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

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

OBJECTIVETo Isolate, purify, characterize, and evaluate the bioactive compounds from the sponge-derived fungus Penicillium sp. FF001 and to elucidate its structure.

METHODSThe fungal strain FF001 with an interesting bioactivity profile was isolated from a marine Fijian sponge Melophlus sp. Based on conidiophores aggregation, conidia development and mycelia morphological characteristics, the isolate FF001 was classically identified as a Penicillium sp. The bioactive compound was identified using various spectral analysis of UV, high resolution electrospray ionization mass spectra, 1H and 13C NMR spectral data. Further minimum inhibitory concentrations (MICs) assay and brine shrimp cytotoxicity assay were also carried out to evaluate the biological properties of the purified compound.

RESULTSBioassay guided fractionation of the EtOAc extract of a static culture of this Penicillium sp. by different chromatographic methods led the isolation of an antibacterial, anticryptococcal and cytotoxic active compound, which was identified as citrinin (1). Further, citrinin (1) is reported for its potent antibacterial activity against methicillin-resistant Staphylococcus aureus (S. aureus), rifampicin-resistant S. aureus, wild type S. aureus and vancomycin-resistant Enterococcus faecium showed MICs of 3.90, 0.97, 1.95 and 7.81 µg/mL, respectively. Further citrinin (1) displayed significant activity against the pathogenic yeast Cryptococcus neoformans (MIC 3.90 µg/mL), and exhibited cytotoxicity against brine shrimp larvae LD50 of 96 µg/mL.

CONCLUSIONSCitrinin (1) is reported from sponge associated Penicillium sp. from this study and for its strong antibacterial activity against multi-drug resistant human pathogens including cytotoxicity against brine shrimp larvae, which indicated that sponge associated Penicillium spp. are promising sources of natural bioactive metabolites.

Animals ; Anti-Bacterial Agents ; chemistry ; pharmacology ; Artemia ; drug effects ; Citrinin ; chemistry ; pharmacology ; Drug Resistance, Multiple, Bacterial ; drug effects ; Lethal Dose 50 ; Methicillin-Resistant Staphylococcus aureus ; drug effects ; Microbial Sensitivity Tests ; Penicillium ; chemistry ; cytology ; Porifera ; microbiology ; Toxicity Tests

OBJECTIVETo investigate the antioxidant, antibacterial and cytotoxic activity of whole Leucas aspera (Labiatae) (L. aspera) alcoholic extract.

METHODSWhole L. aspera powder was extracted by absolute ethanol (99.50%). The ethanolic extract was subjected to antioxidant, antibacterial and brine shrimp lethality assay.

RESULTSThe extract showed potent radical scavenging effect (antioxidant) with IC50 value of (99.58±1.22) µg/mL which was significant (P<0.01) in comparison to ascorbic acid with IC50 value of (1.25±0.95) µg/mL. In case of antibacterial screening, the extract showed notable antibacterial effect against the tested microbial strains. Significant (P<0.05) zone of inhibitions against Gram positive Bacillus subtilis [(12.00±1.32) mm] and Bacillus megaterium [(13.00±1.50) mm], Staphylococcus aureus [(8.00±0.50) mm] and Gram negative Salmonella typhi [(6.00±0.50) mm], Salmonella paratyphi [(8.00±1.00) mm], Shigella dysenteriae [(9.00±1.32) mm] and Vibrio cholerae [(9.00±0.66) mm] was observed. In brine shrimp lethality bioassay, the extract showed the LC50 value as (181.68±2.15) µg/mL which was statistically significant (P<0.01) compared to positive control vincristine sulfate [LC50=(0.76±0.04) µg/mL].

CONCLUSIONSThe results demonstrate that the ethanolic extract of L. aspera could be used as antibacterial, pesticidal and various pharmacologic actives.

