Five secondary metabolites, including a new isopimarane derivative xylaroisopimaranin A (1), were isolated from the endophytic fungus Xylaralyce sp. (HM-1), and their structures were elucidated by 1D, 2D NMR, MS and CD spectra. Their bioactivities were performed to antibacterial, Hep G2 cells cytotoxicity and brine shrimp inhibition. The biological evaluation results showed that the xylaroisopimaranin A (1), xylabisboein B (2), griseofulvin (3) , 5-methylmellein (4) and mellein-5-carboxlic acid (5) displayed no significant Hep G2 cells cytotoxicity and antibacterial acitivity, but they inhibited the brine shrimp with IC₅₀ from 0.5 to 25 µmol/mL.
Artemia ; Fungi ; Griseofulvin ; Hep G2 Cells

OBJECTIVETo investigate the cytotoxicity of the crude ethanol extract of the rhizome of Zingiber zerumbet (Z. zerumbet) (L) Smith. and Curcuma zedoaria (C. zedoaria) Rosc. against Artemia salina Leach.

METHODSFresh rhizomes of Z. zerumbet (L) Smith. and C. zedoaria Rosc. were extracted separately in cold with ethanol (2.5 L) and after concentration a brownish syrupy suspension of ethanol extracts of Z. zerumbet (L) Smith. and C. zedoaria Rosc. was obtained. The cytotoxic effect of the crude ethanol extracts of both plants was determined by brine shrimp lethality bioassay.

RESULTSCrude ethanol extracts of the rhizome of Z. zerumbet (L) Smith. showed the highest cytotoxicity (LC50 was 1.24 µg/mL) against brine shrimp nauplii as compared with C. zedoaria Rosc. (LC50 was 33.593 µg/mL) after 24 h of exposure.

CONCLUSIONSIt can be concluded that the rhizome of Z. zerumbet (L) Smith. and C. zedoaria Rosc. can be used as a source of cytotoxic agent.

Animals ; Artemia ; drug effects ; Curcuma ; metabolism ; toxicity ; Phytotherapy ; Plant Extracts ; pharmacology ; toxicity ; Plants, Medicinal ; toxicity ; Rhizome ; toxicity ; Zingiberaceae ; metabolism ; toxicity

A phytochemical study on the flowe r of Calotropis gigantea (Linn.) using silica gel column chromatography and preparative thin layer chromatography, led to the first time isolation of Di-(2-ethylhexyl) phthalate (compound 1) and anhydrosophoradiol-3-acetate (compound 2). The structures of these compounds were confirmed by spectroscopic analyses (IR, HRTOFMS and NMR). The antibacterial and antifungal activities of ethyl acetate extract, compound 1 and compound 2 were measured using the disc diffusion method. Ethyl acetate extract and compound 1 presented better results than compound 2. The minimum inhibitory concentrations (MICs) of the extract and compounds were found to be in the range of 16~128 microg/ml. The cytotoxicity (LC50) against brine shrimp nauplii (Artemia salina) were also evaluated and found to be 14.61 microg/ml for ethyl acetate, 9.19 microg/ml for compound 1 and 15.55 microg/ml for compound 2.
Acetates ; Artemia ; Calotropis ; Chromatography ; Chromatography, Thin Layer ; Diffusion ; Flowers ; Microbial Sensitivity Tests ; Phthalic Acids ; Salts ; Silica Gel

The crude ethanol extracts (stem and fruits), their fractions and two triterpenes, beta-Amyrin and 12-Oleanene 3beta, 21beta-diol, isolated as a mixture from the chloroform soluble fraction of an ethanolic extract of Duranta repens stem, were evaluated for antibacterial, antifungal activities by the disc diffusion method and cytotoxicity by brine shrimp lethality bioassay. The structures of the two compounds were confirmed by IR, 1H-NMR, 13C-NMR and LC-MS spectral data. The chloroform soluble fraction of stem and ethanol extract of fruits possess potent antishigellosis activity and also exhibited moderate activity against some pathogenic bacteria and fungi but the isolated compound 1 (mixture of beta-Amyrin and 12-Oleanene 3beta, 21beta-diol) showed mild to moderate inhibitory activity to microbial growth. The minimum inhibitory concentrations (MICs) of the extracts (stem and fruits), their fractions and compound 1 were found to be in the range of 32~128 microg/ml. The chloroform soluble fractions of stem and ethanol extract of fruit showed significant cytotoxicity with LC50 value of 0.94 microg/ml and 0.49 microg/ml, respectively against brine shrimp larvae.
Artemia ; Bacteria ; Biological Assay ; Chloroform ; Complex Mixtures ; Diffusion ; Ethanol ; Fruit ; Fungi ; Larva ; Microbial Sensitivity Tests ; Oleanolic Acid ; Salts ; Triterpenes

