In vitro cytotoxic potential of Solanum nigrum against human cancer cell lines

Plants have natural products which use to possess antiproliferative potential against many cancers. In the present study, six isolated fractions (ethyl acetate, petroleum ether, chloroform, n-butanol, ethanol and aqueous) from Solanum nigrum were evaluated for their cytotoxic effect on different cell lines. Hepatic carcinoma cell line (HepG2), cervical cancer cell line (HeLa) and baby hamster kidney (BHK) used as normal non-cancerous cells were evaluated for cytotoxicity against isolated fractions. Cell viability assay was performed to evaluate the cytotoxicity of all fractions on different cell lines followed by the lactate dehydrogenase and vascular endothelial growth factor assays of most active fraction among all screened for cytotoxic analysis. HPLC analysis of most active fractions against cytotoxicity was performed to check the biological activity of compounds. Results displayed the potent cytotoxic activity of ethyl acetate fraction of S. nigrum against HepG2 cells with IC₅₀ value of 7.89 μg/ml. Other fractions exhibited potent anticancer activity against HepG2 cells followed by HeLa cells. Fractions in our study showed no cytotoxicity in BHK cells. Cytotoxic activity observed in our current study exposed high antiproliferative potential and activity of ethyl acetate fraction against HepG2 cells. The results demonstrated that S. nigrum fractions exhibited anticancer activity against hepatic and cervical cancer cell lines with non-toxic effect in normal cells. These results reveal significant potential of S. nigrum for the therapeutic of cancers across the globe in future.     

毛筒壳科真菌次级代谢产物生物活性的评价

毛筒壳科Tubeufiaceae真菌具有产新结构、新活性次级代谢产物的潜力,目前对该科真菌次级代谢产物的研究较少。为了寻找具有生物活性的新化合物,有必要对毛筒壳科真菌次级代谢产物及其活性进行系统深入的研究。本文采用平板对峙法、生长速率法和MTT法,分别测定已分离得到的19株该科真菌活体菌株抑菌活性、发酵物抑菌活性以及发酵物粗提物对不同人体肿瘤细胞株增殖的抑制作用。通过平板对峙法,试验共筛选获得13株活性菌株,其中,红棕毛筒腔菌菌株Tubeufia rubra PF02-2对7种植物病原真菌有明显的抑菌效果,抑制率均高于60%且抑菌谱广。采用生长速率法,发现红棕毛筒腔菌菌株PF02-2经液体发酵后,发酵液对其中4种植物病原真菌仍有一定的抑制作用,且菌丝体部分的乙酸乙酯提取物对马铃薯早疫病病菌Alternaria solani（ZYB）的抑制效果最好。通过MTT法,发现发酵物粗提物对3种肿瘤细胞均具有不同程度的细胞毒活性,其中在300μg/mL时,剑叶莎毛筒腔菌菌株Tubeufia machaerinae ML03-2发酵液部分的乙酸乙酯提取物对人宫颈癌细胞株HeLa和人前列腺癌细胞株PC-3的抑制率（%）分别达到了98.92±0.15和97.86±0.18,在400μg/mL时,对人肝癌细胞株HEPG2的抑制率（%）达到了98.88±0.04;在500μg/mL时,明孢新旋卷孢菌菌株Neohelicosporium hyalosporum ML05-1菌丝体部分的乙酸乙酯提取物对人宫颈癌细胞株HeLa细胞的抑制率（%）为98.32±0.02,在600μg/mL时,对人肝癌细胞株HEPG2的抑制率（%）达到了97.62±0.20,在300μg/mL时,对人前列腺癌细胞株PC-3的抑制率（%）达到了98.91±0.02。该研究结果为开发利用毛筒壳科真菌提供了科学依据。     

The Chemopotential Effect of Annona muricata Leaves against Azoxymethane-Induced Colonic Aberrant Crypt Foci in Rats and the Apoptotic Effect of Acetogenin Annomuricin E in HT-29 Cells: A Bioassay-Guided Approach

