• Journal of Ginseng Research
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• v.22 no.3
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• pp.200-205
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• 1998

Isolated rabbit jejunal segments were used to study the effects of ginseng total saponins (GTS) , protopanaxatriol saponins (PT) and protopanaxadiol saponins (PD) on intestinal contractility. GTS, PT and PD caused a dose-dependent decrease in intestinal spontaneous movements, and PT was the most efficacious of them. The effect of GTS, PT and PD were not blocked by pretreatment with phentolamine (10-6 M), yohimbine (10-6 M), d1-propranolol (10-6 M), naloxone(10-6∼10-5M), Nu-nitro-L-arginine methyl ester (10-4 M), methylene blue (10-5M), and N-ethylmaleimide (10-4 M). However, pretreatment with tetraethylammonium chloride (3-10 mM) antagonized the effect of GTS, PT and PD. Furthermore, 4-amlnopyridine (1 mM) also inhibited the effect of GTS, PT and PD. The results suggest that GTS, PT and PD inhibited the spontaneous movements in isolated rebait jejunum by causing hyperpolarization through an activation of K+ channels directly.

• The Korean Journal of Physiology and Pharmacology
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• v.1 no.2
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• pp.143-149
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• 1997

We studied the effects of ginseng protopanaxadiol (PD) and protopanaxatriol (PT) saponins on the analgesia using several pain tests such as writhing, formalin, and tail-flick test. Using mouse, pretreatment of PD or PT saponins (i.p.) induced inhibition of abdominal constrictions caused by 0.9% acetic acid administration(i.p.). The $AD_{50}$ was around 27 (17-43) mg/kg for PD and 13.5 (3-61) mg/kg for PT saponins in writhing test. Both PD and PT saponins also showed the inhibition of bitings and lickings of hindpaw after administration of 1% formalin. In particular, both PD and PT saponins showed analgesic effects on second phase of pain. The $AD_{50}$ was 44.5 (26-76) mg/kg for PD and 105 (55-200) mg/kg for PT saponins in second phase of formalin test. For first phase pain inhibition by PD or PT saponins, they were required higher concentrations. However, PD saponins showed weak analgesic effects in tail-flick test with high concentration. In conclusion, we found that both PD and PT saponins have the analgesic effects in writhing test and second phase of pain in formalin test. These results suggest that both PD and PT saponins inhibit neurogenic or tonic pain rather than acute pain.

• Journal of Ginseng Research
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• v.21 no.1
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• pp.35-38
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• 1997

We investigated the effects of ginseng protopanaxadiol (PD) and protopanaxatriol (PT) saponins on the spontaneous contractility of intestine. Treatment with PD saponins showed a slight inhibition of spontaneous contraction of rabbit jejunum. In contrast, PT saponins showed much larger inhibition with dose-dependent manner in a range of 25~250 $\mu\textrm{g}$/ml. The inhibitory effect by PT saponins was not desensitized with continuous presence of PT saponins for several minutes. In addition, leu-enkephalin (1 PM) also inhibited the spontaneous contraction of rabbit jejunum but the in- hibition by leu-enkephalin was desensitized rapidly. The presence of PT saponins prevented the desenstization induced by leu-enkephalin. In conclusion, we found that PT saponins exert inhibition of spontaneous contractility of rabbit jejunum and the pattern of inhibition is different from that of opioid.

• Proceedings of the Ginseng society Conference
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• 1998.06a
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• pp.31-39
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• 1998

We have investigated the antinociceptive efficacy of ginseng saponins in mice using l% formalin, which induce two phases of pain (acute and tonic pains) and is known to induce a clinically related pain. Ginseng total saponins (GTS) relieved both phases of pain with EDso of 162 mghg for acute and 92 mg/kg for tonic pain, respectively. Both protopanaxadiol (PD) and protopanaxatriol (PT) saponins did not attenuated acute phase of pain but relieved tonic phase of pain with EDso of 45 mg/kg for PD saponins and 105 mghg for PT saponins, respectively. Moreover, ginsenoside Rc, Rd, and Re among representative ginsenosides such as Rbl, Rc, Rd, Re and Rgl relieved slightly but significantly acute phase of pain and strongly attenuated tonic phase of pain but Rf relieved only tonic phase of pain. However, PD and PT saponins, and the individual ginsenosides tested except GTS did not greatly attenuate thermal noxious pain (tail-flick test). These results suggest that single ginsenoside or mixture of various ginsenosides mainly induce differential antinociception in mice.

• Journal of Pharmaceutical Investigation
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• v.16 no.4
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• pp.135-138
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• 1986

Ginseng total saponins(GS), protopanaxadiol saponins(PD) and protopanaxadiol saponins(PT) antagonized the analgesia in mice induced by morphine. The administrations of 2,4-dihydroxyphenylalanine, and 5-hydroxytryptophan reduced the GS, PD and PT antagonisms of morphine analgesia. Possible mechanisms involved in the antagonistic actions of GS, PD and PT on morphine analgesia were described.

• Archives of Pharmacal Research
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• v.10 no.3
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• pp.188-192
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• 1987

The present study was undertaken to determine the inhibitory effects of orally administered ginseng saponins (GS), protopanaxadiol saponins (PD), protopanaxatriol saponins (PT) and ginseng ether fraction (GE) on the development of morphine induced tolerance and physical dependence in mice and also to determine the hepatic glutathione contents. GS, PD and PT inhibited significantly the development of morphine induced tolerance and physical dependence, but GE was effective only on the inhibition of the development of morphine induced physical dependence. GS, PD, PT and GE also inhibited the hepatic glutathione level decrease induced by morphine multiple injections.

