• 약학회지
• /
• 제34권5호
• /
• pp.348-364
• /
• 1990

The activities of twenty-one flavonoids and their related compounds on the hypersensitivity reaction against various antigens were studied in vitro and in vivo. 1. Generally flavonoids inhibited significantly the homologous passive cutaneous anaphylaxis (PCA) induced by reaginic antibody as compared as anaphylaxis by compound 48/80-induced mast cell degranulation, and so more strongly active in the IgE-mediated anaphylaxis than non-IgE-mediated anaphylaxis. 2. Flavonids inhibited remarkably Arths reaction, hemolysin titer, delayed hypersensitivity, haemagglutinin titer, rosette forming cells and plague forming cells against sheep red blood cells, and so it exhibited that flavonoids inhibited type 2, 3 and 4 hypersensitivity. 3. Quercetin, kaempferol, hesperetin, disodium cromoglycate, malvin and baicalein were active dose-dependently in the all types of hypersensitivity. Fisetin, daidzein, morin, narigin, flavone, catechin, rutin, hesperidin, neophsperidin, apigenin and chrysin were significantly active in the various types of hypersensitivity, but apigenin, rutin and catechin were less active in the delayed hypersensitivity. Taxifolin was significantly active in PCA and histamine-induced anaphylaxis except other types of hypersensitivity. Rotenone and cyanin also inhibited all types of hypersensitivity, but they are toxic. 4. Based on these results from hypersensitivity, the following flavonoid structure-activity relationships became apparent. 1) Flavonoids with $C_{2-3}$ double bond in C-ring were more active than that of $C_{2-3}$ saturation. 2) Flavonoids with $C_4$ ketone group in C-ring were more active than abscence of them except catechin and malvin. 3) Flavonoids with benzene ring at positions 2 or 3 in C-ring exhibited same activities. 4) Flavonoids with opening of the C-ring does not abolish their activities. 5) The glycosylated flavonoids in position 3 or 7 was less active than their aglycone. 6) Flavonoids with the more hydroxy group in A and B-ring were more active. 7) Flavonoids with or without $C_3-OH$ did not change their activities.

• Parasites, Hosts and Diseases
• /
• 제49권1호
• /
• pp.1-8
• /
• 2011

The pathogenesis and pathophysiology of Acanthamoeba infections remain incompletely understood. Phospholipases are known to cleave phospholipids, suggesting their possible involvement in the host cell plasma membrane disruption leading to host cell penetration and lysis. The aims of the present study were to determine phospholipase activities in Acanthamoeba and to determine their roles in the pathogenesis of Acanthamoeba. Using an encephalitis isolate (T1 genotype), a keratitis isolate (T4 genotype), and an environmental isolate (T7 genotype), we demonstrated that Acanthamoeba exhibited phospholipase $A_2$ (PLA$_2$). and phospholipase D (PLD) activities in a spectrophotometry-based assay. Interestingly, the encephalitis isolates of Acanthamoeba exhibited higher phospholipase activities as compared with the keratitis isolates, but the environmental isolates exhibited the highest phospholipase activities. Moreover, Acanthamoeba isolates exhibited higher PLD activities compared with the PLA$_2$. Acanthamoeba exhibited optimal phospholipase activities at $37^{\circ}C$ and at neutral pH indicating their physiological relevance. The functional role of phospholipases was determined by in vitro assays using human brain microvascular endothelial cells (HBMEC), which constitute the blood-brain barrier. We observed that a PLD-specific inhibitor, i.e., compound 48/80, partially inhibited Acanthamoeba encephalitis isolate cytotoxicity of the host cells, while PLA$_2$-specific inhibitor, i.e., cytidine 5'-diphosphocholine, had no effect on parasite-mediated HBMEC cytotoxicity. Overall, the T7 exhibited higher phospholipase activities as compared to the T4. In contract, the T7 exhibited minimal binding to, or cytotoxicity of, HBMEC.