Annona muricata has been used in folk medicine for the treatment of cancer and tumors. This study evaluated the chemopreventive properties of an ethyl acetate extract of A. muricata leaves (EEAML) on azoxymethane-induced colonic aberrant crypt foci (ACF) in rats. Moreover, the cytotoxic compound of EEAML (Annomuricin E) was isolated, and its apoptosis-inducing effect was investigated against HT-29 colon cancer cell line using a bioassay-guided approach. This experiment was performed on five groups of rats: negative control, cancer control, EEAML (250 mg/kg), EEAML (500 mg/kg) and positive control (5-fluorouracil). Methylene blue staining of colorectal specimens showed that application of EEAML at both doses significantly reduced the colonic ACF formation compared with the cancer control group. Immunohistochemistry analysis showed the down-regulation of PCNA and Bcl-2 proteins and the up-regulation of Bax protein after administration of EEAML compared with the cancer control group. In addition, an increase in the levels of enzymatic antioxidants and a decrease in the malondialdehyde level of the colon tissue homogenates were observed, suggesting the suppression of lipid peroxidation. Annomuricin E inhibited the growth of HT-29 cells with an IC50 value of 1.62 ± 0.24 μg/ml after 48 h. The cytotoxic effect of annomuricin E was further substantiated by G1 cell cycle arrest and early apoptosis induction in HT-29 cells. Annomuricin E triggered mitochondria-initiated events, including the dissipation of the mitochondrial membrane potential and the leakage of cytochrome c from the mitochondria. Prior to these events, annomuricin E activated caspase 3/7 and caspase 9. Upstream, annomuricin E induced a time-dependent upregulation of Bax and downregulation of Bcl-2 at the mRNA and protein levels. In conclusion, these findings substantiate the usage of A. muricata leaves in ethnomedicine against cancer and highlight annomuricin E as one of the contributing compounds in the anticancer activity of A. muricata leaves.     

Molecular profiling of marine endophytic fungi from green algae: Assessment of antibacterial and anticancer activities

Bioactive natural metabolites, especially from the marine endophytic fungi, are largely unexplored. Endophytic fungi are being increasingly recognized as a group of organisms that produce novel metabolites of industrial importance. This study investigated the anticancer and antibacterial potential of the marine algal endophyte, Penicillium chrysogenum. The different organic solvent extracts of the endophytic fungi grown on different growth medium were analyzed for anticancer and antibacterial activities. The highest inhibitory activity was observed for the ethyl acetate (EA) extract of the culture filtrate grown in potato dextrose broth (PDB) for 21 days, against the tested human breast cancer cell (MCF-7) line. Similarly, the PDB-EA extract showed an appreciable activity against the human pathogens. The biochemical analysis of the Cha EA metabolites revealed terpenoids, steroids, phenolics and flavones. Gas Chromatography (GCMS) data revealed several bioactive compounds such as anthraquinone and cinnamic acid. The Cha EA extract induced membrane damage and thus, apoptosis in MCF-7cells. The secondary metabolites produced by these marine endophytic fungi have contributed to considerable anticancer and antimicrobial activities and hence, this study is an evidence of potential sources of antimicrobial and anticancer compounds from Penicillium chrysogenum.     

Botryorhodines A-D, antifungal and cytotoxic depsidones from Botryosphaeria rhodina, an endophyte of the medicinal plant Bidens pilosa

An endophytic fungus (Botryosphaeria rhodina) was isolated from the stems of the medicinal plant Bidens pilosa (Asteraceae) that is known for its anti-inflammatory, antiseptic and antifungal effects. The ethyl acetate extract of the fungal isolate exhibits significant antifungal activity as well as potent cytotoxic and antiproliferative effects against several cancer cell lines. Activity-guided fractionation resulted in the isolation of a complex of four depsidones, botryorhodines A-D and the auxin indole carboxylic acid. Botryorhodine A and B show moderate to weak cytotoxic activities against HeLa cell lines with a CC₅₀ of 96.97 μM and 36.41 μM, respectively. In addition, they also show antifungal activity against a range of pathogenic fungi such as Aspergillus terreus (MIC 26.03 μM for botryorhodine A and 49.70 μM for B) and the plant pathogen Fusarium oxysporum (MIC 191.60 μM for botryorhodine A and 238.80 μM for B). A potential role of the endophyte in modulating fungal populations living within or attacking the host plant is discussed.     