Animals ; Anti-Bacterial Agents ; chemistry ; pharmacology ; Antioxidants ; chemistry ; pharmacology ; Artemia ; drug effects ; Biphenyl Compounds ; antagonists & inhibitors ; Dose-Response Relationship, Drug ; Inhibitory Concentration 50 ; Lamiaceae ; chemistry ; Microbial Sensitivity Tests ; Phytochemicals ; chemistry ; pharmacology ; Picrates ; antagonists & inhibitors ; Plant Extracts ; chemistry ; pharmacology ; Toxicity Tests

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

OBJECTIVETo elucidate potential antioxidant, antidiarrheal, cytotoxic, and antibacterial activities of the ethanol extract of Alocasia indica Schott tuber in different experimental models established in vitro and in vivo.

METHODSIn vitro antioxidant activity was evaluated by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging assay. Phenolic content was estimated by using Folin-Ciocalteu's reagent while reducing ability was measured by ferric reducing power assay. In vivo antidiarrheal studies were carried out in mice, and the activity was evaluated in castor oil and magnesium sulfate-induced diarrhea. Disk diffusion assay was utilized to determine antibacterial activity against a number of pathogenic bacterial strains. Acute toxicity test was carried out to measure the safe doses for the extract.

RESULTSIn DPPH radical-scavenging assay, the extract exhibited strong radical-scavenging activity with the 50% inhibitory concentration value of 42.66 μg/mL. Total phenolic content was found to be 542.26 mg gallic acid equivalent per 100 g of dried tuber extract, whereas flavonoid content was found to be 4.30 mg quercetin equivalent/g of dried tuber extract. In reducing power assay, the extract showed strong reducing power in a concentration-dependent manner. The extract significantly (P < 0.01) enhanced the latent period and decreased defecation in both castor oil- and magnesium sulfate-induced diarrhea. The extract also lessened gastrointestinal motility in mice. Potential antibacterial activity was exhibited by the extract against all the tested bacterial strains in disk diffusion assay. The 50% lethal concentration against brine shrimp nauplii was 81.09 μg/mL.

CONCLUSIONThe results demonstrated that the ethanol extract of A. indica has potential antioxidant, antidiarrheal, cytotoxic, and antibacterial activity.

Alocasia ; chemistry ; Animals ; Anti-Bacterial Agents ; pharmacology ; Antidiarrheals ; pharmacology ; Antioxidants ; pharmacology ; Artemia ; drug effects ; Female ; Gastrointestinal Motility ; drug effects ; Male ; Mice ; Plant Extracts ; pharmacology ; toxicity

OBJECTIVETo evaluate antioxidant, antimicrobial and cytotoxic activity of different parts (root, flower, leaf and stem) of Leucas aspera (L. aspera) (Labiatae).

METHODSDifferent parts of L. aspera were extracted with 80% (v/v) methanol. The methanol extracts were subjected to antioxidant, antimicrobial and brine shrimp lethality assay.

RESULTSAll the extracts showed moderate to potent antioxidant activity, among which the root extract demonstrated the strongest antioxidant activity with the IC50 value of 6.552 µg/mL. Methanol extract of root possessed antioxidant activity near the range of vitamin E and thus could be a potential rich source of natural antioxidant. In case of antimicrobial screening, crude extracts of root, flower, leaf and stem showed notable antibacterial activity against tested microorganisms. The root extract showed the highest mean zone of inhibition ranging from 9.0-11.0 mm against tested microorganisms, at a concentration of 100 mg/mL. In the brine shrimp lethality bioassay, it was evident that the methanol root extract did not show significant toxicity. The LC50 value for 12 h and 24 h observation was 2.890 mg/mL and 1.417 mg/mL, respectively.

CONCLUSIONSThe present finding suggests that the methanol root extract of L. aspera could be developed as pharmaceutical products.

Animals ; Anti-Bacterial Agents ; chemistry ; pharmacology ; toxicity ; Antioxidants ; chemistry ; pharmacology ; toxicity ; Artemia ; drug effects ; Bacteria ; drug effects ; Biphenyl Compounds ; metabolism ; Lamiaceae ; chemistry ; Methanol ; Microbial Viability ; drug effects ; Picrates ; metabolism ; Plant Components, Aerial ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; toxicity ; Plant Roots ; chemistry

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