of Euphorbia milii var.: Experimental analysis and in-silico validation

This study was aimed to investigate the anticancer potential of Euphorbia milii (E. milii) using an exquisite combination of phytopharmacological and advanced computational techniques. The chloroform fraction (Em-C) of E. milii methanol extract showed the highest antioxidant activity (IC₅₀: 6.41 ± 0.99 µg/ml) among all studied fractions. Likewise, Em-C also showed significant cytotoxicity (IC₅₀: 11.2 ± 0.8 µg/ml) when compared with that of standard compound 5-fluorouracil (5-FU) (IC₅₀: 4.22 ± 0.6 µg/ml) against hepatocarcinoma cell line (HepG2). However, in a human cervical cancer cell line (HeLa), Em-C demonstrated a non-significant difference in cytotoxicity (22.1 ± 0.8 µg/ml) when compared with that of 5-FU (IC₅₀: 6.87 ± 0.5 µg/ml). Furthermore, Western blot and qRT-PCR analysis revealed that the suppression of HepG2 cells was the consequence of a tremendous decrease in CDK2 and E2F1 protein expression. The GC–MS analysis of Em-C revealed the unique presence of cyclobarbital (CBT) and benzodioxole derivative (BAN) as major constituents. Furthermore, molecular docking of compounds BAN, CBT, and MBT into the binding site of different molecular targets i.e. cyclin dependent kinase 2 (CDK2), thymidylate synthase (TS), caspase 3, BCL2 and topoisomerase II was carried out. Compounds BAN and CBT have demonstrated remarkable binding affinity towards CDK2 and thymidylate synthase, respectively. Molecular dynamic simulation studies have further confirmed the finding of docking analysis, suggesting that CDK2 and TS can act as an attractive molecular target for BAN and CBT, respectively. It can be concluded that these E. milii phytoconstituents (BAN and CBT) may likely be responsible for anti-invasive activity against HepG2 cells.     

In-vitro antibacterial,antioxidant potentials and cytotoxic activity of the leaves of Tridax procumbens

The present study explored the phytochemicals, antibacterial, antioxidant and cytotoxic effect of Tridax procumbens leaves. The leaves were dried and extracted with various organic solvents. The leaves contained the phytochemicals such as alkaloids, carbohydrates, polyphenols and tannins respectively. Antimicrobial potentials of the extracts were determined by performing the disc diffusion techniques. Results revealed that different organic solvents extracts namely methanol, ethanol and ethyl acetate extracts documented comparatively good activity against the studied microbial strains. The methanol extract of leaves of T. procumbens showed combatively better antioxidant potential. The tested plant leaf extract showed high activity against human lung cancer cells than breast cancer cell lines. 250 µg/ml plants extract showed 84 ± 2.8% toxicity against human lung cancer cells.     

Viridiflorol induces anti-neoplastic effects on breast,lung, and brain cancer cells through apoptosis

All active natural molecules are not fully exploited as therapeutic agents, causing delays in the advancement of anticancer drug discovery. Viridiflorol is a natural volatile element that may work as anti-cancer compound. We tested the anticancer properties of viridiflorol at different concentrations ranging from 0.03 to 300 μM in vitro on three cancer cells including breast (MCF-7), lung (A549) and brain (Daoy). The cancer cells responses were documented after treatment using MTT and Annexin V assays. Viridiflorol showed cytotoxic effects against all tested cell lines, reducing cell viability in a concentration-dependent manner with variable IC₅₀ values. Daoy and A549 cell lines were more sensitive to viridiflorol when compared with temozolomide and doxorubicin, respectively. Viridiflorol demonstrated the highest anticancer activity against the Daoy cells with an estimated IC₅₀ of 0.1 µM followed by MCF-7 at 10 µM, and A549 at 30 µM. In addition, upon exposure to concentrations ranging from 30 µM to 300 µM of viridiflorol, early and late apoptotic cell death was induced in a concentration dependent manner in Daoy (55.8%-72.1%), MCF-7 (36.2%-72.7%) and A459 (35%-98.9%) cell lines, respectively. In conclusion, viridiflorol demonstrates cytotoxic and apoptotic ability in three different cancer cell lines (brain, breast and lung).     