• 동의생리병리학회지
• /
• 제19권3호
• /
• pp.779-784
• /
• 2005

Mast cells are a potent source of mediators that regulate the inflammatory response in allergic reaction. To evaluate the atopic allergic effect of Asiasari radix(AR), the author investigated a possible effect of AR on mast cell-mediated allergic reaction, cytokines secretion and mRNA expression in vivo and in vitro. In mice orally administered by AR (0.01, 0.1 and 1.0 g/kg) for 1 h, compound 48/80-induced ear swelling was significantly reduced (P < 0.05). AR had inhibitory effects on tumor necrosis factor $(TNF)-{\alpha}$, interleukin (IL)-8, and IL-6 secretion from HMC-1. Significant reduced levels of $TNF-{\alpha}$ mRNA was observed in the human mast cell line (HMC-1) with AR (1.0 mg/ml). In addition, AR had no cytotoxic effect on cell viability. These results suggest that AR contributes to the treatment of atopic allergic reactions, and that its action may be due to inhibition of cytokine secretion and mRNA expression in HMC-1.

• Korean Journal of Acupuncture
• /
• 제20권3호
• /
• pp.81-90
• /
• 2003

Objectives : This experimental research has been done to study the effects of herbal-acupuncture with Juglandis Semen on the anti-allergic reaction. Methods : ICR mice were injected intraperioneally with compound 48/80 to induce the immediately type hypersensitivity (anaphylaxis). ICR mice were sensitized by PC and SRBC to induce the delayed type hypersensitivity. Sprage-Dawley rats were injected subcutaneously with egg albumin to measure the WBC. ICR mice and Sprage-Dawley rats were injected with Juglandis Semen herbal-acupuncture for the anti-allergic reaction test. Results : 1. In the restraint effect of systemic anaphylactic reaction, the mortality of mice decreased 20% each before 10 minutes and after 5 minutes. 2. In the contact dermatitis induced by PC, both Treat Ⅰand Treat Ⅱ group showed significant(p<0.01, p<0.05) decrease in comparison with the Control group, and also Treat Ⅲ group showed significance(p<0.005). 3. In the delayed type hypersensitivity in mice challenged by SRBC, Treat Ⅰ group showed significant(p<0.05) decrease in comparison with the Control group, and there was significance(p<0.05, p<0.05) in Treat Ⅲ and Treat Ⅳ group. 4. The change of the WBC in allergic rats induced by egg albumin showed significant(p<0.01, p<0.05, p<0.05) decrease in Treat Ⅰ, Treat Ⅱ and Treat Ⅲ group. Conclusions : The restraint effects of Juglandis Semen herbal-acupuncture on the anti-allergic reaction showed significance statistically. And also allergic group treated with $BL_{17}$ acupuncture (Treat Ⅲ group) showed same results.

• 대한화장품학회지
• /
• 제24권3호
• /
• pp.17-23
• /
• 1998

Inner nutshell of Castanea mollisima BL (chestnut) has been used as an anti-aging and anti-wrinkle agent from the ancient time in east Asia. In order to develop new anti-aging and anti-wrinkle, ethanolic extract of inner nutshell of Castanea mollisima BL (Cor-285) was prepared and various biological activities were evaluated. Cor-285 showed potent antioxidant activity, Especially, Cor-285 possessed potent free radical scavenging activity in vitro (IC50:7.6 g/ml) compared to gallic acid (IC50:12.5 g/ml), Cor-285 showed the preventive effect against UV-induced cytotoxicity of fibroblast at concentration of 25-250 g/ml. When Cor-285 was evaluated for its anti-allergic activity, it effectively inhibited histamine release from mast cells induced by compound 48/80 (86% inhibition at 10 mg/ml). The inhibitory activity was stronger than that of glycyrrhiznate. Cor-285 also showed in vivo inhibition against delayed hypersensitivity as well as croton-oil induced ear edema in mice when topically applied These results strongly suggest that Cor-285 may reduce immunoregulatory 1 inflammatory skin trouble. From the attempts to isolate the constituents, citropten (simple coumarin) and ellagic acid, a well known radical scavenger, were isolated. In a clinical trial of twenty healthy volunteers with aged skin,6 weeks application of Cor-285 (3% cream) decreased wrinkle about 26% and increased moisturizing 20% on the skin. All of these results indicate that Cor-285 may be an effective anti-aging and anti-wrinkle agent.