Cytotoxic activity of hirsutanone,a diarylheptanoid isolated from Alnus glutinosa leaves

BackgroundThe low efficacy of cancer therapy for the treatment of patients with advanced disease makes the development of new anticancer agents necessary. Because natural products are a significant source of anticancer drugs, it is important to explore cytotoxic activity of novel compounds from natural origin.PurposeThe aim of this work is to evaluate the cytotoxic capacity of hirsutanone, a diarylheptanoid isolated from Alnus glutinosa leaves. Hirsutanone cytotoxic way of action was also studied.Material and methodsThe cytotoxic ability of Alnus glutinosa leaves ethyl acetate extract was studied over HeLa and PC-3 cell lines, with the MTT colorimetric assay. Hirsutanone was isolated from this extract using chromatographic methods, and its structure elucidated by spectroscopic analysis. HT-29 cell viability after hirsutanone treatment was determined using SRB assay. In order to understand hirsutanone way of action, cytotoxicity was evaluated adding the diarylheptanoid and antioxidants. DNA topoisomerase II (topo II) poison activity, was also evaluated using purified topo II and a supercoiled form of DNA that bears specific topo II recognition and binding region; topo II poisons stabilize normally transient DNA-topo II cleavage complexes, and lead an increased yield of linear form as a consequence of a lack of double-strand breaks rejoining.ResultsThe diarylheptanoid hirsutanone was isolated from Alnus glutinosa (L.) Gaertn. (Betulaceae) leaves extract that showed cytotoxic activity against PC-3 and HeLa cell lines. Hirsutanone showed cytotoxic activity against HT-29 human colon carcinoma cells. Pre-treatment with the antioxidants NAC (N-acetylcysteine) and MnTMPyP (Mn(III)tetrakis-(1-methyl-4-pyridyl)porthyrin) reduced this activity, suggesting that reactive oxygen species (ROS) participate in hirsutanone-induced cancer cell death. Using human topo II and a DNA supercoiled form, hirsutanone was found to stabilize topo II-DNA cleavage complexes, acting as a topo II poison.ConclusionOur data suggest that, like curcumin, an induction of oxidative stress and topo II-mediated DNA damage may play a role in hirsutanone-induced cancer cell death. Since both compounds share similar structure and cytotoxic profile, and curcumin is in clinical trials for the treatment of cancer, our results warrant further studies to evaluate the anticancer potential of hirsutanone.     

伊犁野生郁金香内生烟曲霉的分离鉴定及活性

【背景】对郁金香的研究主要集中在种质资源、引种栽培、扩繁育种及化学成分分析方面,而关于伊犁野生郁金香内生菌的研究尚未见报道。【目的】从伊犁野生郁金香中筛选出内生真菌并对其进行抑菌及抗氧化活性研究。【方法】采用组织块培养法和平板划线法对伊犁野生郁金香内生菌进行分离纯化;用斜面低温保存法对内生菌进行保存;以形态学方法和分子生物学方法对分离出的内生真菌进行鉴定;通过液体发酵得到次级代谢产物,对乙酸乙酯萃取发酵产物进行滤纸片抑菌分析。使用Fe3+总还原能力法、2-2′二苯基-1-三硝基苯肼(2,2′-diphenyl-1-picrylhydrazyl,DPPH)自由基法、 2′-联氨-双-3-乙基苯并噻唑啉-6-磺酸[2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonicacid,ABTS]自由基法及羟基自由基法比较菌株乙酸乙酯层和水层的抗氧化活性。【结果】从伊犁野生郁金香中分离获得一株内生真菌,经鉴定为曲霉属(Aspergillus)烟曲霉(Aspergillus fumigatus),简称为YGL-1。YGL-1对金黄色葡萄球菌(Staphylo...     

