Pharmacology of guaiazulene, with special reference to anti-inflammatory effect due to histamine-release inhibition

Yamasaki, Hidemasa; Irino, Shôzo; Uda, Akio; Uchida, Karyo; Ohno, Hiroyuki; Saito, Noriaki; Kondo, Kazuji; Jinzenji, Kei; Yamamoto, Takashi

doi:10.1254/fpj.54.362

Cited by 20 publications

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“…Another interesting fact is that guaiazulene, nicotinamide, and salicylate, which had been reported as the substances inhibiting histamine release from our laboratory (7,8), showed hardly any effect on oxygen uptake in the concentration at which histamine release is inhibited. 3) Effect of succinate on histamine release by chemical substances from lung tissue of non-sensitized guinea pig Examinations were made on the possibility of histamine release by succinate inde pendent of anaphylactic reaction.…”

Section: )mentioning

confidence: 85%

Energy Metabolic Aspect of Histamine Release in Anaphylaxis

Yamasaki

Muraoka

Endo

1960

Japanese Journal of Pharmacology

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There are some evidences suggesting participation of enzyme process in the mechanism of histamine release during anaphylactic reaction. Mongar and Schild (1-3) reported that oxygen and calcium are essential in the release of histamine by antigen from the chopped lung tissue of a sensitized guinea pig, that there are optimal temperature and pH in this reaction, and that this reaction is inhibited by enzyme inhibitors such as cyanide, iodo acetate, and p-chloromercuribenzoate.More recently, Moussatch6 and Danon (4, 5), using lung slices of a guinea pig, indicated that the endogenous tissue respiration and the release of histamine are increased by addition of succinate during anaphylaxis. The present paper describes some observations on the relationship between histamine release and energy metabolism in the in vitro anaphylactic reaction, with special reference to the effect of succinate which is deemed important. METHODSSensitization. Young guinea pigs weighing 250 300 g were sensitized by injections of a saline solution of 10 % egg albumin (Merck $ 960) 1 c.c. under the back skin and I c.c. in the peritoneal cavity. The animals were submitted to the experiment 3 6 weeks later. Preparation of minced lung tissue. Both lungs and a piece of ileum were excised from a guinea pig bled by severence of carotid artery. Sufficient sensitization was checked by the contraction of an ileal segment suspended in a Tyrode bath containing antigen. The excised lungs were washed with physiological saline solution. Gross moisture was wiped off with a filter paper, and cut into fine pieces of 1.5x 1 mm size by a tissue mincer especially devised for this purpose (6). The tissue particles obtained were suspended in 50 c.c. of Krebs-Ringer solution and shaken at 37'C for 20 minutes to remove spontaneous ly releasable histamine ; then collected on a filter paper wetted with Krebs-Ringer solution and divided into ten to twelve masses of 100 mg each by the aid of fang's torsion balance.

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Section: )mentioning

confidence: 85%

Energy Metabolic Aspect of Histamine Release in Anaphylaxis

Yamasaki

Muraoka

Endo

1960

Japanese Journal of Pharmacology

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“…therapeutic effect on various types of inflammation, widely known empirically. The anti-inflammatory effect is suggested to be due to the presence of azulene in the essential oil component of chamomile leachate [15] [16].…”

Section: Accepted Articlementioning

confidence: 99%

“…Chamomile has been one of the most commonly used herbal medicines since ancient times, and among its many benefits is its therapeutic effect on various types of inflammation, which is widely known empirically. The anti‐inflammatory effect is suggested to be due to the presence of azulene in the essential oil component of chamomile leachate [ 15 , 16 ]. The emergence of azulene as a therapeutic agent was prompted by research on azulene derivatives, with guaiazulene and chamazulene being the two most effective.…”

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Guaiazulene derivative 1,2,3,4‐tetrahydroazuleno[1,2‐b] tropone reduces the production of ATP by inhibiting electron transfer complex II

2021

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Molecularly targeted therapy has been employed for treatment of various types of cancers. However, cancer cells often acquire resistance to molecularly targeted drugs that inhibit specific molecular abnormalities, such as constitutive activation of kinases. Even in cancer cells that have acquired resistance, enhanced anabolism, including the synthesis of nucleotides, amino acids, and lipids, is common to normal cancer cells. Therefore, there is a renewed interest in effectively eliminating cancer cells by specifically targeting their abnormal energy metabolism. Multiple strategies are currently being developed for mitochondrial-targeted cancer therapy, with agents targeting oxidative phosphorylation, glycolysis, the tricarboxylic acid cycle, and apoptosis. In this study, we found that one of the guaiazulene derivatives, namely 1,2,3,4-tetrahydroazuleno[1,2-b] tropone (TAT), inhibited the proliferation of cancer cell lines stronger than that of normal cells. Additionally, we showed that TAT inhibited energy production in cancer cell lines, resulting in apoptosis. Analyses done in cancer cell lines

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“…Mention must also be made of the work of YAMASAKI et al (1958), according to which guaiazulene inhibits the passive cutaneous anaphylaxis (PCA) of rats by i.p. injection or external application to the local skin.…”

Section: The Azulenesmentioning

confidence: 99%

Anti-Inflammatory Substances of Plant Origin

Gábor¹

1979

Handbook of Experimental Pharmacology

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Pharmacology of guaiazulene, with special reference to anti-inflammatory effect due to histamine-release inhibition

Cited by 20 publications

References 0 publications

Energy Metabolic Aspect of Histamine Release in Anaphylaxis

Energy Metabolic Aspect of Histamine Release in Anaphylaxis

Guaiazulene derivative 1,2,3,4‐tetrahydroazuleno[1,2‐b] tropone reduces the production of ATP by inhibiting electron transfer complex II

Anti-Inflammatory Substances of Plant Origin

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