Preliminary screening of antioxidant and cytotoxic potential of green seaweed,Halimeda opuntia (Linnaeus) Lamouroux

Marine natural products have displayed numerous advantageous effects on biological activities, including antioxidants and cytotoxicity. The total lipids, carotenoids, chlorophyll a and b content, total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity of methanolic crude extract of the green seaweed Halimeda opuntia were all measured in this study. The TPC of the extracts was determined according to the Folin-Ciocalteu method, yielding a result of 55.04 ± 0.98 mg GAE/g of extract. As determined by the aluminium chloride colorimetric method, the TFC of the extract was 40.02 ± 0.02 mg QE/g of extract. Antioxidant activity was determined by using a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay with different concentrations that ranged between 200 and 1000 µg/mL, noted H. opuntia as the highest in DPPH reduction (63.61 %) at 1000 µg/mL concentration. Total antioxidant capacity (TAC) of the extract was 57.36 ± 0.004 mg AAE/g extract at concentration of 1.0 mg/mL. The cytotoxic activity of this seaweed was pre-screened against a panel of cell lines including estrogen receptor-positive human breast adenocarcinoma (MCF-7), estrogen negative human breast adenocarcinoma (MDA-MB-231), human colorectal adenocarcinoma (HT-29), human hepatocellular carcinoma (HepG2), and mouse embryonic fibroblast (3T3) using the MTT assay. The content of total lipids in H. opuntia was 1.60 ± 0.002 %. Total carotenoids were 115.57 ± 0.98 µg/g, while chlorophyll a and b were 148.73 ± 2.60 µg/g and 290.83 ± 9.46 µg/g, respectively. In terms of cytotoxicity activity, methanolic extract of H. opuntia was found to be highly cytotoxic to MCF-7 cells, with an IC₅₀ of 25.14 ± 1.02 g/mL, and slightly less so to 3T3 cells (IC₅₀ 65.23 ± 0.25 µg/mL). This study's findings suggest that natural pigments (carotenoids and chlorophyll), phytochemicals like phenolic and flavonoid compounds found in this species may play an important role and could be used as a natural cancer treatment.     

Microwave-assisted synthesis of novel 5-substituted benzylidene amino-2-butyl benzofuran-3-yl-4-methoxyphenyl methanones as antileishmanial and antioxidant agents

A series of 5-substitutedbenzylideneamino-2-butylbenzofuran-3-yl-4-methoxyphenyl methanones is synthesized and evaluated for antileishmanial and antioxidant activities. Compounds 4f (IC₅₀?=?52.0?±?0.09?µg/ml), 4h (IC₅₀?=?56.0?±?0.71?µg/ml) and 4l (IC₅₀?=?59.3?±?0.55?µg/ml) were shown significant antileishmanial when compared with standard sodium stibogluconate (IC₅₀?=?490.0?±?1.5?µg/ml). Antioxidant study revealed that compounds 4i (IC₅₀?=?2.44?±?0.47?µg/ml) and 4l (IC₅₀?=?3.69?±?0.44?µg/ml) have shown potent comparable activity when compared with standard ascorbic acid (IC₅₀?=?3.31?±?0.34?µg/ml). Molecular docking study was carried out which replicating results of biological activity in case of initial hits 4f and 4h suggesting that these compounds have a potential to become lead molecules in drug discovery process. In silico ADME study was performed for predicting pharmacokinetic profile of the synthesised antileishmanial agents and expressed good oral drug like behaviour.     

Target and non-target effects of Foeniculum vulgare and Matricaria chamomilla combined extract on Culex pipiens mosquitoes

The present study focused on extracting green larvicides from extracts of the combination of Foeniculum vulgare and Matricaria chamomilla using different solvents of increasing polarity in a Soxhlet extractor and evaluating their ovicidal, larvicidal, and cytotoxic activities. The most promising among all tested extracts was hexane extract. The ovicidal activity of the hexane PH2 extract resulted in a significant (p < 0.05) decrease in egg hatchability from 95.00 ± 6.16% to 15 ± 9.04% at doses ranging from 62.5 to 500 µg/mL. The larval mortality with the hexane extract ranged from 13.33 ± 3.3% to 93.33 ± 3.3% at doses ranging from 31.25 to 250 µg/mL, respectively. The LC₅₀ and LC₉₀ values of the larvicidal activity of the hexane extract were estimated to be 148.3 and 242.17 µg/mL, respectively, after 24 h of exposure. Similarly, the LC₅₀ values after 48 and 72 h of exposure were 124.93 and 100.3 µg/mL, respectively, against the third instar of Cx. pipiens. PH2 treatment of larvae resulted in histopathological changes such as degenerated epithelial cells and destruction of microvilli on the epithelial cells. The PH2 extract achieved a dose-dependent decrease in the rate of cell survival. The IC₅₀ value of PH2-treated HUVECs was 192.07 µg/mL after 24 h of incubation. The cells showed changes in cellular and nuclear morphology. In conclusion, the hexane extract of PH2 could be used in mosquito management programs.     