Biological Evaluation of Endophytic Fungus, Chaetomium globosum JN711454, as Potential Candidate for Improving Drug Discovery

The main objective of this research work focused on investigating the biological and chemical aspects of endophytic fungus Chaetomium globosum, for pharmaceutical purposes to improve the drug discovery process. The endophytic C. globosum was isolated from healthy leaves of Egyptian medicinal plant Adiantum capillus-veneris collected from Saint Katherine Protectorate, Sinai, Egypt. The identification of C. globosum was on the basis of classical and molecular taxonomy. Gene encoding for 18S rRNA was partially sequenced, submitted to the GenBank and got the accession number JN711454, to resolve the phylogenetic relations with fungal ancestor using phylogenetic tree. To explore the biosynthetic power of endophytic C. globosum JN711454, the fungus was cultivated over five different media, oatmeal, rice, yeast malt glucose, potato dextrose agar (PDA) and Czapek’s dox media, for 3 weeks at 30 °C, followed by extraction with different solvents, ethyl acetate (EA), and methanol. The ethyl acetate extract of C. globosum cultivated on PDA medium was the most potent extract. It showed strong antioxidant activity with EC₅₀ 11.5 μg/ml, potent anticancer activity with 55 % toxicity toward HepG-2 cells at 100 μg/ml and 66 % cytotoxicity to FGC₄ cells at 250 μg/ml, promising butyrylcholinesterase inhibitory activities (>85 %), and moderate antimicrobial and stopped the attachment of HSV-2 virus to VERO cells. The metabolomic profiling of PDA–EA extract using LC–MS revealed the presence of several metabolites to which the observed bioactivities could be attributed. Here we report for the first time inhibitory activity of endophytic C. globosum JN711454 secondary metabolites to butyrylcholinesterase, one of neuro hydrolase enzymes that play a major role in development of Alzheimer’s disease.     

Screening and characterization of endophytic fungi of Panax ginseng Meyer for biocontrol activity against ginseng pathogens

Forty endophytic fungi isolated from ginseng plants were screened to identify metabolites that had antifungal activity against ginseng microbial pathogens. The metabolites from the fungi were extracted from the liquid culture filtrates using ethyl acetate and then evaluated in vitro for antimicrobial activity against ginseng pathogens (Alternaria panax, Botrytis cinerea, Colletotrichum panacicola, Cylindrocarpon destructans, Rhizoctonia solani, and Phytophthora cactorum). Six of the fungi (Colletotrichum pisi, Fusarium oxysporum, Fusarium solani, Phoma terrestris, unknown 1 and 2) showed effective antimicrobial activity against all or some of the ginseng pathogens, with the extract of P. terrestris showing the strongest antimicrobial activity. The extract also showed inhibitory activity against spore germination of the pathogens. Gas chromatography–mass spectrometry (GC–MS) analysis of P. terrestris extract revealed that forty-one compounds were present in metabolites containing mainly N-amino-3-hydroxy-6-methoxyphthalimide (32% of the total metabolites) and 5H-dibenz [B, F] azepine (7%). Treatment with P. terrestris extract also caused morphological changes and reduced expression of the genes involved in mycelial growth and virulence. Treatment also induced defense-related genes in detached Arabidopsis leaves that were inoculated with the pathogens. These results indicate the antimicrobial potential for use of metabolites extracted from the ginseng endophytic fungi as alternatives to chemicals for biocontrol.     

盐角草内生真菌分离鉴定及抑制水产腐败细菌菌株的筛选

盐角草是一种耐盐植物,有重要的食用、药用价值.为研究盐角草的内生真菌及其活性次生代谢产物的多样性,该文对采集于广西北部湾沿海盐角草的内生真菌进行分离纯化,采用RAPD对内生真菌多样性进行分析,采用ITS基因序列对内生真菌进行鉴定,并对内生真菌提取物抑制等3种水产腐败细菌的活性进行筛选.结果表明:(1)从北部湾盐角草植物...     

