• Korean Journal of Pharmacognosy
• /
• v.43 no.1
• /
• pp.6-9
• /
• 2012

The $CH_2Cl_2$ soluble part of the leaves of Helianthus tuberosus L. (Compositae) exhibited a potent cytotoxic activity against the cultured human tumor cell lines including A-549, SK-OV-3, SK-MEL-2, XF498 and HCT-15 in vitro. Bioassaydirected fractionation of the $CH_2Cl_2$ soluble part of this plant led to the isolation of four cytotoxic sesquiterpene lactones having ${\alpha}$-methylene-${\gamma}$-lactone ring in the molecule. On the basis of physical and spectral evidences, their structures were characterized as ${\Delta}^{4,15}$-isoatripliciolide tiglate (1), ${\Delta}^{4,15}$-isoatripliciolide methacrylate (2), budlein A isobutylate (3) and budlein A tiglate (4). The ${\Delta}^{4,15}$-isoatripliciolide tiglate (1) showed the most potent cytotoxic activity ($0.26{\mu}M<ED_{50}<2.16{\mu}M$) against all of the cell lines tested.

• Archives of Pharmacal Research
• /
• v.26 no.11
• /
• pp.925-928
• /
• 2003

Four guaia-12,6-olide type sesquiterpene lactones, aguerin B (1), 8$\alpha$-acetoxyzaluzanin C (2), cynaropicrin (3), and deacylcynaropicrin (4), were isolated from the flowers of Hemisteptia Iyrata Bunge. It is the first report on the isolation of compounds 1-4 from Hemisteptia species. All the isolates (1-4) were examined for their cytotoxic activity against SK-OV-3, LOX-IMVI, A549, MCF-7, PC-3, and HCT-15 human cancer cell lines.

• Proceedings of the Korean Society of Life Science Conference
• /
• 2001.02a
• /
• pp.69-69
• /
• 2001

• Applied Biological Chemistry
• /
• v.46 no.3
• /
• pp.235-239
• /
• 2003

Thirteen sesquiterpene lactones isolated from the flower of Chrysanthemum coronarium L., which has been widely cultivated in Korea as a vegetable for a long time, were investigated their antimicrobial activities against eight bacteria and five phytopathogenic fungi. The antimicrobial activities of dihydrochrysanolide (6) and 1-epi-dihydrochrysanolide (7) showed strong activities against all the bacteria such as Bacillus subtilis, Bacillus cereus, Staphylococcus aureus and Vibrio parahaemolyticus. Especially, Staphylococcus aureus was investigated that have very strong antibacterial activity to $1.56\;{\mu}g{\cdot}disc^{-1}$, respectively. Also, most of sesquiterpene lactones, which have ${\alpha}-methylene-{\gamma}-butyrolactone$ group, were exhibited strong activity to Gram(+) bacteria than Gram(-) bacteria. In the antifungal test, Rhizoctonia solani and Phytophthora capsici known as phytopathogenic fungi have exhibited all extensive activity about compounds that have ${\alpha}-methylene-{\gamma}-butyrolactone$ group.

• Korean Journal of Pharmacognosy
• /
• v.29 no.3
• /
• pp.243-247
• /
• 1998

A diverse panel of human tumor cell lines and a mouse melanoma cell line (B16-F1) were used for the cytotoxicity test of the nine sesquiterpene lactones with ${\beta}-methylene-{\gamma}-lactone$ group isolated from Hemisteptia lyrata, Chrysanthemum zawadskii and Chrysanthemum boreale. In the cell adhesion inhibitory activity test against B16-F1 mouse melanoma cell, hemistepcin B, cumambrin B, costunolide and tulipinolide were shown significant activities with $IC_{50}$ range of 2.2, 4.1, 0.9 and $0.3\;{\mu}g/ml$, respectively. In the cytotoxicity test against human tumor cells, the most active compound was costunolide having $IC_{50}$ values of below $0.3\;{\mu}g/ml$ against all the tested cell lines except for UACC62. Cumambrin A, hendelin and costunolide exhibited more strong activity against HCT15 and UO-31 cell lines than a positive control, adriamycin. All tested compounds showed an $IC_{50}$ values of below $5.0\;{\mu}g/ml$ against all the tested cell lines.