Cytotoxic effects of stem bark extracts and pure compounds from Margaritaria discoidea on human ovarian cancer cell lines

Margaritaria discoidea (Baill.) G. L. Webster (Euphorbiaceae) is a well-known medicinal plant in Africa used for the treatment of various diseases. So far, no cytotoxic effects of plant extracts on cancer cell lines have been reported.Aim of the studyTo evaluate the cytotoxicity against human ovarian cancer cells of extracts of M. discoidea and characterize the major bioactive compounds.MethodsBoth organic and aqueous extracts of this plant were obtained by maceration. The sulforhodamine B cell proliferation assay was used for evaluation of their cytotoxic activities and the potential bioactive compounds were characterized by gas chromatography–mass spectrometry.ResultsThe organic extract of M. discoidea showed stronger cytotoxicity than the aqueous extract with IC₅₀ values of 14.4 ± 3.0, 14.2 ± 1.2 and 34.7 ± 0.5 µg/ml on OVCAR-8, A2780 and cisplatin-resistant A2780cis ovarian cancer cells, respectively. The organic extract was further subjected to bioassay-guided fractionation by partitioning with n-hexane, ethyl acetate, and n-butanol in water. The ethyl acetate fraction was the most potent on the three ovarian cancer cell lines. A GC–MS analysis of trimethylsilyl derivatives of this fraction indicated the presence of phenolic compounds such as gallic acid and the alkaloid securinine. The IC₅₀ values of these two compounds were determined to be in the range of 3–16 µM, which indicated that they could contribute to the cytotoxic activity of the extract of M. discoidea.ConclusionsThis study has evaluated the cytotoxicity of stem bark extracts of M. discoidea against ovarian cancer cells and provided a basis of further development of this plant for the treatment of ovarian cancer.     

A new isoflavonol and other constituents from Cameroonian propolis and evaluation of their anti-inflammatory,antifungal and antioxidant potential

Propolis is rich in diverse bioactive compounds. Propolis samples were collected from three localities of Cameroon and used in the study. Column chromatography separation of propolis MeOH:DCM (50:50) extracts yielded a new isoflavonol, 2-hydroxy-8-prenylbiochanin A (1) alongside 2′,3′-dihydroxypropyltetraeicosanoate (2) and triacontyl p-coumarate (3) isolated from propolis for first time together with seven compounds: β-amyrine (4), oleanolic acid (5), β-amyrine acetate (6), lupeol (7), betulinic acid (8), lupeol acetate (9) and lupenone (10). These compounds were tested for their inhibitory effect on oxidative burst where intracellular reactive oxygen species (ROS) were produced from zymosan stimulated human whole blood phagocytes and on production of nitric oxide (NO) from lipopolysaccharide (LPS) stimulated J774.2 mouse macrophages. The cytotoxicity of these compounds was evaluated on NIH-3 T3 normal mouse fibroblast cells, antiradical potential on 2,2-diphenyl-1-picrylhydrazylhydrazyl (DPPH·) as well as their anti-yeast potential on four selected candida species. Compound 1 showed higher NO inhibition (IC₅₀ = 23.3 ± 0.3 µg/mL) than standard compound L-NMMA (IC₅₀ = 24.2 ± 0.8 µg/mL). Higher ROS inhibition was shown by compounds 6 (IC₅₀ = 4.3 ± 0.3 µg/mL) and 9 (IC₅₀ = 1.1 ± 0.1 µg/mL) than Ibuprofen (IC₅₀ = 11.2 ± 1.9 µg/mL). Furthermore, compound 1 displayed moderate level of cytotoxicity on NIH-3 T3 cells, with IC₅₀ = 5.8 ± 0.3 µg/mL compared to the cyclohexamide IC₅₀ = 0.13 ± 0.02 µg/mL. Compound 3 showed lower antifungal activity on Candida krusei and Candida glabrata, MIC of 125 μg/mL on each strain compared to 50 μg/mL for fuconazole. The extracts showed low antifungal activities ranging from 250 to 500 μg/mL on C. albicans, C. krusei and C. glabrata and the values of MIC on Candida parapsilosis were 500 μg/mL and above. DPPH* scavenging activity was exhibited by compounds 1 (IC₅₀ = 15.653 ± 0.335 μg/mL) and 3 (IC₅₀ = 89.077 ± 24.875 μg/mL) compared to Vitamin C (IC₅₀ = 3.343 ± 0.271 μg/mL) while extracts showed moderate antiradical activities with IC₅₀ values ranging from 309.31 ± 2.465 to 635.52 ± 11.05 µg/mL. These results indicate that compounds 1, 6 and 9 are potent anti-inflammatory drug candidates while 1 and 3 could be potent antioxidant drugs.     

