Organizing co mmittee

STUDY OF THE ACUTE TOXICITY OF NEW DIAZOIMINO 
DERIVATIVES OF GOSSYPOL
 
 
N.Kh. Yakubova, N.A. Tagayalieva, L.U. Makhmudov,
Q.R. Baratov
K.Zh. Rezhepov, M.B. Gafurov 
 
A.S. Sadykov Institute of Bioorganic Chemistry Academy of Sciences of the Republic of 
Uzbekistan, 100125 Tashkent, Uzbekistan, Mirzo Ulugbek str, 83.
e-mail: [e-mail]
 
 
It is known that the use of gossypol in practical medicine is limited due to it’s high 
toxicity and other side effects on the body.
It is known from the literature that Schiff 
bases of gossypol, obtained by amino compounds of various nature, exhibit a number of 
biological 
activities, 
including 
anticancer, 
antiviral, 
immunomodulatory, 
immunosuppressive and similar activities. With this in mind, we studied the acute 
toxicity of a number of newly synthesized gossypol diazoimino derivatives with 
nitrogen-containing heterocyclic and aliphatic amino compounds.
Diazoimino derivatives of gossypol XAN-III, XAN-IV, XAN-V, NY-I, NY-X were 
studied for acute toxicity when administered intragastrically to mice. The results are 
shown in the table. With the introduction of substances XAN-III, XAN-IV, XAN-V, 
NY -I, NY-X to mice once intragastrically at a dose of 2000 mg/kg, after 5-10 minutes, 
the animals observed washing, narrowing of the eyes, bunching and urination. Mice 
returned to normal within 1-3 hours. The death of animals was not observed (0/5). 
Further, throughout the entire period of research (14 days), observations of surviving 
animals were carried out. Observation of experimental animals according to the studied 
indicators did not reveal any deviations in the condition of the hair and skin, the 
position of the tail, the consistency of fecal masses, diuresis, and changes in body 
weight from the animals of the control group.
Thus, the study of the acute toxicity of substances after intragastric administration in 
accordance with the modified OECD classification showed that the samples XAN-III, 
XAN-IV, XAN-V, NY-I, NY-X correspond to the V-class of substance toxicity 
(Practically non-toxic), LD50 ˃ 2001 mg/kg. 
Table. Acute toxicity rates for intragastric administration of samples XAN-III, 
XAN-IV, XAN-V, NY-I, NY-X to mice 
№ Samples 
Animal species / 
route of 
administration 
Doses, 
mg/kg 
Number of dead / 
number of animals 
in the group 
LD
50
, mg/kg 
Toxicity class
1. 
XAN-III 
mouse/i/s 
2000 
0/5 
˃2001 (V class) 
2. 
XAN-IV 
mouse/i/s 
2000 
0/5 
˃2001 (V class) 
3. 
XAN-V 
mouse/i/s 
2000 
0/5 
˃2001 (V class) 
4. 
NY-I 
mouse/i/s 
2000 
0/5 
˃2001 (V class) 
5. 
NY-X 
mouse/i/s 
2000 
0/5 
˃2001 (V class) 
Control 
mouse/i/s 
5,0 ml 
0/5 
5 samples of gossypol diazoimino derivatives with nitrogen-containing 
heterocyclic and aliphatic compounds XAN III, XAN IV, XAN V, NY I, NY X when 
administered intragastrically correspond to the V class of substance toxicity (practically 
non-toxic), LD
50
˃ 2001 mg/kg. 

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Poster presentation 
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