Antiulcerogenic activity of the hydroalcoholic extract of leaves of Annona muricata Linnaeus in mice

Annona muricata Linnaeus, popularly known as “graviola” and also called soursop, is a species typical of countries with a tropical climate, and it is used in folk medicine as an anticancer, analgesic and antispasmodic agent. The aim of the present study was to validate the gastroprotective activity of the hydroalcoholic extract of the leaves of A. muricata (HEAM) and to investigate the underlying mechanisms of action for this effect. Gastric lesions were induced in mice by absolute ethanol, acidified ethanol or indomethacin. Before, the animals were pretreated with saline, omeprazole or HEAM orally at doses of 50–400 mg/kg. To determine the mechanism of action of the extract, we investigated, using specific inhibitors, the involvement of nitric oxide (NO), prostaglandins (PGEs), ATP-dependent K⁺ channels and α2-noradrenergic receptors. HEAM showed significant antiulcer activity against lesions induced by absolute ethanol, acidified ethanol or indomethacin, which was mediated by endogenous gastric prostaglandins.     

The chemical composition,antifungal, antioxidant and antimutagenicity properties of bioactive compounds from fungal endophytes associated with Thai orchids

Some plant‐derived bioactive compounds produced by fungal endophytes have been proven to have antimicrobial and antioxidant activities. In this study, endophytic fungi were isolated from 20 orchid samples collected in northern Thailand from 12 genera of orchids. In total, 97 isolates were isolated from the leaves (44.3%), stems (40.2%) and flowers (15.5%) of the orchid samples. The antifungal activity was investigated of the endophytic isolates against the plant pathogenic fungi. The results showed that 13 endophytic isolates provided antifungal activities against Fusarium sp., Colletotrichum sp. and Curvularia sp. The endophyte CK F05‐5, which was isolated from the flower part of Dendrobium lindleyi, was chosen for further testing because it the highest level of antifungal activity against Fusarium sp. The isolate CK F05‐5 was identified as Fusarium oxysporum on the basis of its ITS sequences of 5.8 s rRNA, and phytochemical analysis revealed the presence of coumarins. The ethyl acetate extract of CK F05‐5 was examined for its total phenolic content and antioxidant activity using Folin–Ciocalteu's reagent and 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) radical scavenging assay, respectively. The phenolic content was 160.51 mg of GAE/g of extract, and the free radical scavenging activity was 89.61 µg/ml at the half maximal inhibitory concentration (IC₅₀). The antimutagenic potential of the ethyl acetate extract of CK F05‐5 against Trp‐P‐1 mutagenic substances was determined using the Ames test which revealed that the extract of CK F05‐5 at 10 mg/plate had the highest antimutagenic activity against Trp‐P‐1 (51.2%) and 39.6% for strains TA98 and TA100, respectively. The active compounds present in the acetate extract of CK F05‐5 were examined using GC‐MS analysis, which displayed the presence of gibepyrone A, pyrrolo [1, 2‐a] pyrazine‐1, 4‐dione, hexahydro‐3‐(2‐methylpropyl) and indoleacetic acid as major components. Based on the results, this endophytic fungus contains various bioactive components that have various biological activities. This useful information could help in producing potentially valuable and novel pharmaceutical products.     

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.     

Broad-spectrum In vitro antimicrobial activities of Streptomyces sp. strain BCNU 1001

