• Biomolecules & Therapeutics
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• 제21권5호
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• pp.332-337
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• 2013

Microglial activation plays an important role in the development and progression of various neurological disorders such as cerebral ischemia, multiple sclerosis, and Alzheimer's disease. Thus, controlling microglial activation can serve as a promising therapeutic strategy for such brain diseases. In the present study, we showed that kalopanaxsaponin A, a triterpenoid saponin isolated from Kalopanax pictus, inhibited inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and tumor necrosis factor (TNF)-${\alpha}$ expression in lipopolysaccharide (LPS)-stimulated microglia, while kalopanaxsaponin A increased anti-inflammatory cytokine interleukin (IL)-10 expression. Subsequent mechanistic studies revealed that kalopanaxsaponin A inhibited LPS-induced DNA binding activities of NF-${\kappa}B$ and AP-1, and the phosphorylation of JNK without affecting other MAP kinases. Furthermore, kalopanaxsaponin A inhibited the intracellular ROS production with upregulation of anti-inflammatory hemeoxygenase-1 (HO-1) expression. Based on the previous reports that JNK pathway is largely involved in iNOS and proinflammatory cytokine gene expression via modulating NF-${\kappa}B$/AP-1 and ROS, our data collectively suggest that inhibition of JNK pathway plays a key role in anti-inflammatory effects of kalopanaxsaponin A in LPS-stimulated microglia.

• Archives of Pharmacal Research
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• 제21권1호
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• pp.24-29
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• 1998

To search for the anti-diabetic principle from the stem bark of Kalopanax pictus, seven kinds of chemical constituents including hederagenin glycosides and phenolic glycosides wre isolated. The anti-diabetic evaluation of these isoltes in the streptozotocin-induced diabetic rats exhibited that kalopanaxsaponin A has a potent anti-diabetic activity in contrast to a mild activity of hederagenin. In addition, significant hypocholesterolemic and hypolipidemic activities of kalopanaxsaponin A and hederagenin were observed. The structure-activity relationship of kalopanaxsaponin A was also investigated in the present work.

• Biomolecules & Therapeutics
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• 제20권5호
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• pp.457-462
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• 2012

The stem-bark of Kalopanax pictus (KP, family Araliaceae), of which main constituent is kalopanaxsaponin B, has been used for asthma, rhinitis, and arthritis in Chinese traditional medicine. To clarify anticolitic effect of KP, we examined anti-inflammatory effect of KP extract and kalopanaxsaponin B in lipopolysaccharide (LPS)-stimulated peritoneal macrophage and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitic mice. Of KP extracts, KP BuOH-soluble fraction most potently inhibited LPS-induced IL-$1{\beta}$, IL-6 and TNF-${\alpha}$ expression, as well as NF-${\kappa}B$ activation. However, KP BuOH fraction increased IL-10, an anti-inflammatory cytokine. KP BuOH fraction also inhibited colon shortening and myeloperoxidase activity in TNBS-induced colitic mice. KP BuOH fraction also potently inhibited the expression of the pro-inflammatory cytokines, IL-$1{\beta}$, IL-6, and TNF-${\alpha}$ as well as the activation of NF-${\kappa}B$. Kalopanaxsaponin B, a main constituent of KP, inhibited TNBS-induced colonic inflammation, including colon shortening, and TNBS-increased myeloperoxidase activity pro-inflammatory cytokine expression and NF-${\kappa}B$ activation in mice. Based on these findings, KP, particularly its main constituent, kalopanaxsaponin B, may ameliorate colitis by inhibiting NF-${\kappa}B$ pathway.