BACKGROUND: High-NaCl diet is a contributing factor for cardiac hypertrophy. The role of HSP22 as a protective protein during cardiac hypertrophy due to hypernatremia is unclear. Accordingly, this study aimed to establish a cellular hypernatremic H9C2 model and to compare the expression of HSP22 in Ca2+ homeostasis between a high-NaCl and angiotensin II-induced hypertrophic cellular H9C2 model. METHODS: Real-time PCR was performed to compare the mRNA expression. Flow cytometry and confocal microscopy were used to analyze the cells. RESULTS: The addition of 30 mM NaCl for 48 h was the most effective condition for the induction of hypertrophic H9C2 cells (termed the in vitro hypernatremic model). Cardiac cellular hypertrophy was induced with 30 mM NaCl and 1 µM angiotensin II for 48 h, without causing abnormal morphological changes or cytotoxicity of the culture conditions. HSP22 contains a similar domain to that found in the consensus sequences of the late embryogenesis abundant protein group 3 from Artemia. The expression of HSP22 gradually decreased in the in vitro hypernatremic model. In contrast to the in vitro hypernatremic model, HSP22 increased after exposure to angiotensin II for 48 h. Intracellular Ca2+ decreased in the angiotensin II model and further decreased in the in vitro hypernatremic model. Impaired intracellular Ca2+ homeostasis was more evident in the in vitro hypernatremic model. CONCLUSION: The results showed that NaCl significantly decreased HSP22. Decreased HSP22, due to the hypernatremic condition, affected the Ca2+ homeostasis in the H9C2 cells. Therefore, hypernatremia induces cellular hypertrophy via impaired Ca2+ homeostasis. The additional mechanisms of HSP22 need to be explored further.
Angiotensin II* ; Angiotensins* ; Artemia ; Cardiomegaly ; Consensus Sequence ; Diet ; Embryonic Development* ; Female ; Flow Cytometry ; Homeostasis ; Hypernatremia ; Hypertrophy ; In Vitro Techniques ; Microscopy, Confocal ; Pregnancy ; Real-Time Polymerase Chain Reaction ; RNA, Messenger

In the search for novel potent fungi-derived bioactive compounds for bioinsecticide applications, crude ethyl acetate culture filtrate extracts from 110 mangrove fungal endophytes were screened for their toxicity. Toxicity tests of all extracts against brine shrimp (Artemia salina) larvae were performed. The extracts with the highest toxicity were further examined for insecticidal activity against Spodoptera litura larvae and acetylcholinesterase (AChE) inhibition activity. The results showed that the extracts of five isolates exhibited the highest toxicity to brine shrimp at 50% lethal concentration (LC50) values of 7.45 to 10.24 ppm. These five fungal isolates that obtained from Rhizophora mucronata were identified based on sequence data analysis of the internal transcribed spacer region of rDNA as Aspergillus oryzae (strain BPPTCC 6036), Emericella nidulans (strains BPPTCC 6035 and BPPTCC 6038), A. tamarii (strain BPPTCC 6037), and A. versicolor (strain BPPTCC 6039). The mean percentage of S. litura larval mortality following topical application of the five extracts ranged from 16.7% to 43.3%. In the AChE inhibition assay, the inhibition rates of the five extracts ranged from 40.7% to 48.9%, while eserine (positive control) had an inhibition rate of 96.8%, at a concentration of 100 ppm. The extracts used were crude extracts, so their potential as sources of AChE inhibition compounds makes them likely candidates as neurotoxins. The high-performance liquid chromatography profiles of the five extracts differed, indicating variations in their chemical constituents. This study highlights the potential of culture filtrate ethyl acetate extracts of mangrove fungal endophytes as a source of new potential bioactive compounds for bioinsecticide applications.
Acetylcholinesterase ; Artemia ; Aspergillus oryzae ; Chromatography, Liquid ; Complex Mixtures ; DNA, Ribosomal ; Emericella ; Endophytes* ; Larva ; Mortality ; Neurotoxins ; Physostigmine ; Rhizophoraceae ; Spodoptera ; Statistics as Topic ; Toxicity Tests

