• Molecules and Cells
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• v.38 no.8
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• pp.705-714
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• 2015

We investigated the role of HDAC3 in anti-cancer drug-resistance. The expression of HDAC3 was decreased in cancer cell lines resistant to anti-cancer drugs such as celastrol and taxol. HDAC3 conferred sensitivity to these anti-cancer drugs. HDAC3 activity was necessary for conferring sensitivity to these anti-cancer drugs. The down-regulation of HDAC3 increased the expression of MDR1 and conferred resistance to anti-cancer drugs. The expression of tubulin ${\beta}3$ was increased in drug-resistant cancer cell lines. ChIP assays showed the binding of HDAC3 to the promoter sequences of tubulin ${\beta}3$ and HDAC6. HDAC6 showed an interaction with tubulin ${\beta}3$. HDAC3 had a negative regulatory role in the expression of tubulin ${\beta}3$ and HDAC6. The down-regulation of HDAC6 decreased the expression of MDR1 and tubulin ${\beta}3$, but did not affect HDAC3 expression. The down-regulation of HDAC6 conferred sensitivity to taxol. The down-regulation of tubulin ${\beta}3$ did not affect the expression of HDAC6 or MDR1. The down-regulation of tubulin ${\beta}3$ conferred sensitivity to anti-cancer drugs. Our results showed that tubulin ${\beta}3$ serves as a downstream target of HDAC3 and mediates resistance to microtubule-targeting drugs. Thus, the HDAC3-HDAC6-Tubulin ${\beta}$ axis can be employed for the development of anti-cancer drugs.

• Natural Product Sciences
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• v.4 no.3
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• pp.143-147
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• 1998

Examination of the chemical constituents of the dried leaves of Isodon eriocalyx (Dunn.) Hara led to the isolation of four new diterpenoids, named maoecrystal Q-T (1-4). Their structures were elucidated as $16(R)-methoxymethyl-6{\beta},\;7{\beta}-dihydroxy-7{\alpha},20-epoxy-ent-kaur-2,3-ethenylene-1$, 15-dione(1), $1{\beta},18-diacetoxy-6{\beta},7{\beta}-dihydroxy-7{\alpha},20-epoxy-ent-kaur-16-en-15-one\;(2),\;6{\beta},\;7{\beta}-dihydroxy-15{\beta}-acetoxy-7{\alpha},20-epoxy-ent-kaur-16-en-1-one$ (3) and $7{\beta}-hydroxy-6{\beta},15{\beta}-diacetoxy-1{\alpha},11{\beta}-acetonide-7{\alpha},20-epoxy-ent-kaur-16-ene$ (4), respectively, on the basis of spectroscopic methods. Meanwhile, five known diterpeonids eriocalyxin B (5), maoecrystal B-D (6-8) and trichokaurin (9) were also obtained.

• Archives of Pharmacal Research
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• v.22 no.4
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• pp.428-431
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• 1999

Seven known oleanolic acid glycosides (1-7) were isolated form the MeOH extract of Tiarella polyphylla. The structures were identified to be 3-O-($\beta$-glucopyranosyl) oleanolic acid (1), 3-O-[$\beta$-D-glucopyranosyl-(1 3)-$\beta$-D-glucopyranosyl] oleanolic acid (2), 3-O-D-[$\beta$-D-glucopyranosyl-(1 2)-$\beta$-D-glycopyranosyl] oleanolic acid (3), 3-O-[$\beta$-D-glucopyranosyl-(1 3)-$\beta$-D-glucopyranosyl] oleanolic acid 28-O-$\beta$D-glucopyranosyl ester (4), 3-O-[$\beta$-D-glucopyranosyl-(1 2)-$\beta$-D-glucopyranosyl] oleanolic acid 28-O-$\beta$-D-glucopyranosyl ester (5), 3-O-[a-L-rahmnopyranosyl-(1 3)-$\beta$-D-glucururonopyranosyl] oleanolic acid (6), and 3-O-[$\alpha$-L-rhamnopyranosyl-(1 3)-$\alpha$-D-glucuronopyranosyl] oleanolic acid 28-O-$\alpha$-D-glucopyranosyl ester (7) on the basis of physicochemical and spectral data. These triterpene glycosides were tested for the anti-complement activity and hemolytic activity. Bisdesmosidic saponins, 4, 5, and 7, showed anti-complement activity; in contrast, monodesmosidic saponins, 1-3, and 6, showed direct hemolytic activity. Methyl esterified monodesmosidic saponins showed anti-complement activity at a low concentration and hemolytic activity at a high concentration.