• Journal of Ginseng Research
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• v.19 no.2
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• pp.101-107
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• 1995

The present study was undertaken to examine the effects of ginseng saponins [ginseng total saponin (GTS), protopanaxadiol saponin (PD) and protopanaxatriol saponin (PT)] on the hyperactivity, reverse tolerance and dopamine receptor super-sensitivity induced by cocaine. A single treatment with cocaine produced hyperactivity. Repeated administration of cocaine developed reverse tolerance and dopamine receptor super-sensitivity was also developed in reverse tolerant mice which had received the same cocaine. The hyperactivity and the developments of reverse tolerance and dopamine receptor super-sensitivity by cocaine were inhibited by ginseng saponins. From these results, it is proposed that ginseng saponins may be useful for the prevention and therapy of the adverse actions of cocaine. In addition, the rank order of inhibitory potential was observed as PT>GTS>PD. Key words Cocaine, hyperactivity, reverse tolerance, dopamine receptor super-sensitivity, ginseng saponins.

• Proceedings of the Ginseng society Conference
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• 1987.06a
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• pp.38-46
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• 1987

The present study was undertaken to determine the inhibitory effects of orally administered ginseng saponins (GS), protopanaxadiol saponins(PD) and protopanaxatriol saponins(PT) on the development of morphine induced tolerance and physical dependence in mice, and to determine the increases in the loss of morphine tolerance and dependence. The study also sought to determine the hepatic glutathione contents, which are closely related to the degree of detoxication of morphinone, a novel metabolite of morphine, and the effects of ginseng saponins on morphine 6-dehydrogenase. The results of the present study showed that GS, PD and PT administered orally inhibited the development of morphine-induced tolerance and dependence. GS, PD and PT, however, increased the loss of morphine tolerance and dependence. GS, PD and PT inhibited the reduction of hepatic glutathione concentration in mice treated chronically with morphine, and the activity of morphine 6-dehydrogenase. So we hypothesized that these results were partially due to the dual action of the test drugs, the inhibition of morphine production and the activation in morphine-glutathione conjugation due to the increased glutathione level for detoxication.

• The Korean Journal of Physiology and Pharmacology
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• v.2 no.2
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• pp.201-207
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• 1998

To evaluate the possibility that the ginseng saponins could be developed as an anti-arteriosclerotic agent, we examined the inhibitory effects of ginseng saponins (total saponin[TS], panaxatriol[PT], panaxadiol[PD]) on the expression of c-fos mRNA and the proliferation of cultured rat aortic vascular smooth muscle cells (VSMCs) stimulated by angiotensin II (Ang II). TS and PT (1.0 mg/ml) suppressed c-fos mRNA induction in VSMCs stimulated by $10^{-5}$ M Ang II. The order of inhibitory potency was PT>TS. Ginseng saponins ($0.01{\sim}1.0$ mg/ml) inhibited the proliferation of VSMCs stimulated by Ang II in a concentration dependent manner, the inhibitory potency was TS＞PT＞PD at $0.1{\sim}1.0$ mg/ml. These results suggest that ginseng saponins may suppress Ang II-stimulated proliferation of aortic VSMCs which can be seen in atherosclerosis, hypertension and restenosis.

• Proceedings of the Ginseng society Conference
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• 1993.09a
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• pp.84-93
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• 1993

It has been reported that ginseng is effective in the central nervous system, immune system, and the strong inflammatory responses. However, there has been no research report yet about the effect of ginseng on allergic hypersensitivity reactivity. To confirm the ginseng effects on the release of mediators(histamine. leukotrienes etc.) which cause the hypersensitivity reactivity and inflammatory response, we used actively sensitized guinea pig airway tissues by utilizing the superfusion technique. In this procedure. the contractile response and mediators released after antigen stimulation of sensitized tissues, and IgG and IgE antibody products were measured in sera of immunized animals. Then the results of the controll group were compared to those of ginseng pretreatment groups. In the total saponin(TS) and panaxatriol(PT) pretreatment, histamine release decreased by $20\%$ in the tracheal tissues after active sensitization by ovalbumin(OVA, 10mg/kg), but in the lung parenchyma, histamine release decreased by $40\%.$ Panaxadiol(PD) significantly decreased histamine release by $40\%$ in the both tissues after active sensitization. TS, PT and PD of ginseng poorly blocked leukotrienes (LTs) and prostagrandin $D_2(PGD_2)$ release(less than $10\%$). Ginseng TS and PT had no effect on the serum IgG antibody production by ovalbumin, whereas PD significantly increased serum IgG antibody contents(approximately by 2 times). However, $IgG_1$ antibody products in the serum of guinea pig actively sensitized with ovalbumin after PD pretreatment were decreased, compared to that with ovalbumin alone. IgE antibody production by passive cutaneous anaphylaxis(PCA) titer in the TS pretreatment increased 3 times more than in the absence of TS(PCA titer by PT was not detected). These studies show that some ginseng saponins can in part act to inhibit mediator release in antigen - induced airway smooth muscle by inducing the IgG antibody production which has been changed in the specificity.