Streptomyces sp. strain BCNU 1001 was isolated from forest soil samples. Cultural, morphological, and physiological characteristics as well as 16S rDNA analysis revealed that the isolate, BCNU 1001, belonged to the genus Streptomyces. The antimicrobial activity of the ethyl acetate extract was confirmed using the broth microdilution technique. The minimum inhibitory concentration (MIC) of the BCNU 1001 ethyl acetate extract was 0.25 mg/mL for Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa, and 0.125 mg/mL for Micrococcus luteus, Staphylococcus aureus, and Pseudomonas fluorescens. The MIC of the BCNU 1001 ethyl acetate extract for Aspergillus niger, Candida albicans, and Saccharomyces cerevisiae was 0.5, 0.125, and 0.25 mg/mL, respectively. BCNU 1001 was also active against dermatophytic fungi such as Trichophyton mentagrophytes and T. rubrum. Furthermore, BCNU 1001 was also found to be effective against Methicillin-resistant Staphylococcus aureus (MRSA), and its ethyl acetate extract showed MIC = 0.5 mg/mL against MRSA. The most abundant antimicrobial compound was identified as a 2-hydroxybenzyl alcohol through analysis utilizing a nuclear magnetic resonance spectroscopy. This compound was seen to be very effective against some kinds of bacteria and fungi.     

Cytotoxic cycloartane triterpenoids from the leaves of Markhamia stipulata var. canaense

From the most cytotoxic fraction of the ethyl acetate extract of Markhamia stipulata var. canaense V.S. Dang leaves, two new cycloartane-type triterpenoids, named Markhacanasin A (1) and Markhacanasin B (2); were isolated by various chromatographic methods Their structures were elucidated by IR, UV, HR-ESI–MS, NMR (1D & 2D) experiments. The cytotoxicity of two new compounds against five human cancer cell lines (HeLa, HepG2, MCF-7, Jurkat and NCI-H460) were evaluated by SRB assay. As results, 1 exhibited significant cytotoxic activity against all cancer cell lines (IC₅₀ ranged from 14.72 to 29.55 μM) while 2 did not show activity.     

Bionectria ochroleuca NOTL33—an endophytic fungus from Nothapodytes foetida producing antimicrobial and free radical scavenging metabolites

Endophytic fungi are reported to produce diverse classes of secondary metabolites. This study investigated the antimicrobial and free radical scavenging activity of a foliar endophytic fungus from Nothapodytes foetida, a medium sized tree known to produce the antineoplastic compound camptothecin. The fungal isolate was identified as Bionectria ochroleuca based on the ITS rDNA analysis. The differences among endophytic, pathogenic and free living Bionectria ochroleuca were established by RNA secondary structure analysis. The metabolites showed a broad spectrum of antibacterial, antifungal and anti-dermatophytic activity. Minimum inhibitory concentration values of ethyl acetate extracts were in the range of 78–625 μg/mL against all test organisms, except for Pseudomonas aeruginosa (5 mg/mL). Antimicrobial components in the ethyl acetate extract were identified by GC-MS analysis. The isolate was also produced volatile antifungal compounds. A dose-dependent free radical quenching was observed in the ethyl acetate extract. This is the first report on Bionectria sp. as an endophyte of N. foetida. The results indicate that the B. ochroleuca NOTL33 isolate is a potential source of antimicrobial agents and could be used as an effective biofumigant.     

Chemical evaluation and antibacterial activity of novel bioactive compounds from endophytic fungi in Nelumbo nucifera

The objective of this study was to characterize an endophytic fungi producing-bioactive compound from the aquatic plant, Nelumbo nucifera. All parts of such plant were cleaned with surface sterilization technique and cultured on potato dextrose agar to isolate endophytic fungi. The identification was characterized by morphological and molecular technique. Fungal isolates were screened to discover antimicrobial activities by disc diffusion method against Methicillin-resistant Staphylococcus aureus DMST20651 (MRSA). MIC and MBC for those crude fungal extracts were determined. Finally, the chemical profile of crude extract was determined by gas chromatography and mass spectrometry. Six endophytic fungi were isolated from the surface-satirized parts of N. nucifera. Based on disc diffusion assay, the highest antibacterial activity against MRSA was isolate ST9.1 identified as Aspergillus cejpii. Results demonstrated that the ethyl acetate extraction had more active fractions with MIC of 2.5 mg/ml and MBC concentration of 50.0 mg/ml. The crude extracts were developed to identify the chemical constituents by gas chromatography and mass spectrometry. The major component of crude extract of endophytic fungi was 5-(1H-Indol-3-yl)-4,5-dihydro-[1,2,4]triazin-3-ylamine (C₁₁H₁₁N₅). Thus, the plant could be used in the treatment of infectious diseases caused by bacterial pathogen.     