• 약학회지
• /
• 제55권1호
• /
• pp.39-44
• /
• 2011

Many reports indicate that $18{\beta}$-glycyrrhetinic acid ($18{\beta}$-GA) from Glycyrrhizae Radix has anti-inflammatory and immunoregulatory activities, whereas reports regarding anticancer activity of the compound are few. In present study, we investigated antitumor effect of $18{\beta}$-GA on tumor caused by A549 cancer cell in mice. Data resulting from the cytotoxicity assay showed that $18{\beta}$-GA caused killing of A549 cells. $LD_{50}$ values of $18{\beta}$-GA were app. 180 ${\mu}M$ and 80 ${\mu}M$, corresponding to 48 hr- and 72 hr-treatments, displaying that the killing activity was more effective as the $18{\beta}$-GA treatment was prolonged. Based on these data, antitumor effect of $18{\beta}$-GA was tested in nude mice. For induction of the tumor, A549 ($3{\times}10^6$ cells/mouse) was injected subcutaneously into the lateral abdomen of nude mice (Balb/c nu/nu). To determine the antitumor effect, nude mice with tumor were given $18{\beta}$-GA (1 mg/200 ${\mu}l$/mouse) intraperitoneally every three days for four times. Tumor-sizes were measured with a caliper for a period of 24 days. Results showed that the $18{\beta}$-GA treatment reduced the tumor-sizes (P<0.05) as compared with negative control nude mice that received diluent (DPBS). The reduction degree was greater than reduction degree by doxorubicin (60 ${\mu}g$/mouse), and the pattern of reduction was almost sustained during the entire period of the observation. In conclusion, our studies demonstrate that $18{\beta}$-GA has antitumor activity to the A549 cancer cell-caused tumor.

• 대한한방소아과학회지
• /
• 제19권2호
• /
• pp.13-30
• /
• 2005

Objective: Danguieumja-gagambang (DGEJGB), a traditional Korean prescription, has been used as therapeutics for allergic diseases such as atopic dermatitis (AD). In this study, we compared with regulatory Effect of Atopic Allergic Reaction by Prescriptions A and by Prescriptions B. Methods : To evaluate and compare the atopic allergic effectiveness of two prescription (A, B) of DGEJGB, the author investigated a possible effect of DGEJGB on mast cell-mediated allergic reaction, cytokine secretion and mRNA expression in vivo and in vitro. Results : Mast cells are a potent source of mediators that regulate the inflammatory response in allergic reaction. In mice orally administered A, B of DGEJGB ( 0.1, 0.1 and 1.0 g/kg) for 1 h, compound 48/80-induced ear swelling was significantly reduced. Significant reduced levels (P < 0.05). of tumor necrosis factor $(TNF)-{\alpha}$ was observed in the human mast cell line (HMC-1) with DGEJGB (A). IL-6 and IL-8 secretion were significantly inhibited by DGEJGB (A, B). In addition, $TNF-{\alpha}$ and IL-8 mRNA expression were reduced by DGEJGB (A) at the dose of 0.01 mg/ml without cell toxicity. Conclusions : These results suggest that DGEJGB (A) contributes to the treatment of atopic allergic reactions rather than DGEJGB (B), and that its action may be due to inhibition of cytokine secretion and mRNA expression HMC-1.

