NEW ANTIHISTAMINES - - CITRAL AND BETA-IONONE

• Document Type: CREST
• Collection: General CIA Records
• Document Number (FOIA) /ESDN (CREST): CIA-RDP80-00809A000600290393-4
• Release Decision: RIPPUB
• Original Classification: C
• Document Page Count: 2
• Document Creation Date: December 22, 2016
• Document Release Date: September 28, 2011
• Sequence Number: 393
• Publication Date: March 10, 1950
• Content Type: REPORT

Sanitized Copy Approved for Release 2011/09/28: CIA-RDP80-00809A000600290393-4
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CENTRAL INTELLIGENCE AGENCY REPORT
INFORMATION FROM
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Medical - Chemotherapy
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Aug 1949
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SUPPLEMENT TO
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THIS IS UNEVALUATED INFORMATION
NEW ANTIHISTAMINES -- CITRAL AND BETA-IONONE
M. L. Rokhlina
Cen Ophthalmological Inst imeni Gelmgolts
Inst Dir: Prof A. A. Kolen
During the last decade many foreign scientists have worked on synthesizing
antihistamines. The experimental use of citral and beta-ionone in the Soviet
Union (initiated by Professor Be]akhovskiy) is extremely important.
Citral was first extracted in the USSR on a commercial scale in 1930. It
can be obtained from the oil of Eucalyptus Staigerlane and from other essential
oils. It is a light yellow or greenish oily fluid with an agreeable odor like
that of lemon. From its chemical structure it may considered an aliphatic alde-
hyde.
In 1941 it was found that beta-?.onone (from which Vitamin A is synthesized)
and ioncite (a compound of beta-ionone and citral) produced antithyroid, epithe-
lizing, and regenerative effects similar to those of Vitamin A. Beta-ionone is
synthesized from citral and, from its chemical structure, may be considered part
of the molecule of Vitamin A1.
Our joint studies with A. A. Bodrova (Chair of Biology of the former Fourth
Moscow Medical Institute) showed that induced A avitaminosis in rats was not cured
by beta.ionone admixtures but that its development was arrested. This indicates
that it has a possible relation to the synthesis of Vitamin A in the organism and
may partially replace it.
Experimental tests proved that beta-ionone and citral inhibited thyroidin-
induced thyrogenic metamorphoses in axolotls and that beta-ionone and that beta-
ionone and especially citral have antithyroid effects.
Twii NAVY ~NSpe I DISTRIBUTION
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Gonadotropic reaction in young female mice and male rats is greatly increased
by simultaneous introduction of prolan (chorionic gonadotropin) and beta-ionone
or carotine. Beta-ionone (or carotine) also strengthens the effect of pituitary
extrects on the weight of the adrenal glands.
It was established experimentally that citral and beta-ionone, like carotine,
may either strengthen or inhibit the action of hormones. Hence, together with
hormones, they may influence the processes of growth and puberty.
Experiments on the interdependence of the effects of citral or beta-ionone
and that of mediators (acetyl choline, adrenalin, and histamine) are outlined be-
low.
Experiments on the eyes of frogs showed that citral, like adrenalin reduced
the contraction induced by v-trnnic substances and even dilated the pupil. Its
pronounced antihistaminic action was demonstrated by experiments on the isolated
hearts of frogs, and on isolated intestines of guinea pigs in vitro, where spasms
induced by histamine were greatly decreased by introducing citral.
Data from these three series of tests were the basis for subsequent clinical
ubservations (in association with our laboratory) on many diseases involving dis-
turbances of histamine metabolism.
Cit:al wds used by Prof F. I. Dobromyl'skiy in inhalants and gargles, as well
as internally as an antihistaminic, in over 200 cases of pulmonary and laryngeal
tuberculosis. It proved effective as an analgesic, antiphlogistic, and epitheliz-
ing agent. It also facilitated elimination of dysphagia and of the perifocal zone
of infection in acute or exacerbated processes.
Applications of a warm solution of citral (2 cubic centimeters of one-percent
alcoholic solution in 50 cubit centimeters of water) have been found to have an anal
gesic effect in ulcerous ginaivostomatitis, glossalgia, and hyperesthenia of the
dentine. A 0.01-percent solution of citral or beta-ionone was used successfully
by Pertsova, Belousova, and Mogilevskaya as an analgesic and epithelizing agent
which was administered in drops for keratitis, and with the addition of fomenta-
tions, in blepharitis.
To ascertain the comparative effects of citral and adrenalin on the vascu-
lar system, tests were made with various citral concentrations on the isolated
ear of a rabbit and hind legs of a frog. It was discovered that a 1:10,000 solu-
tion of citral neutralized the effect of adrenalin and produced rapid and strong
vasodilation.
On the initiative Balakhovskiy, citral and beta-ionone were used success-
fully in treating hyperthyreosis, hypertonia (three drops of a one-percent al-
coholic solution of citral per day), and vegetative crises during menopause.
The use of beta-ionone is impeded by the fact that its synthesis is a compli-
cated process, while citral is available as a natural product and also produces
a more active anLithyroid, antihistaminic, and vasomotor effect.
Soviet-manufactured citral and beta-fonone produce no toxic effects. In
fact, since they are chemically related to Vitamin A, as mentioned above, they
have a similar biological action.
Discovery of the medicinal effect of citral as an antihistamine in glaucoma
and in dysphagia due to pulmonary and laryngeal tuberculosis is an indisputable
Soviet achievement.
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