• Korean Journal of Pharmacognosy
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• v.27 no.4
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• pp.389-396
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• 1996

Spiraea prunifolia var. simpliciflora (Rosaceae) is a deciduous. latifoliate shrub growing in most parts of Korea. The roots of this plant have been used for malaria, as antipyretics and emetics. From the roots of this plant, sterol glycoside and two triterpenoids were isolated and the structures were elucidated by chemical and spectroscopic methods. They were identified as $3{\beta}-hydroxyurs-12-ene-28-oic$ acid (ursolic acid.1), $2{\alpha}$, $3{\beta}$, $19{\alpha}-trihy-droxyurs-12-ene-28-oic$ acid (tormentic acid.2) and ${\beta}-sitoste-rol-3-O-{\beta}-D-glucopyranoside$ (3).

• Journal of Life Science
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• v.17 no.9 s.89
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• pp.1298-1302
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• 2007

A hallmark of cancers is 'leaky' tight junctions (Tjs). TJs mediated paracellular permeability is elevated and TJs maintained cell polarity is frequently lost. Concomitantly, TJs-associated proteins including members of the claudin family of proteins are dysregulated. Recent findings indicate that these TJs changes can contribute to cancer progression. In this study, we examined the effects of ${\beta}-lapachone$, a quinone compound obtained from the bark of the lapacho tree (Tabebuia avellanedae), on the Tjs-associated regulators in human hepatocarcinoma cell lines, HepG2 and Hep3B. ${\beta}-lapachone$ treatment downregulated the levels of insulin-like growth factor 1 receptor (IGF-lR) proteins in both HepG2 and Hep3B cells. But the levels of claudin-3 and -4 proteins were increased in ${\beta}-lapachone$-treated HepG2 and Hep3B cells. And also the zonnula occludens-l (la-I) and p-catenin protein levels by ${\beta}-lapachone$ were increased in a time-dependent manner. However, claudin-3 and -4 mRNA levels were uninhibited by ${\beta}-lapachone$ in HepG2 and Hep3B. The present results suggest that the upregulation of claudin-3 and -4 protein levels by ${\beta}-lapachone$ occurs by a post-transcriptional mechanism and points to a novel mechanism by ${\beta}-lapachone$.

• Korean Journal of Pharmacognosy
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• v.23 no.1
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• pp.14-19
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• 1992

A mixture of acylglucosyl sterols together with ${\beta}-sitosterol$, ${\beta}-sitosterol\;3{\beta}-O-glucoside$ and fatty acids was isolated from the roots of Caragana chamlagu as their acetate forms and the structure elucidated by chemical and spectroscopic means. The major acylglucosyl sterol was ${\beta}-sitosteryl\;3-O-[6'-O-oleoyl]-{\beta}-D-glucopyranoside$ while the minor components were $6'-O-palmitoyl-\;and\;6'-O-stearoyl-{\beta}-D-glucosyl$ sitosterol congeners. The isolation and structure elucidation of these acylglucosyl sterols are reported for the first time from the genus Caragana.

• Archives of Pharmacal Research
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• v.27 no.1
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• pp.57-60
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• 2004

Glycyrrhizin (18$\beta$-glycyrrhetinic acid-3-O-$\beta$-D-glucuronopyranosyl-(1$\rightarrow2)-\beta$-D-glucuronide, GL) was transformed to 18$\beta$-glycyrrhetinic acid-3-O-$\beta$-D-glucuronide (GAMG) by Streptococcus LJ-22. The antiallergic activities of GL and GAMG was measured using a RBL cell assay system and contact hypersensitivity model mice. GAMG exhibited anti-allergic activity with $IC_{50}$ values of 0.28 mM. GAMG, which is sweeter than GL, and 18$\beta$-glycyrrhetinic acid, which is a GAMG metabolite by human intestinal bacteria, also inhibited the passive cutaneous anaphylaxis and skin contact inflammation. In conclusion, GAMG may be useful as a new sweet food additive and an anti-allergic agent.

