• Archives of Pharmacal Research
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• v.28 no.10
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• pp.1131-1134
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• 2005

Two new benzopyrans 6-[1'-oxo-3'(R)-hydroxy-butyl]-5,7 -dimethoxy-2,2-dimethyl-2H-1-ben-zopyran (1) and 6-[1'-oxo-3'(R)-methoxy-butyl]-5,7 -dimethoxy-2,2-dimethyl-2H-1-benzopyran (2) were isolated from the leaves of Mallotus apelta Muell.-Arg., (Euphorbiaceae). Their chemical structures were elucidated by spectroscopic analyses, especially by 1D-, 2D-NMR and MS spectra. Compound 1 was found to have strong cytotoxic effect against two human cancer cell lines as human hepatocellular carcinoma (Hep-2, $IC_{50}\;:\;0.49\;{\mu}g/mL$) and rhabdosarcoma (RD, $IC_{50}\;:\;0.54\;{\mu}g/mL$), while compound 2 showed moderate activity against Hep-2 cell line ($IC_{50}\;:\;4.22\;{\mu}g/mL$) by in vitro assay.

• YAKHAK HOEJI
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• v.42 no.6
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• pp.634-638
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• 1998

The effects of MeOH extracts from 88 herbal medicines on monoamine oxidase (MAO) acitivity were investigated. MAO was purified from mouse brain and its activity was determined by fluorospectrophotometer using kynuramine as a substrate. The $K_m\;and\;V_{max}$ values (n=4) of MAO were $78.2{\pm}4.0\;{\mu}M$ and $0.65{\pm}0.05$ nmol/min/mg protein, respectively. Four MeOH extracts from Melilotus sauvelolens, Eupatorium lindleyanum Bupleurum longiradiatum and Sorbaria sirbiforia showed a strong inhibitory effect with less than $100{\mu}g/ml$ in their $IC_{50}$ values on MAO activity. Six MeOH extracts including Agastache rugosa showed a mild inhibitory effect with 100~200${\mu}$g/ml in their $IC_{50}$ values. Twenty-two MeOH extracts including Melandryum seoulense exhibited a week inhibition of MAO activity with 200~300${\mu}$g/ml in their $IC_{50}$ values.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.30 no.6
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• pp.909-915
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• 1997

The nitrite scavenging effect of methanol extracts of marine algae were evaluated to discover new natural nitrite scavengers. Among the tested seaweeds, Ecklonia stolonifera, an edible brown algae, showed the strongest scavenging effect. The MeOH extract was then sequentially partitioned into $CH_2Cl_2,\;CH_2Cl_2$ insoluble interface, EtOAc, n-BuOH, and $H_2O$ layers. The EtOAc and n-BuOH fraction demonstrated high levels of nitrite-scavenging activity while the $CH_2Cl_2,\;CH_2Cl_2$ insoluble interface, and $H_2O$ fractions were inactive. A column chromatography of the EtOAc fraction through silica gel and Sephadex LH-20 yielded phloroglucinol and a new compound tentatively named phlorotannin A. The nitrite scavenging activity of phloroglucinol $(IC_{50}=3.9{\mu}g/ml)$ was more potent than that of L-ascorbic acid $(IC_{50}=65.0{\mu}g/ml)$. However, phlorotannin A $(IC_{50}=193.2{\mu}g/ml)$ showed only low levels of activity. From the above results, it is possible to suggest that both the MeOH extract and their fractions and isolated phloroglucinol and phlorotannin A obtained from E. stolonifera may be applicable as scavengers of nitrite, which is a precursor for the formation of carcinogenic N-nitroso compounds.

• Food Science and Preservation
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• v.15 no.4
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• pp.518-523
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• 2008

This study sought to prepare Doenjang with added Ulmi cortex, to improve functionality and flavor, while retaining the original Doenjang scent. Ulmi cortex powders were added during fermentation. The Ulmi cortex-containing Doenjang showed lower pH and less salinity than did the Doenjang prepared without Ulmi cortex. Sensory evaluation data showed that Doenjang with Ulmi cortex tasted sweeter, and less salty, and was preferred over Doenjang without Ulmi cortex. In the DPPH assay, Doenjang with Ulmi cortex showed much higher free-radical scavenging ability (IC50 of 29.16 g/mL)did Doenjang without Ulmi cortex(IC50 of 155.67 g/mL), indicating that Ulmi cortex Doenjang has higher antioxidant levels. Doenjang prepared with 1%(w/v) Ulmi cortex powder was best in terms of consumer preference and functionality.

• Preventive Nutrition and Food Science
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• v.20 no.3
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• pp.176-182
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• 2015

Abalone protein was hydrolyzed by enzymatic hydrolysis and the optimal enzyme/substrate (E/S) ratios were determined. Abalone protein hydrolysates (APH) produced by Protamex at E/S ratio of 1:100 showed angiotensin I converting enzyme inhibitory activity with $IC_{50}$ of 0.46 mg/mL, and APH obtained by Flavourzyme at E/S ratio of 1:100 possessed the oxygen radical absorbance capacity value of $457.6{\mu}M$ trolox equivalent/mg sample. Flavourzyme abalone protein hydrolysates (FAPH) also exhibited $H_2O_2$ scavenging activity with $IC_{50}$ of 0.48 mg/mL and $Fe^{2+}$+ chelating activity with $IC_{50}$ of 2.26 mg/mL as well as high reducing power. FAPH significantly (P<0.05) protected $H_2O_2$-induced hepatic cell damage in cultured hepatocytes, and the cell viability was restored to 90.27% in the presence of FAPH. FAPH exhibited 46.20% intracellular ROS scavenging activity and 57.89% lipid peroxidation inhibition activity in cultured hepatocytes. Overall, APH may be useful as an ingredient for functional foods.

