• Korean Journal of Pharmacognosy
• /
• v.43 no.3
• /
• pp.224-230
• /
• 2012

Schizandrin (SZ), was isolated from the fruit of Schizandra chinensis, has been reported to have many biological properties, including anti-inflammatory and antitumor activities. However, its anti-allergic effects are not completely elucidated. We focused on the anti-allergic effects of SZ in PMA/ionomycin (PI)-induced rat basophilic leukemia (RBL-2H3) cells and P815 mast cells. Cytokines (IL-4, IL-13), synthesized by basophils and mast cells, are implicated in pathological conditions such as asthma and allergy. The production of IL-4 and IL-13 was quantified by ELISA and the mRNA expression was detected by using RT-PCR assay. In this study, we found that SZ did not show cytotoxic effect at up to 100 ${\mu}M$ on RBL-2H3 cells and mast cells. In addition, SZ inhibited the production of IL-4 and IL-13 and also decreased the level of mRNA in PI-induced RBL-2H3 cells and mast cells in a dose-dependent manner. Thus, we suggest that SZ may have the effect on preventing allergic disorders by inhibiting IL-4 and IL-13 cytokines.

• Korean Journal of Pharmacognosy
• /
• v.49 no.3
• /
• pp.262-269
• /
• 2018

Sparassis crispa (Wulf.) is an edible/medicinal mushroom and has been reported to biological activities such as antitumor, anti-angiogenesis, antioxidant and wound healing. However, there have not been many researches on osteoarthritis of S. crispa. The aim of this study was to investigate the effects of S. crispa extract on rats with osteoarthritis induced by MIA. Osteoarthritis is a gradually developmental disease that early stage, causes joint stiffness and complains of joint pain. In addition, it gives rise to edema and hypo-function. The results of this study, S. crispa extract effectively inhibited ROS production, increased the production of antioxidant protein SOD and catalase in knee joint cartilage tissue. In addition, S. crispa extract inhibited the expression of pro-inflammatory cytokines and enzymes such as NOX4 and $P47^{phox}$, which are involved in the expression of COX-2, iNOS and the production of ROS. Also, S. crispa extract inhibited the destruction of synovial tissue, cartilage tissue and proteoglycans in articular cartilage in rats.

• Natural Product Sciences
• /
• v.8 no.2
• /
• pp.35-43
• /
• 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.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1995.04a
• /
• pp.85-85
• /
• 1995

전년도에 ara-C 유도체 중에서 ara-CDP-DL-PTBA가 각종 암세포주에 대한 뛰어난 항암작용이 보고된바 있으며, 이후 시료의 대량확보, Bulk Formulation 및 전임상등의 세가지 분야에 관해 연구를 수행하였다. Ara-CDP-DL-PTBA를 수용액에 현탁, 초음파분쇄후 NICOMP Analysis에 의하여 micellar solution의 입자도를 알아 본 결과 fresh prepared micelles은 11,1mm size가 88.63%이며 50,5mm가 11.37%로 나타나 평균 19,0mm가 되고, Reconstructed micells은 10.9mm size가 99.87%이며 356.1mm가 0.13%로 나타나 평균 11.0mm가 된다. Ara-C와 Ara-CDP-DL-PTBA의 대사작용을 알아본 결과, ara-C는 투여 1시간째 2,850 $\pm$ 450 pmol, 4시간째 450$\pm$190 pmol, 24시간째 30 pmol 이하로 ara-CTP의 혈중 농도가 급격히 감소하는 반면에 ara-CDP-DL-PTBA는 1시간째 650$\pm$120 pmol, 2시간째 1,800$\pm$500 pmol, 24시간째 300$\pm$90 pmol으로 ara-CTP의 혈중 농도가 서서히 감소하였다.

• YAKHAK HOEJI
• /
• v.60 no.3
• /
• pp.135-140
• /
• 2016

Heat shock protein 90 (Hsp90) is a ubiquitous molecular chaperone, which is associated with stabilization of many oncogenic proteins for cancer cell survival. Hsp90 is overexpressed 2-10 fold higher in cancer cells than normal cells. Due to its potential to simultaneously disable multiple signaling pathway, Hsp90 has been identified as a validated target for cancer therapy. Accordingly, we designed and synthesized 2',4'-dimethoxychalcone derivatives to inhibit Hsp90 chaperone function. Among 2',4'-dimethoxychalcone derivatives, we found that compound 1g disrupted Hsp90 chaperoning function and impaired the growth of cancer cells. These findings indicated that 1g could serve a potential lead compound to target Hsp90 in cancer chemotherapy.

