• Archives of Pharmacal Research
• /
• v.25 no.5
• /
• pp.652-654
• /
• 2002

Brine shrimp assay-guided fractionation and isolation of the EtOAc soluble fraction of Phryma leptostachya L. (Phrymacaceae) gave two active compounds, phrymarolin II (1) and ursolic acid (2), which were identified by physicochemical and spectroscopic methods. Compound 1 exhibited potent lethality with $LD_{50}$ value of 0.0013 $\mu\textrm{g}$/ml, whereas 2 showed moderate lethality with $LD_{50}$ value of 27.0 $\mu\textrm{g}$/ml against brine shrimp. The cytotoxic activities of 1 and 2 were also evaluated against one murine and five human cancer cell lines employing the sulforhodamin B (SRB) method. Compound 2 exhibited cytotoxic activity against L1210 and SK-MEL-2 cells with $ED_{50}$ values of 3.70 and 9.27 mg/ml, respectively, whereas 1 was devoid of any cytotoxic activity against all cancer cells tested.

• Advances in Traditional Medicine
• /
• v.9 no.2
• /
• pp.182-185
• /
• 2009

Amoora cucullata (Meliaceae), a mangrove plant, has folkloric reputation as a medicinal agent in Bangladesh. In this study, the n-hexane, ethyl acetate and methanolic extracts of the stem bark of this plant were subjected to microbiological investigation and brine shrimp lethality bioassay. In case of antimicrobial screening, the ethyl acetate and methanolic extracts appeared to be potent in terms of both zone of inhibition and spectrum of activity showing the average zones of inhibition 8 - 14 mm and 9 - 16 mm, respectively. In the brine shrimp lethality bioassay, the methanolic extract demonstrated highest cytotoxicity having $LC_{50}$ of $0.549{\mu}g/ml$, whereas the ethyl acetate and n-hexane extract showed $LC_{50}$ of 7.943 and $17.180{\mu}g/ml$, respectively.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1998.11a
• /
• pp.89-94
• /
• 1998

Marine sponges are recognized as a plentiful source of diverse biologically active secondary metabolites. Recently, we have initiated a research to discover antitumor constituents from the marine sponges collected from Korean Waters. Marine sponges collected from the South Sea of Korea were screened for several biological activities including such as brine shrimp lethality and cytotoxicity. Significant brine shrimp lethality was detected in the crude extract of a two-sponge association of Poecillastra sp. and Jaspis sp. A cross-section of this sample showed two layers of morphologically distinct sponges. The thin and dirty yellow outer layer was identified as Poecillastra sp. (Pachastrellidae), the surface of which was very rough. The light-grey inner layer was identified as Jaspis sp. (Jaspidae), the surface of which was smooth. This two-sponge association appears to be consistent as these sponges were always found in associated form regardless of collection site or collection period. Investigation of the bioactive constituents monitored by brine shrimp lethality assay led to the isolation of pectenotoxin II (PTX2) and psammaplin A as causative compounds for the brine shrimp lethality. $^1$H- and $\^$13/C-nmr signals of PTX2 was fully assigned utilizing TOCSY, HETCOR, Long-range HETCOR, and Homonuclear J-resolved 2D experiments. PTX2 displayed very potent and selective cytotoxicities in the 60 cell line panel antitumor assay at the NCI. PTX2 has progressed to acute toxicity determination and in vivo antitumor assay at the NCI (Table 1). However, significant in vitro antitumor activity of PTX2 can not be affirmed in the in vivo assay.

• Advances in Traditional Medicine
• /
• v.6 no.2
• /
• pp.121-125
• /
• 2006

The crude ethanol extract of the stem bark of Trewia polycarpa (Family: Euphorbiaceae) was subjected to acetic acid induced writhing inhibition, Brine Shrimp lethality bioassay and 1, 1-diphenyl-2-picryl hydrazyl free radical scavenging assay for screening of analgesic, cytotoxic and antioxidant activity respectively. The extract produced significant (P < 0.001) writhing inhibition in acetic acid induced writhing in mice at the dose of 125, 250 and 500 mg/kg body weight respectively, which were comparable to the standard drug diclofenac sodium. The extract showed significant lethality to Brine Shrimp and the $LC_{50}$ value was $8\;{\mu}g/ml$. The extract showed prominent free radical scavenging activity ($IC_{50}$ about ${\sim}10\;{\mu}g/ml$) compare to standard drug ascorbic acid ($IC_{50}about\;{\sim}15\;{\mu}g/ml$). The results tend to suggest that the crude ethanol extract of the bark might possess analgesic, cytotoxic and antioxidant activities or active constituent(s) responsible for the activities.

• Advances in Traditional Medicine
• /
• v.5 no.1
• /
• pp.21-28
• /
• 2005

The leaf extracts of Araucaria bidwillii Hook. (Araucariaceae) were evaluated for their cytotoxic effect in various human cancer cell lines. Preliminary investigation by brine shrimp lethality assay indicated that $LC_{50}$ value of various successive extracts were found to be less than $1000\;{\mu}g/ml$, where the ethyl acetate extract showed maximum activity of less than $100\;{\mu}g/ml$. Further cytotoxic evaluation of various leaf extracts of Araucaria bidwilli Hook was carried out in four different human cancer cell lines-acute myeloblastic leukemia (HL-60), chronic myelogenic leukemia (K-562), breast adenocarcinoma (MCF-7) and cervical epithelial carcinoma (HeLa). Cytotoxicity was assessed by trypan blue dye exclusion method and 3-(4,5-dimethyl thiazole-2yl)-2,5-diphenyl tetrazolium bromide (MTT) reduction assay. From the present investigation it was found that the ethyl acetate and methanol extract of Araucaria bidwilli Hook was found to be more effective in leukemic cell lines and was less effective in MCF-7 and HeLa. The $IC_{50}$ value of the ethyl acetate extract in leukemic cell lines was found to be $28.18\;and\;34.64\;{\mu}g/ml$ and methanol extract was found to be $33.11\;&\;39.81\;{\mu}g/ml$. It can be concluded that various extract from the leaves of Araucaria bidwillii Hook. posses cytotoxic activity tested in brine shrimps and various human carcinoma cell lines.