• Journal of Microbiology and Biotechnology
• /
• 제16권9호
• /
• pp.1464-1467
• /
• 2006

Artemisia princeps Pampanini, which is named as Sajabalssuk (SJ-1) in Korea, was fermented with lactic acid bacteria (LAB), and their antiallergic activities were investigated. When SJ-l was fermented with some LAB isolated from human feces, the inhibition of NO production in RAW264.7 cells and antioxidant activities of SJ-1 were not affected. However, the inhibitory activity of SJ-1 against degranulation of RBL-2H3 cells induced by IgE was increased by LAB fermentation. Among the LAB tested, Bifidobacterium infantis K-525 provided the most potent inhibitory effect of SJ-1 against degranulation of RBL-2H3 cells. SJ-1 extract fermented with B. infantis K-525 (F-SJ-1) potently inhibited the mouse passive cutaneous anaphylaxis reaction induced by IgE with antigen, skin dermatitis induced by 12-O-tetradecanoylphorbol-13-acetate, and scratching behaviors induced by compound 48/80. These inhibitory activities of F-SJ-1 were more potent than those of SJ-1. These findings suggest that the inhibition of SJ-1. extract against IgE-induced allergic diseases, such as rhinitis and asthma, can be enhanced by LAB fermentation.

• Journal of Ginseng Research
• /
• 제44권2호
• /
• pp.215-221
• /
• 2020

Background: Panax ginseng has been used for a variety of medical purposes in eastern countries for more than two thousand years. From the extensive experiences accumulated in its long medication use history and the substantial strong evidence in modern research studies, we know that ginseng has various pharmacological activities, such as antitumor, antidiabetic, antioxidant, and cardiovascular system-protective effects. The active chemical constituents of ginseng, ginsenosides, are rich in structural diversity and exhibit a wide range of biological activities. Methods: Ginsenoside constituents from P. ginseng flower buds were isolated and purified by various chromatographic methods, and their structures were identified by spectroscopic analysis and comparison with the reported data. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H- tetrazolium bromide method was used to test their cytotoxic effects on three human cancer cell lines. Results: Six ginsenosides, namely 6'-malonyl formyl ginsenoside F₁ (1), 3β-acetoxyl ginsenoside F₁ (2), ginsenoside Rh₂₄ (6), ginsenoside Rh₂₅ (7), 7β-hydroxyl ginsenoside Rd (8) and ginsenoside Rh₂₆ (10) were isolated and elucidated as new compounds, together with four known compounds (3-5 and 9). In addition, the cytotoxicity of these isolated compounds was shown as half inhibitory concentration values, a tentative structure-activity relationship was also discussed based on the results of our bioassay. Conclusion: The study of chemical constituents was useful for the quality control of P. ginseng flower buds. The study on antitumor activities showed that new Compound 1 exhibited moderate cytotoxic activities against HL-60, MGC80-3 and Hep-G2 with half inhibitory concentration values of 16.74, 29.51 and 20.48 μM, respectively.

• 동의생리병리학회지
• /
• 제21권3호
• /
• pp.617-625
• /
• 2007

Samul-Tang (SMT) has been used for nourishing of the blood, hematopoiesis as a herbal medicine history. The purpose of this study is to find out anti-allergic inflammatory reaction of SMT. To clarify the mechanism, the effect of SMT on vascular permeability of rat cutaneous tissue and histamine and cytokines (IL-6, IL-8, TNF-${\alpha}$) release from mast cells were observed. The results are the pretreatment with SMT significantly decreased the compound 48/80-induced degranulation and histamine release from RPMC, SMT also inhibited the anti-DNP lgE-induced increment of vascular permeability of rat cutaneous tissue. SMT significantly reduced the PMA plus A23187-induced increment of expression of IL-6, IL-8, and TNF-${\alpha}$ in HMC-1 Cell. The Present study provide evidence that SMT inhibits mast cell-derived inflammatory allergic reactions by blocking histamine release and pro-inflammatory cytokine expression, and suggest the mechanisms of action. Furthermore, in vivo and in vitro anti-allergic effect of SMT suggests a possible therapeutic application of this agent in inflammatory allergic diseases.