A newly synthesized Nickel (II) tyrosine complex was screened as potential antimicrobial agent against a number of medically important bacteria (Bacillus subtilis, Streptococcus beta-haemolytica, Escherichia coli, Shigella dysenterae) and fungi (Aspergillus fumigatus, Candida albicans, Aspergillus niger, Aspergillus flavus, Penicillium sp.) strains. were used for antifungal activity. The antimicrobial activity was evaluated using the Agar Disc method. Moreover, the minimum inhibitory concentration of the complexes was determined against the same pathogenic bacteria and the values were found between 4~64 microg ml(-1). Brine shrimp bioassay was carried out for cytotoxicity measurements of the complexes. The LC50 values were calculated after probit transformation of the resulting mortality data and found to be 6 microg ml(-1).
Agar ; Artemia ; Aspergillus flavus ; Aspergillus niger ; Bacteria ; Biological Assay ; Candida albicans ; Escherichia coli ; Fungi ; Mass Screening* ; Microbial Sensitivity Tests ; Mortality ; Nickel* ; Penicillium ; Shigella ; Streptococcus ; Tyrosine*

OBJECTIVETo investigate the toxicity of methanol extract of various parts (Root, Stem, Leaf, Flower and Fruit) of Lantana camara (L. Camara) in Artemia salina.

METHODSThe methanol extracts of L. camara were tested for in vivo brine shrimp lethality assay.

RESULTSAll the tested extract exhibited very low toxicity on brine shrimp larva. The results showed that the root extract was the most toxic part of L. camara and may have potential as anticancer agent.

CONCLUSIONSMethanolic extract of L. camara is relatively safe on short-term exposure.

Animals ; Artemia ; drug effects ; Dose-Response Relationship, Drug ; Lantana ; chemistry ; Lethal Dose 50 ; Plant Components, Aerial ; chemistry ; Plant Extracts ; toxicity ; Plant Roots ; chemistry

OBJECTIVETo investigate the antioxidant and cytotoxic activity of the flower of Acanthus ilicifolius (A. ilicifolius).

METHODSAntioxidant activity was determined as antiradical efficiency with diphenyl picrylhydrazil (DPPH) method and cytotoxic assay was undertaken using brine shrimp lethal toxicity test.

RESULTSA. ilicifolius flower contained terpenoid, phenolic compounds, and alkaloid. The methanol extract of A. ilicifolius flower showed the highest antiradical efficiency (AE=1.41×10(-3)) against DPPH radicals and the highest cytotoxicity (LC50=22 µg/mL) against brine shrimp nauplii.

CONCLUSIONSIt is suggested that active compounds of A. ilicifolius flower solved in methanol play a role to inhibit free radical activity and kill Artemia salina nauplii. The substances can be considered as potential antioxidant and cytotoxic agents as well as imminent candidate for cancer therapy.

Acanthaceae ; chemistry ; Animals ; Antioxidants ; pharmacology ; Artemia ; drug effects ; Biphenyl Compounds ; chemistry ; pharmacology ; Cytotoxins ; toxicity ; Flowers ; chemistry ; Lethal Dose 50 ; Picrates ; chemistry ; pharmacology ; Plant Extracts ; chemistry ; pharmacology

OBJECTIVETo investigate the antibacterial and cytotoxic activity of fourteen different edible vegetables methanolic extract from Bangladesh.

METHODSThe antibacterial activity was evaluated using disc diffusion assay method against 12 bacteria (both gram positive and gram negative). The plant extracts were also screened for cytotoxic activity using the brine shrimp lethality bioassay method and the lethal concentrations (LC50) were determined at 95% confidence intervals by analyzing the data on a computer loaded with "Finney Programme".

RESULTSAll the vegetable extracts showed low to elevated levels of antibacterial activity against most of the tested strains (zone of inhibition=5-28 mm). The most active extract against all bacterial strains was from Xanthium indicum which showed remarkable antibacterial activity having the diameter of growth inhibition zone ranging from 12 to 28 mm followed by Alternanthera sessilis (zone of inhibition=6-21 mm). All extracts exhibited considerable general toxicity towards brine shrimps. The LC50 value of the tested extracts was within the range of 8.447 to 60.323 µg/mL with respect to the positive control (vincristine sulphate) which was 0.91 µg/mL. Among all studied extracts, Xanthium indicum displayed the highest cytotoxic effect with LC50 value of 8.447 µg/mL.

CONCLUSIONSThe results of the present investigation suggest that most of the studied plants are potentially good source of antibacterial and anticancer agents.

Animals ; Anti-Bacterial Agents ; pharmacology ; Artemia ; drug effects ; Bacteria ; drug effects ; Bangladesh ; Lethal Dose 50 ; Microbial Sensitivity Tests ; Plant Extracts ; pharmacology ; toxicity ; Species Specificity ; Vegetables ; chemistry