• Advances in Traditional Medicine
• /
• v.10 no.4
• /
• pp.304-309
• /
• 2010

Scutellaria pinnatifida A. Hamilt. (Lamiaceae) is an endemic Turkish herb. This plant is also endemic to Iran, and grows abundantly in other central and western Asian countries. Several species of the Scutellaria are known for their traditional uses in the treatment of hypertension, arteriosclerosis, inflammatory diseases, hepatitis, allergy, cancer and diarrhoea. Free-radical-scavenging property, antibacterial activity and brine shrimp toxicity of the n-hexane, dichloromethane (DCM) and methanol (MeOH) extracts of S. pinnatifida were assessed using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay, the resazurin microtitre plate based assay, and the brine shrimp lethality assay, respectively. The DCM and MeOH extracts exhibited free-radical-scavenging property, with the $RC_{50}$ values of 0.362 and 0.127 mg/ml, respectively. Among the solid-phase extraction fractions of the MeOH extract, the 50% aqueous-MeOH fraction showed the highest level of free-radicalscavenging activity ($RC_{50}$ = 0.039 mg/ml). While the DCM extract showed low level of antibacterial activity against Bacillus subtilis and ampicillin-resistant Escherichia coli, the MeOH extract was active against B. cereus, B. subtilis, E. coli and ampicillin-resistant E. coli. However, the minimum inhibitory concentrations (MIC) of the MeOH extract against these bacterial strains were >10 mg/ml. None of the extracts showed any significant toxicity towards brine shrimps ($LD_{50}$ = > 1.00 mg/ml).

• Korean Journal of Pharmacognosy
• /
• v.38 no.3 s.150
• /
• pp.227-233
• /
• 2007

Seven compounds were isolated from the n-BuOH soluble fraction of stem of Rhododendron mucronulatum as cytotoxic principles against brine shrimp lethality test. On the basis of spectral data, seven compounds were identified as (-)-catechin (1), (+)-epicatechin (2), taxifolin (3), scopoletin (4), quercetin (5), $taxifolin-3-O-{\alpha}-L- arabinopyranoside$ (6), and astragalin (7). Among tested compounds, $taxifolin-3-O-{\alpha}-L-arabinopyranoside$ (6) exhibited potent activity with $LC_{50}$ value at 4.6 ${\mu}g/ml$.

• Archives of Pharmacal Research
• /
• v.22 no.5
• /
• pp.524-528
• /
• 1999

cis-Annonacin (1) and the mixture of (2,4)-cis-and trans-isoannonacins (2 and 3), three known mono-tetrahydrofuran annonaceous acetogenins, have been isolated form the seeds of Annona cherimolia by the use of the brine shrimp lethality test (BST) for bioactivity directed fractionation. Their structures were elucidated based on spectroscopic and chemical methods. 1 showed potent cytotoxicities in the brine shrimp lethality test (BST) and among six human solid tumor cell lines with notable selectivity for the pancreatic cell line (PaCa-2) at about 1,000 times the potency of adriamycin. The mixture of 2 and 3 is over 10,000 times cytotoxic as adriamycin in the pancreatic cell line (PaCa-2). All of the compounds are about 10 to 100 times as cytotoxic as adriamycin in the prostate cell line (PC-3).

• Archives of Pharmacal Research
• /
• v.24 no.4
• /
• pp.300-306
• /
• 2001

A novel and two known bioactive mono-tetrahydrofuran (THF) annonaceous acetogenins, annomocherin (1), annonacin (2) and annomontacin (3), have been isolated from the fractionated ethanolic extracts of the seeds of Annona cherimolia, guided by the brine shrimp lethality test (BST). Their structures were elucidated on the basis of spectroscopic and chemical methods. All compounds have a relative stereochemistry of threo/trans/threo for the mono-THF ring with two flanking hydroxyls. Compound 1 has a double bond at C-23/ 24 of aliphatic chain. Compound 1 was isolated from natural sources for the first time, and was named annomocherin. Two known Compounds 2 and 3 which have never been isolated from this species before, were obtained. Compound 1 exhibited potent and selective cytotoxicities against the breast carcinoma (MCF-7) and kidney carcinoma (A-498) cell lines with 100 to 1,000 times the potency of adriamycin. In brine shrimp lethality test (BST), 1-3 exhibited cytotoxicity.

• Natural Product Sciences
• /
• v.6 no.3
• /
• pp.131-134
• /
• 2000

The methanol, dichloromethane, petroleum ether, 90% methanol and 1-butanol fractions of 40 Malaysian medicinal plants belonging to 25 families were tested for brine shrimp lethality. Various parts and fractions of eight (20%) plants, viz. Annona muricata, Cerbera odollam. Calophyllum inophyllum, Entada phaseoloides, Pithecellobium jiringa, Crotolaria retusa, Morinda elliptica and Sellaginella willdenovii showed very strong toxicity $(LC_{50}:$<$100\;ppm)$. The methanol extract of the seed of Calophyllum inophyllum showed exceptionally toxic activity $(LC_{50}:$<$5\;ppm)$.