• Natural Product Sciences
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• 제9권3호
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• pp.158-160
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• 2003

Polyacetylenes were isolated from Panax ginseng C.A. Meyer (Family Araliaceae), and their inhibitory effects on growth, infection and VacA vacuolation of Helicobacter pylori (HP) were investigated. Ginseng polyacetylenes did not inhibit the infection of HP into KATO cells. However, polyacetylenes inhibited HP growth and vacuolation of Hela by VacA toxin. Panaxytriol showed the most potent inhibition with $IC_{50}$ values of 0.05 and 0.046 mg/ml, respectively.

• 약학회지
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• 제32권2호
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• pp.137-140
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• 1988

To investigate polyacetylene compounds isolated from petroleum ether extract of panax ginseng effect on the macromolecule synthesis, lympoid lukemia L1210 cell was incubated with them at 4, 8, 12,16 hours. Panaxydol, panaxynol and panaxytriol as cytotoxic substances inhibited the synthesis of macromolecule such as DNA, RNA and protein. Panaxydol which had the most potent cytotoxicity among these three compounds showed the strongest inhibitory effect on DNA, RNA and protein synthesis. For DNA and RNA synthesis, panaxynol and panaxytriol decreased the rate of inhibition with the incubation time but panaxydol had a strongest inhibitory effect at 16 hour incubation time. Protein synthesis was markedly inhibited by all these polyacetylene compounds. It was obserbed that there is a relationship between cytotoxicities of polyacetylene compounds and the inhibition of macromolecule synthesis.

• 생약학회지
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• 제20권3호
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• pp.154-161
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• 1989

Effects of panaxydol, panaxynol and panaxytriol isolated from Panax ginseng C.A. Meyer on some enzyme activities were determined. Activities of ATPase, membrane-bound enzyme from Sarcoma 180 and rat liver were slightly inhibited by panaxydol. Activities of 5'-nucleotidase, membrane-bound enzyme and succinate cytochrome c reductase in mitochonidria from sarcoma 180 and rat livers were significantly inhibited in a dose-dependent manner by panaxynol. The inhibitory effects of panaxydol and panaxynol on succinate cytochrome c reductase activities were more potent than those on 5'-nucleotidase activities and panaxynol was found to be a very potent inhibitor of succinate cytochrome c reductase. Activities of glucose-6-phosphatase in endoplasmic reticulum from Sarcoma 180 and rat livers were not affected by all three polyacetylenes. These results suggested that the inhibitory effects of panaxydol and panaxynol on enzyme activities might contribute to their biological activities.

• Toxicological Research
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• 제4권1호
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• pp.13-22
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• 1988

The inhibitory effect of three polyacetylene compounds, panaxydol, panaxynol and panaxytriol isolated from Panax ginseng C.A. Meyer on $CCl_4$induced lipid peroxidation in vivo and in vitro hepatic microsomal lipid peroxidation induced by ADP-$Fe^{3+}$, NADPH and NADPH-cytochrome P-450 reductase were investigated. Their effects on lowering the lipid peroxide levels both in serum and liver and lowering the serum enzyme (GOT, GPT, LDH) activities without the $CCl_4$-induction were also determined. Male ICR mice were pretreated i.p. with polyacetylene compounds or DL-${\alpha}$-tocopherol before administration of $CCl_4$ i.p. and 20 hr after the administration of $CCl_4,$ serum and liver were analyzed. Hepatic microsome was isolated and used for the in vitro NADPH-dependent lipid peroxidation system. Except for panaxynol, treatment with polyacetylenes to control mice did not reduce the levels of lipid peroxides and serum enzyme activities. Panaxynol itself inhibited lipid peroxidation in the liver of normal mice. Polyacetylene compounds protected from the $CCl_4$-induced hepatic lipid peroxidation and lowered serum lipid peroxide levels. Polyacetylenes also inhibited the in virto hepatic microsomal lipid peroxidation in a dose-dependent manner. The results suggest that panaxydol, panaxynol and panaxytriol seem to be the antioxidant components which contribute the anti-aging activities of Panax ginseng C.A. Meyer.

• Toxicological Research
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• 제4권2호
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• pp.95-105
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• 1988

The effects of polyacetylenes on living membrances, rat erythrocyte and murine leukemic L1210 cell as well as artificial lipid bilayer were determined to investigate the cytotoxic mechanism of polyacetylenes against cancer cell lines. As results, panaxydol and panaxynol caused erythrocyte hemolysis dose-dependently while panaxytriol had no lysis. For liposomes composed of phosphatidyl choline (PC) and phosphatidic acid(PA), all three polyacetylenes supressed the osmotic behavior at the same degree.