Synthesis and evaluation of novel sulfonamide analogues of 6/7-aminoflavones as anticancer agents via topoisomerase II inhibition

A series of new sulfonamide analogues of 6/7-aminoflavones were synthesized by using molecular hybridization approach. These new sulfonamide analogues were screened for antiproliferative activity against human hepatocellular carcinoma (HepG-2), human lung cancer cell line (A-549), human colorectal adenocarcinoma (Caco-2) cancer cell lines. Compounds 5p, 5q, 5t, 5v, 5w and 5x exhibited good anticancer activity against selected cancer cell lines. These compounds were further evaluated to predict their ability to inhibit topoisomerase-II enzyme. Compound 5x has shown potent antiproliferative activity (IC₅₀ value 0.98 µM) as compared to standard drug Adriamycin (IC₅₀ = 0.94 µM) indicating that these compounds exhibits anticancer activity via inhibition of topoisomerase-II enzyme. Docking results also have supported above observations by indicating that compounds are held in the active pocket by combination of various hydrogen and hydrophobic interactions with Top II-DNA-etoposide enzyme.     

Green synthesis of silver nanoparticles using Citrus limon peels and evaluation of their antibacterial and cytotoxic properties

The present work aimed to synthesis silver nanoparticles (AgNPs) using biological waste products Citrus limon peels, its characterization, antimicrobial activities and the cytotoxic effect of the synthesized green AgNPs. Characterization of the prepared AgNPs showed the formation of spherical, and few agglomerated AgNPs forms as measured by UV–visible spectrophotometer. The average size of the prepared AgNPs was 59.74 nm as measured by DLS technique. The spectrum of the synthesized AgNPs was observed at 3 KeV using the EDX. On the other hand, FTIR analysis of the green synthesized AgNPs showed the presence of alcohols, phenolics, mono-substituted alkynes, aliphatic primary amines, sodium salt, amino acid, or SiOH alcohol groups. The antimicrobial studies of the formed AgNPs showed positive activity against most of the studied human pathogenic bacteria with varying degrees. Finally, the evaluation of the cytotoxic effect of the green synthesized AgNPs were done using two types of cell lines, human breast cancer cell line (MCF-7) and human colon carcinoma cell line (HCT-116). The results revealed the concentration has a direct correlation with cell viability. The 50% inhibitory concentration (IC₅₀) of MCF-7 cell line was in of 23.5 ± 0.97 µL/100 µL, whereas the HCT-116 cell line was in 37.48 ± 5.93 µL/100 µL.     

Development of alternative medicinal sources from golden berry,bananas and carrot wastes as antioxidant,cytotoxic and antimicrobial agents

Discovering new medicinal sources from food wastes is a beneficial and valuable way instead of their disposal. Fruits and vegetables waste can be an inexpensive and readily available source of bioactive compounds to be used in pharmaceutical industries. The aim of this study is to highlight the in vitro antioxidant, cytotoxic, and antimicrobial activities of the total extracts of banana peels (Musa acuminate), carrot peels (Daucus carota) and golden berry husk (Physalis peruviana) besides evaluating their in vivo acute and chronic toxicity profiles as well as their antimutagenic activity. Also, we investigated their phenolic and flavonoid contents spectrophotometrically and by HPLC. Results showed that D. carota peels revealed the highest antioxidant activity (29.903 mg TE/g) using DPPH free radical scavenging assay. Cytotoxic outcomes (SulphoRhodamine-B method) showed that the highest cytotoxic activity of M. acuminate peels (IC₅₀: 20.7 μg/mL) was exerted on HEPG2 cell line, where D. carota peels (IC₅₀: 18.8 μg/mL) showed the highest cytotoxic activity on PC-3 cell line. In addition, pH. peruviana husk (IC₅₀: 10.5 ± 1.0 μg/mL) showed a potent cytotoxic activity on HCT-116 that is non-significant from the standard Doxorubicin (IC₅₀: 11.5 ± 0.8 μg/mL). For the antimicrobial activity (agar diffusion assay), most of the total extracts revealed notable activities against all tested pathogens relative to the standards; ciprofloxacin and ketoconazole, specially Ph. peruviana husk that showed a potent inhibitory activity (inhibition zone diameter of 29 mm.) against C. albicans even more than the standard ketoconazole (inhibition zone diameter of 28 mm.). These promising biological activities are mainly related to the high content of flavonoids and phenolic compounds identified and quantified in their total extracts. Moreover, the three extracts proved their in vivo safety on the short and long terms as well as their possible antimutagenic effect on the genotoxicity of the drug cyclophosphamide (CP) in both bone marrow cells and spermatocyte cells.     