• Journal of Microbiology and Biotechnology
• /
• v.19 no.6
• /
• pp.566-572
• /
• 2009

Lentinus edodes is a well-known edible and medicinal mushroom used in Oriental cultures. Recently, L. edodes has attracted a lot of attention owing to its antifungal activity, antibacterial activity, antiviral activity, hepatoprotective effect, antitumor activities, and immunomodulatory and cytotoxic effects. In this study, the water-soluble crude polysaccharides, CPF and CPB, which were obtained from the fruiting body and culture cell-free broth of L. edodes by hot-water extraction and ethanol precipitation, were fractionated by DEAE cellulose and Sepharose CL-6B column chromatography, resulting in six polysaccharide fractions, CPFN-G-I, CPFN-G-II, CPFN-G-III, CPFA-G, CPBN-G, and CPBA-G Among these fractions, CPFN-G-I, CPBN-G, and CPBA-G were shown to stimulate the functional activation of macrophages including NO production, cytokine expression, and phagocytosis.

• Journal of Ginseng Research
• /
• v.21 no.1
• /
• pp.1-12
• /
• 1997

Ginseng, the root of Panax ginseng C.A. Meyer, is well-known oriental herbal medicine. The number of paper reporting the effects on its physiological, pharmacological, and behavioral effects has been increased every year, since ginsenosides isolated from ginseng are known to be biologically active components. This brief review summarizes some of new findings from recently published papers on ginsenosides or ginseng saponins. Therefore, this paper includes the various effects of ginsenosides on neuronal cell growths, on behavior of experimental animals, on enzyme activities, on the release and uptake of neurotransmitters, on neuronal cell excitability, on the motility of intestine, on antitumor activity, on cardiovascular system and metabolism. In spite of various effects of ginsenosides on various cells or organs, it is still to date impossible for one to clearly explain the exact mechanism on the action of ginsenosides. However, in this article I will discuss several papers providing possible explanations on the physiological and pharmacological actions including signal transudation pathway of ginsenosides. The elucidation of the exact mechanism of ginsenosides on cellular or molecular level will not only give us a chance to explain why people have used ginseng as an elixir of life for several thousands of year but also give us a crucial chance to apply ginseng to modern medicine.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.19 no.2
• /
• pp.501-507
• /
• 2005

Shikonin is a chemically characterized component of traditional herbal medicine, the root of Lithospermum erythrorhizon and has been shown to possess antitumor activities. Here we investigated anticancer potential of shikonin and its possible mechanism of action in LLC cells. Shikonin inhibited the proliferation of LLC cells in a concentration-dependent manner. It was also demonstrated that shikonin induced apoptosis in LLC cells by Annexin V staining and TUNEL staining analysis. Shikonin treatment was caused that decrease of Bcl-2, activation of caspases and cleavage of PARP. And shikonin also induced that the activation of mitogen-activated protein kinases (MAPKs), such as extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and p38. Interestingly, the cell proliferation inhibition induced by shikonin was recovered by specific inhibitors of JNK and p38 but the inhibitor of MEK, the upstream kinase of ERK, did not recover. Additionally, shikonin administration at doses of 5 mg/kg in C57BL/6 mice strongly inhibited the primary tumor growth of LLC. Taken together, these results suggest that shikonin may suppress LLC cell proliferation by inducing an apoptotic process via activation of caspases and MAPKs

• Biomolecules & Therapeutics
• /
• v.8 no.3
• /
• pp.228-234
• /
• 2000

We have synthesized a novel platinum(II) coordination complex containing trans-ι-1,2-diaminocy-clohexane (DACH) as a carrier ligand and 1,2-dichloroethane (DCE) as a leaving group. A new series of [Pt(trans-ι-DACH)(DCE)](PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocar-cinoma cells and normal primary cultured kidney cells. The new platinum complex has demonstrated high efficacy in the cytotoxicity against MKN-45/P, MKN-45/ADM and MKN-45/CDDP cell-lines. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues, determined by MTT assay, the [$^3H$]-thymidine uptake arid glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum(II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new, clinically available anticancer chemotherapeutic agents.

• Natural Product Sciences
• /
• v.8 no.4
• /
• pp.170-172
• /
• 2002

In continuous efforts for discovery of novel potent antitumor agents from natural products, fifty-seven methanolic extracts derived from indigenous Korean plants were primarily evaluated for in vitro cytotoxic activity in cultured human lung (A549) and colon (Col2) cancer cells. As a result, 16 plant extracts were found to be active against A549 cells and 15 extracts were active against Col2 cells in the criteria of $IC_{50}$<$50\;{\mu}g/ml$. In particular, the extracts of Calystegia soldanella $(IC_{50}$<$8.0\;{\mu}g/ml\;in\;A549;IC_{50}=27.4\;{\mu}g/ml\;in\;Col2)$, Heloniopsis orientalis $(IC_{50}=4.6\;{\mu}g/ml\;in\;A549; IC_{50}=4.5\;{\mu}g/ml\;in\;Col2)$, and Thuja koraiensis $(IC_{50}=1.2\;{\mu}g/ml\;in\;A549;IC_{50}=0.6\;{\mu}g/ml\;in\;Col2)$ showed a potent cytotoxic activity. Further study for the identification of active compounds from these lead extracts might be warranted.