• Bulletin of the Korean Chemical Society
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• v.34 no.5
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• pp.1349-1354
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• 2013

Twenty two new 5-fluorouracil (5-FU) derivatives, 2-butoxy-4-substituted 5-fluoropyrimidines, were synthesized and characterized by IR, $^1H$ NMR, MS, HRMS. All compounds were preliminarily evaluated by MTT assay on human liver BEL-7402 cancer cell line in vitro. Ten compounds were selected to test their cytotoxic activity against A549, HL-60 and MCF-7 cancer cell lines in vitro. These compounds were more sensitive to BEL-7402 than other cell lines, particularly, cytotoxic activity of compounds 6b, 6d-f, 6p, 6s-u were in sub-micromolar scale. The highest cytotoxic potency against A549, HL-60 and MCF-7 was shown by 2-butoxy-4-chloro-5-fluoropyrimidine (5) with $IC_{50}$ values of 0.10, 1.66 and $0.59{\mu}M$, respectively. Compounds 6d and 6e were effective against MCF-7 with $IC_{50}$ $9.73{\mu}M$ and HL-60 with $IC_{50}$ $8.83{\mu}M$, respectively.

• Archives of Pharmacal Research
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• v.25 no.2
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• pp.151-153
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• 2002

Three pseudoguaianolide type sesquiterpenes, bigelovin(1), 2,3-dihydroaromaticin (2), and ergolide (3) were isolated as inhibitory constituents against inducible nitric oxide synthase (iNOS) from the flowers of Inula britannica var. chinensis. Bigelovin (1) exhibited a highly potent inhibitory activity on lipopolysaccharide (LPS)-induced iNOS in murine macrophage RAW 264.7 cells with an $IC_{50}$ value of 0.46 mM, which is about 8 times more potent than the known selective inhibitor of iNOS, $L-N^6-(1-iminoethyl)Iysine{\;}(IC_{50}{\;}3.49{\;}{\mu}M)$. 2,3-Dihydroaromaticin (2) and ergolide (3) also exhibited potent inhibitory activities on LPS-induced iNOS with $IC_{50}$ values of 1.05 and $0.69{\;}{\mu}M$, respectively.

• Archives of Pharmacal Research
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• v.19 no.6
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• pp.456-461
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• 1996

Vascular relaxation action of crude extracts of two kinds of Coptidis rhizoma (Coptis chinensis and Coptis japonica, Ranunculaceae) was investigated and compared with that of berberine and palmatine, active alkaloid components of these plants. The results show that total extracts, berberine, and palmatine induced a concentration-dependent vasodilatation of rat thoracic aorta contracted with phenylephrine (PE). Palmatine, unlike to berberine, did not inhibit contraction induced by KCI. In calcium-free media, not only berberine but also crude extracts inhibited calcium-induced contraction. Furthermore, pretreatment of crude extracts inhibited contraction induced by PE noncompetitively. In PE-induced contraction, berberine was 2.5 times more potent than Coptis chinensis in the relaxation of rat aorta in terms of $IC_{50}$ values. Analysis of the effects of crude extracts on the Emax and $IC_{50}(PE)IC_{50}(KCI)$ ratios provides information on selectivity and indicates that extracts exhibit greater inhibition of the contrac tile response induced by PE than by KCI. We concluded that crude extracts have .alpha.-adrenoceptor blocking action and possesses inhibitory effect on calcium influx, which may be at least in part responsible for the antihypertensive action.

• Archives of Pharmacal Research
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• v.26 no.6
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• pp.463-465
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• 2003

Four protostane-type triterpenes, alisol B 23-acetate (1a), alisol C 23-acetate (2a), alisol B(3a), and alisol A 24-acetate (4a), were isolated from the rhizome of Alismatis plantago-aquatica L. var. orientale Samuelson (Alismataceae) and eleven protostane derivatives (compounds 1-11) were obtained by selective modification from alisol B 23-acetate (1a). These compounds were investigated for their anti-complement activity against the classical pathway of the complement system. Alisol B (3a) and alisol A 24-acetate (4a) exhibited anti-complement activity with $IC_{50} values of 150 and 130 \mu$ M. Among the synthetic derivatives, the tetrahydroxylated protostane triterpene (9) showed moderate inhibitory activity with $IC_{50} value of 97.1 \mu$ M. Introduction of an aldehyde group at C-23 (10; $IC_{50} value, 47.7 \mu$ M) showed the most potent inhibitory effect on the complement system in vitro.

• Natural Product Sciences
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• v.8 no.4
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• pp.133-136
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• 2002

GC-MS data on the volatile oil (CS-oil) of Chrysanthemum sibiricum herbs led to the identification of 2-methoxythioanisol, (+)-camphor, geraniol, citral, thymol, eugenol, ${\beta}-caryophyllene$ oxide, ${\beta}-caryophyllene$, ${\beta}-eudesmol$, juniper camphor together with an unknown substance using the mass spectral library and literature data. CS-oil exhibited significant cytotoxicities on HL-60 $(IC_{50}\;12.5\;{\mu}g/ml)$ cell and mild on HepG-2 cell $(IC_{50}\;102.4\;{\mu}g/ml)$, though the antioxidant ability was found not to be potent $(IC_{50}\;97.2\;{\mu}g/ml)$. However, the component eugenol showed potent antioxidant ability but mild cytotoxicity. Methyleugenol with no phenolic OH showed less potent cytotoxic and antioxidative properties than eugenol suggesting that phenolic OH plays an important role for the cytotoxic and antioxidant abilities. The oil-pretreatment prevented lipid peroxidation induced by bromobenzene in the rat. Therefore, it was demonstrated that CS-oil could be a cytotoxic agent with antioxidant properties.