• Journal of fish pathology
• /
• v.37 no.1
• /
• pp.133-138
• /
• 2024

This study is a report on combinational effects between four sesquiterpene lactones (SLs) from bay laurel (Laurus nobilis) leaves, and oxytetracycline (OTC) or amoxicillin (AMX) against four fish pathogenic bacteria such as Vibrio anguillarum, V. harveyi, Edwardsiella tarda, and Streptococcus iniae. Individually, four SLs exerted little antibacterial activity against fish pathogenic bacteria. However, when combined with OTC or AMX, they showed synergistic interaction against pathogenic bacteria. Especailly, zaluzanin C (1) reduced the MIC of OTC (or AMX) eight-fold. Our results showed that combinations of SLs with antibiotics (ABTs) are more effective than ABTs alone to control pathogenic bacteria. The highest synergistic effect was observed when zaluzanin C (1) was combined with OTC or AMX against V. harvey or S. iniae, displaying significant reductions of MICs up to 8-fold (0.125 to 0.015 ㎍/mL and 0.0078 to 0.0009 ㎍/mL). In addition, zaluzanin C (1) improved the antibiotic potency of OTC against OTC resistant V. harveyi (250 ㎍/mL to 62.5 ㎍/mL). Synergism between ABTs and phytochemical such as SLs could be a therapeutically helpful concept to improve the efficacy of ABTs and prevent antibiotic resistance. These results suggest that SLs can be used as an alternative to reduce antibiotic resistance in aquaculture.

• Proceedings of the PSK Conference
• /
• 2001.10a
• /
• pp.141.2-141.2
• /
• 2001

• YAKHAK HOEJI
• /
• v.51 no.2
• /
• pp.145-149
• /
• 2007

Saussurea Radix, the dried roots of Saussurea lappa Clark (Compositae), has been used in oriental traditional medicine for aromatic stomachic. Present study was carried out for the anticancer effect of Saussurea Radix. Bioassay-directed fractionation of Saussurea Radix led to the isolation of two sesquiterpenes, dehydrocostuslactone (1) and costunolide (2). The structures of 1 and 2 were elucidated by spectral methods (MS, IR, $^1$H and $^{13}$C NMR). These compounds showed a potent cell proliferation activity against human breast cancer cell MCF-7 and MDA-MB-453.

• KSBB Journal
• /
• v.28 no.2
• /
• pp.74-79
• /
• 2013

There are a large number of bioactive sesquiterpene lactones from compositae plants including Hemistepita lyrata Bunge. In the present study, we purified two sesquiterpene lactones, Hemistepsin A and B, from H. lyrata and evaluated their antimicrobial activities against Malassezia obutusa. Chromatographic separation was used for the preparation of Hemistepsin A and B, and the identity of these compounds was confirmed by NMR. Strong inhibition of growth of M. obutusa was obtained with all doses of Hemistepsin A tested. Moreover, antifungal activity of Hemistepsin A occurred in a dose-dependent manner. Hemistepsin B also showed potent antifungal activity at the dose of $800{\mu}m/disc$. From these results, it was suggested that Hemistepsin A and B be beneficial for the preparation of the useful agent for treating scalp diseases occurred by dandruff-causing Malassezia species.

• Natural Product Sciences
• /
• v.25 no.1
• /
• pp.16-22
• /
• 2019

Inula helenium L. is rich source of eudesmane-type sesquiterpene lactones, mainly alantolactone and isoalantolactone, which have the various pharmacological functions. In this study, we examined the inhibitory effects of nitric oxide (NO) production of hexane, methylene chloride, ethyl acetate, butanol, and water fractions from I. helenium and investigated the anti-inflammatory effect of hexane fraction of I. helenium (HFIH) in LPS-induced RAW 264.7 cells. Quantification of alantolactone and isoalantolactone from HFIH was carried out for the standardization by multiple reaction monitoring using triple quadrupole mass spectrometer. HFIH significantly inhibited inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) protein as well as their downstream products NO and prostaglandin $E_2$ ($PGE_2$) in LPS-stimulated RAW 264.7 cells. Moreover, HFIH suppressed $NF-{\kappa}B$ transcriptional activity by decreasing the translocation of p65 to the nucleus. The in vivo study further confirmed that HFIH attenuated the paw edema induced by carrageenan in an acute inflammation model. These findings suggest that HFIH may be useful as a promising phytomedicine for inflammatory-associated diseases.