• Journal of Ginseng Research
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• 제13권1호
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• pp.49-55
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• 1989

정상 wistar rat strain의 체중 및 장기무게 변화 그리고 사료, 물 섭취량의 변화 등을 조사함으로써 polyacetylene 화합물들의 투여량에 따른 독성변수(toxicological parameter)의 범위를 추정하고자 하였다. 또한, ICR mouse strain의 Sarcoma-180으로 유도되는 고형암의 억제와 관련해서 polyacetylene 화합물들의 투여량에 따른 독성변수(toxicological parameter)와의 관계를 관찰하고자 하였다. Panaxydol 40$\mumoles/kg b.w.을 3일간 연속 복강 투여했을때 wistar rat의 체중증가율은 대조군보다 약 17% 감소하였으나, polyacetylene 의 투여를 중지하면 약 4일 경과후부터 체중증가율이 정상으로 회복되었다. 이 투여량을 20$\mumoles/kg b.w.로 줄이면 대조군과의 체중증가율의 차이는 약 10% 정도로 완화되며 그 체중감소율은 panaxydol, panaxynol, panaxytriol의 순으로 증가하였다. 이때 장기무게의 관찰 결과는 대조군과 polyacetylene 화합물들 투여군 사이에 의미있는 차이가 없는 것으로 나타났다. 또한 정상 mice의 간세포에 대한 electron micrograph 관찰결과, panaxydol 40$\mumoles/kg b.w./day 투여시에도 대조군에 비하여 별다른 미세조직의 변화가 관찰되지 않았다.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1984년도 학술대회지
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• pp.159-168
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• 1984

생약의 화학적 특성에 대한 계속적인 연구가 이루어짐에 따라 우리는 홍삼 및 백삼의 화학성분을 상대적으로 규명하였다. 홍삼은 극성이 약한 분획에서 5개의 새로운 배당체(20R-ginsenoside $Rg_{2},\;Rh_{1};20R$, 20S-ginsenoside $Rg_{3}; ginsenoside\;Rh_{2}$와 새로운 아세칠렌 화합물(Panaxytriol)을 함유하는 특징적인 성분들이 gins - enoside Rh1, Rg2와 함께 분리되었다. ginsenoside Rh2는 배양된 종양세포에 대해 세포독소 효과를 보여주었다. 백삼은 수용성 분획에서 특징적인 성분이 있는 것으로 밝혀졌으며, 여기에서 malonly-ginsenosides Rb1, Rb2, Rc 및 Rd로 명명된 새로운 배당체 성분이 분리되었다. Malona-ginsenosides는 백삼에서는 주요한 배당체이지만, 홍삼에서는 검출되지 않았다.

• Journal of Ginseng Research
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• 제19권2호
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• pp.114-116
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• 1995

Panax ginseng ginsenosides were examined for their affects on the DNA synthesis. The DNA 1 synthesis was measured by the thymidine incorporation into NIH3T3 cells. The ginsenoside, panaxytriol, $Rh_1$ and $Rh_2$ showed reduced [$^{3}H$]-thymidine incorporation. However, other ginsenosides of $Rh_1$, $Rh_2$ and $Rh_3$ did not inhibit DNA synthesis. Among the various ginsenosides, ginsenoside $Rh_2$ was found to be the most inhibitory on DNA synthesis. We suggest $Rh_2$ as one of the potential choice of antiproliferative drugs.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.163.3-163.3
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• 2003

Panax ginseng C.A. Meyer (Family Araliaceae) was treated at low ($60^{\circ}C$, LT), mild ($100^{\circ}C$, MT) and high ($120^{\circ}C$, HT) temperatures, some components (panaxytriol, ginsenosides and polysaccharides) were isolated, and their inhibitory effects on growth, infection and VacA vacuolation of Helicobacter pylori (HP) were investigated. The molecular weights of polysaccharides were decreased according to the increasing processed temperature. Ginseng polysaccharides inhibited the HP infection into KATO III cells, but did not inhibit HP growth and VacA vacuolation of HeLa cells. (omitted)

• Journal of Ginseng Research
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• 제44권6호
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• pp.770-774
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• 2020

Background: Fermentation has been shown to improve the biological properties of plants and herbs. Specifically, fermentation causes decomposition and/or biotransformation of active metabolites into high-value products. Polyacetylenes are a class of polyketides with a pleiotropic profile of bioactivity. Methods: Column chromatography was used to isolate compounds, and extensive NMR experiments were used to determine their structures. The transformation of polyacetylene in red ginseng (RG) and the production of cazaldehyde B induced by the extract of RG were identified by TLC and HPLC analyses. Results: A new metabolite was isolated from RG fermented by Chaetomium globosum, and this new metabolite can be obtained by the biotransformation of polyacetylene in RG. Panaxytriol was found to exhibit the highest antifungal activity against C. globosum compared with other major ingredients in RG. The fungus C. globosum cultured in RG extract can metabolize panaxytriol to Metabolite A to survive, with no antifungal activity against itself. Metabolites A and B showed obvious inhibition against NO production, with ratios of 42.75 ± 1.60 and 63.95 ± 1.45% at 50 µM, respectively. A higher inhibitory rate on NO production was observed for Metabolite B than for a positive drug. Conclusion: Metabolite A is a rare example of natural polyacetylene biotransformation by microbial fermentation. This biotransformation only occurred in fermented RG. The extract of RG also stimulated the production of a new natural product, cazaldehyde B, from C. globosum. The lactone in Metabolite A can decrease the cytotoxicity, which was deemed to be the intrinsic activity of polyacetylene in ginseng.