• 생약학회지
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• 제37권3호
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• pp.184-189
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• 2006

To find the monthly variation of kalopanaxsaponin contents in the leaves of Kalopanax pictus with thorns (KPT) and with no thorns (KPN), the leaves monthly collected from May to September were extracted with MeOH and then the kalopanaksaponin fractions were prepared. KPT collected on May showed the lowest saponin content of the KPTs whereas KPT on August exhibited the highest saponin content. From September, the saponin content in the loaves decreased. The highest saponin content was shown to be 7.3% in KPN collected on August. Evaluation of six kalopanaxsaponins A, I, J, B, H and K (KPA, KPI, KPJ, KPB, KPH, and KPK) were performed using TLC densitometer. In this measurement, considerably higher KPB and KPH, both hederagenin bisdesmosides, were found whereas very low contents In monodesrnosides KPI and KPJ were observed. In conclusion, it was shown that the leaves of KPN of August could be a biomaterial source for the kalopanaxsaponin fraction. It was also suggested that measurement of the weight of kalopanaxsaponin fraction and the content of KPB as the representative compound for kalopanaxsaponins will be used for the quantitative evaluation of the kalopanaxsaponins of K. pictus.

• Natural Product Sciences
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• 제8권2호
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• pp.35-43
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• 2002

Glycosides of herbal medicines, such as glycyrrhizin, ginsenosides, kalopanaxsaponins, rutin and ponicirin, were studied regarding their metabolic fates and pharmacological actions in relation to intestinal bacteria using germ-free, gnotobiotic and conventional animals. When glycyrrhizin (GL) was orally administered, $18{\beta}-glycyrrhetinic\;acid\;(GA)$, not GL, was detected in plasma and intestinal contents of gnotobiotic and conventional rats. However, GA could not be detected in germ-free rats. When GL was incubated with human intestinal bacteria, it was directly metabolized to GA (>95%) or via $18{\beta}-glycyrrhetinic\;acid-3-{\beta}-D-glucuronide$(>5%). Orally administered GL was effective in gnotobiotic and conventional rats for liver injury induced by carbon tetrachloride, but was not effective in germ-free rats. When ginseng saponins were orally administered to human beings, compound K in the plasma was detected, but the other protopanxadiol saponins were not detected. The compound K was active for tumor metastasis and allergy. When kalopanaxsaponins were incubated with human intestinal microflora, they were metabolized to kalopanaxsaponin A, kalopanaxsaponin I and hederagenin. These metabolites were active for rheumatoid arthritis and diabetic mellitus while the other kalopanxsaponins were not. When flavonoid glycosides were orally administered to animals, aglycones and/or phenolic acids were detected in the urine. The metabolic pathways proceeded by intestinal bacteria rather than by liver or blood enzymes. These metabolites, aglycones and phenolic acids, showed antitumor, antiinflammatory and antiplatelet aggregation activities. These findings suggest that glycosides of herbal medicines are prodrugs.

• Archives of Pharmacal Research
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• 제24권2호
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• pp.119-125
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• 2001

We have reported that kalopanaxsaponin A (KPS-A) Isolated from Kalopanax pictus have anti-rheumatoidal activity in the rat treated with Freunds complete adjuvant (FCA) reagent. In addition, it has been also reported that KPS-A is a potent antioxidant in the rheumatoidal rat. This research was undertaken to examine whether the saponins of KPS-A and -1 could adjust the abnormal lipid metabolisms and hematological changes in immunological diseases. KPS-A significantly inhibited the increases in both triglycerides and total proteins in addition to the decrease in total cholesterol induced by FCA reagent treatment. KPS-A treatment decreased the number of leucocytes elevated by FCA reagent treatment. Excess dose of the methanol extract produced no severe toxicity on the body weight, wet organ weights and hepatic functions. Since $LD_50$ value of K. pictus methanol extract was shown to be 4,033 ${mg/kg}$, it could be estimated to be a safe agent for anti-rheumatoidal herbal medicines.

• 한국약용작물학회:학술대회논문집
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• 한국약용작물학회 2008년도 추계학술발표회
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• pp.289-290
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• 2008

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.265.1-265.1
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• 2002

In the previous study. we isolated kalopanaxsaponin A and pictoside A from the EtOAc fraction of Kalopanax pictus extract. In the present study, the BuOH fraction of K pictus extract was hydrolyzed by alkali and antirheumatic effect of the fraction was evaluated. It was found that the hydrolysate of the BuOH fraction showed inhibition of adjuvant-induced arthritis in rats. Of the EtOAc and BuOH fractions of the hydrolysate, only the former exhibited anti-arthritic activity. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.210.3-211
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• 2001

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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• pp.97.1-97.1
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• 2000