• Bulletin of the Korean Chemical Society
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• v.1 no.2
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• pp.45-49
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• 1980

During the homolytic reactions of $CCl_4$ or $Cl_3CBr with ${\beta}-halo^1$-styrenes,$\beta$-haloradicals are key intermediates. They are to be stabilized via three pathways; $\beta$-cleavage, halogen transfer and telomerization. The three reaction paths are delicately controlled by the energetics of their formation and stabilization. When the formation of a $\beta$-haloradical is accompanied by considerable excess of energy from an exothermic reaction, $\beta$ -cleavage is often dominant over the halogen transfer. On the other hand, if the radical forms via a reversible reaction, two processes become competitive. $\beta$-Eliminated bromine atoms from ${\beta}$ -bromoradicals generate $Br_2$ via $Cl_3CBr + {\cdot}Br {\leftrightarrow} Br_2 + {CCl_3}{\cdot}{Br_2}$ may act as a better scavenger than Cl3CBr for the ${\beta}$-bromoradicals. Different reactivities of chlorine, bromine and trichloromethyl radicals towards olefinic pi-bond are clarified in terms of the beat content of the addition reactions.

• Journal of Aquaculture
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• v.19 no.4
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• pp.247-253
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• 2006

This study was conducted to investigate the effects of dietary supplementation of ${\beta}-1,3$ glucan on growth and immune responses in juvenile olive flounder, Paralichthys olivaceus fed the white fish meal based diets for 6 weeks. Five experimental diets supplemented with ${\beta}-1,3$ glucan at 0, 0.01, 0.025, 0.05, 0.1 % (Control, $G_{0.01},\;G_{0.025},\;G_{0.05}\;and\;G_{0.1}$, respectively) of diet on a dry-matter basis. Five experimental diets were formulated to be isonitrogenous and isocaloric to contain 50.0% crude protein and 16.7 kJ available energy $g^{-1}$. Fish averaging $3.2{\pm}0.1\;g\;(mean{\pm}SD)$ were randomly distributed in each aquarium as triplicate groups of 15 fish. Weight gain (WG, %), specific growth rate (SGR, %), and feed efficiency (FE, %) of fish fed $G_{0.1}$ diet were found significantly higher than those of fish fed Control, $G_{0.01},\;G_{0.025}\;and\;G_{0.05}$ diets (P<0.05). However, there was no significant difference among the fish fed control, $G_{0.01},\;G_{0.025}$. Chemiluminescent responses (CL) of fish fed $G_{0.1}$ diet were significantly higher than those of fish fed the other diets. Serum lysozyme activities of fish fed $G_{0.05}$ and $G_{0.1}$ diets were higher than those of fish fed control, $G_{0.025}$ and $G_{0.05}$ diets. Fish fed $G_{0.1}$ diet showed a significantly lower cumulative mortality than did fish fed control diet throughout the challenge test (P<0.05). These results suggested that based on growth rate, feed efficiency, non-specific immunity and protection against microbial infections the optimum dietary ${\beta}-1,3$ gulcan could be greater than 0.05% but less than 1.0% in juvenile olive flounder, Paralichthys oilvaceus.

• Molecules and Cells
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• v.27 no.3
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• pp.299-305
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• 2009

Over-expression of phospholipase D (PLD) 1 or PLD2 down-regulated CKII activity in NIH3T3 cells. The same results were found with catalytically inactive mutants of PLD isozymes, indicating that the catalytic activity of PLD is not required for PLD-mediated CKII inhibition. Consistent with this, 1-butanol did not alter CKII activity. The reduction in CKII activity in PLD-over-expressing NIH3T3 cells was due to reduced protein level, but not mRNA level, of the $CKII{\beta}$ subunit. This PLD-induced $CKII{\beta}$ degradation was mediated by ubiquitin-proteasome machinery, but MAP kinase and mTOR were not involved in $CKII{\beta}$ degradation. PLD isozymes interacted with the $CKII{\beta}$ subunit. Immunocytochemical staining revealed that PLD and $CKII{\beta}$ colocalize in the cytoplasm of NIH3T3 cells, especially in the perinuclear region. PLD binding to $CKII{\beta}$ inhibited $CKII{\beta}$ autophosphorylation, which is known to be important for $CKII{\beta}$ stability. In summary, the current data indicate that PLD isozymes can down-regulate CKII activity through the acceleration of $CKII{\beta}$ degradation by ubiquitin-proteasome machinery.