In vitro bioactivities and preparation of nanoemulsion from coconut oil loaded Curcuma aromatica extracts for cosmeceutical delivery systems

Curcuma aromatica (CA) is a herbaceous plant in the Zingiberaceae family. It has antioxidative activity and anti-inflammatory properties. The purpose of this study was to investigate the effect of solvents and extraction methods on CA rhizomes. The crude extracts were tested for phenolic and flavonoid contents, antioxidative activity by DPPH and lipid peroxidation assay, and protein denaturation inhibition. The crude extracts with 95% ethanol by maceration technique showed good results. It had phenolic content at 99.28 ± 1.09 mg GAE/g extract, flavonoid content at 397.00 ± 27.54 mg QE/g extract, antioxidative activity by DPPH assay and lipid peroxidation assay at IC₅₀ value of 0.55 ± 0.02 mg/ml and 0.60 ± 0.10 mg/ml, respectively. The percentage of protein denaturation inhibition was 65.97 ± 4.68%. The crude extract with 95% ethanol by maceration technique was selected to formulate nanoemulsion. Nanoemulsion formulation consisted of DI water, Tween 80, CA extract, coconut oil and Span 80 at 72.50, 12.93, 7.07, 5.00 and 2.5%w/w, respectively. Its appearance was an opaque yellow liquid with no precipitation and no phase separation at room temperature. The particle size, pH, and viscosity were 70.20 ± 0.38 nm, 5.87 ± 0.01 and 3.56 ± 0.24 cP, respectively. Nanoemulsion loaded CA extract had bioactivities and highly stable characteristics after heating–cooling test for 6 cycles. This study has demonstrated the potential of nanoemulsion from coconut oil loaded CA extract for further development to novel cosmetic products.     

Design and synthesis of aminocoumarin derivatives as DPP-IV inhibitors and anticancer agents

DPP-IV “a moonlighting protein” has immerged as promising pathway to control Type 2 diabetes as well as found to play key role in earlier stages of cancer. Here we have reported design, synthesis and applications of aminocoumarin derivatives as DPP-IV inhibitors. Compounds have been synthesized and studied for their DPP-IV inhibition activity. Three compounds have shown moderate inhibition at 100 µM concentration. All compounds were also screened for their anticancer activity against A549 (Lung cancer cell line), MCF-7 (Breast cancer cell line) using MTT assay. One of the compounds has shown very good anticancer activity with IC₅₀ value 24 ± 0.1 nM against A549 cell line.     

Glutathione S-transferase pi (GST-pi) inhibition and anti-inflammation activity of the ethyl acetate extract of Streptomyces sp. strain MJM 8637

To investigate the anti-cancer properties of soil-borne actinobacteria, MJM 8637, the glutathione S-transferase pi (GST-pi) assay, anti-tumor necrosis factor (TNF)-α assay, the level of antioxidant potential by DPPH radical scavenging activity, NO scavenging activity, and ABTS radical scavenging activity in ethyl acetate extract were determined. The 16S rDNA sequencing analysis revealed that Streptomyces sp. strain MJM 8637, which was isolated from Hambak Mountain, Korea, has 99.5% similarity to Streptomyces atratus strain NBRC 3897. The physiological and the morphological characteristics of the strain MJM 8637 were also identified. The ethyl acetate extract of MJM 8637 inhibited TNF-α production approximately 61.8% at concentration 100 μg/ml. The IC₅₀ value of the strain MJM 8637 extract on GST-pi was identified to be 120.2 ± 1.6 μg/ml. In DPPH, NO, and ABTS radical scavenging assays, the IC₅₀ values of the strain MJM 8637 extract were found to be 977.2 μg/ml, 1143.7 μg/ml, and 454.4 μg/ml, respectively. The ethyl acetate extract of the strain MJM 8637 showed 97.2 ± 1.3% of cell viability at 100 μg/ml in RAW 264.7 cell viability assay. The results obtained from this study suggest that the ethyl acetate extract of Streptomyces sp. strain MJM 8637 could be considered as a potential source of drug for the cancers that have multidrug resistance with its GST-pi inhibition and anti-inflammation activities, and low cytotoxicity.