The first bioactivity studies of Acantholimon lycopodioides from high altitude Karakoram-Himalayan desert

Couple of ethnopharmacological surveys in the Indian Ladakh and Pakistani Shigar valleys has reported the medicinal use of Acantholimon lycopodioides against cardiac and gastric disorders that however, remains without scientific rationale or experimental validations. Here, we assess the in vitro bio/therapeutic activities of A. lycopodioides extracts as well as chloroform, ethyl acetate, n-butanol and aqueous fractions. The in vitro β-carotene-linoleic acid bleaching and DPPH radical scavenging methods demonstrated a very high anti-oxidative property of chloroform and ethyl acetate fractions compared to others. Cell viability assay (MTT) on human cervical (HeLa), breast (MDA-MB321) and liver (HepG2) cancer cells revealed their differential cytotoxicity, except the chloroform fraction. Of these, the precipitate exerted highest cytotoxicity on HepG2 cells followed by aqueous fraction on MDA-MB321 cells. Notably, the non-cytotoxicity of chloroform fraction coincided with its highest anti-oxidative activity. Further, the chloroform fraction showed marked hepatoprotection (up to 84%) against 3′7′dichlorofluorescin triggered free radicals induced oxidative damage. Also, the hepatoprotective chloroform fraction mildly activated CYP3A4 in HepG2 cells (dual-luciferase assay). Moreover, the A. lycopodioides extracts and fractions showed differential anti-bacterial and anti-fungal activities. Of these, while S. aureus was more sensitive to the water-insoluble extract, ethyl acetate fraction showed moderate activity against E. coli and C. albicans. On the other hand, the chloroform fraction showed promising activity against S. Aureus, C. albicans, P. vulgaris and E. faecalis. In conclusion, our data for the first time, demonstrated promising anti-oxidative, hepatoprotective, anti-cancer, anti-microbial and CYP3A4 activating salutations of A. lycopodioides. This warrants further studies towards isolation and identification of its therapeutically active principles.     

Induction of apoptosis in human cervical carcinoma HeLa cells by neoechinulin A from marine-derived fungus Microsporum sp.

Recently, the relationship between apoptosis and cancer has been emphasized and the induction of apoptosis is recognized as one of the key mechanisms of anti-cancer agents. Marine-derived fungi are valuable sources of structurally diverse bioactive compounds with anticancer activity. In the present study, a marine-derived fungus, Microsporum sp. was cultured and a prenylated indole alkaloid, neoechinulin A was isolated from the culture broth extract. Neoechinulin A has shown cytotoxic effect on human cervical carcinoma HeLa cells and its apoptosis induction in HeLa cells was investigated by the expressions of p53, p21, Bax, Bcl-2, Caspase 9, and Caspase 3 proteins. Western blot analysis has revealed that neoechinulin A could induce cell apoptosis through down-regulating of Bcl-2 expression, up-regulating of Bax expression, and activating the caspase-3 pathway. Collectively, these results suggest that neoechinulin A could be a potential candidate in the field of anticancer drug discovery against human cervical cancer.     

Two new compounds from Cryptoporus volvatus

Two new compounds with the aldehyde group, cryptoporusal A (1) and 9-formyl-4-hydroxy-6, 9-dimethyl-1-O-β-D-xylosopyranosyl-8a,9-dihydro-ace-naphthylen-8-one (2), were isolated from the ethyl acetate extract of the fruiting bodies of Cryptoporus volvatus (Pk.) Hubbard. Their structures were elucidated by extensive spectroscopic studies, and comparison with literature data. Furthermore, they were evaluated for their in vivo cytotoxicity against five human cancer cell lines and antioxidant activity. Compound 1 exhibited strong cytotoxicity against HL-60 and both showed high ferric reducing capacity.