Environmental Engineering Reference
In-Depth Information
TABLE 11.8
Antiarrhythmic Activity of Stevioside and Its Complexes with 
Lappaconitine
Rat Survival Rate (%)
Regimen of Administration
Complex + Arrhythmogen
Arrhythmogen + Complex
Agent
Dose (mg/kg)
CaCl 2
Adrenaline
CaCl 2
Adrenaline
Stevioside
0.120
40
50
0
0
Complex 1:1
0.150
100
100
20
0
Complex 4:1
0.150
100
100
20
0
Complex 8:1
0.135
80
100
100
0
Complex 16:1
0.128
80
40
20
20
Lappaconitine
0.290
50
0
0
0
Arrhythmogens: CaCl 2 (250 mg/kg), adrenaline (0.3 mg/kg) administered intravenously.
arrhythmias in animals. Both complexes showed low activity in the developed calcium arrhythmia
model and no activity at all in the adrenaline arrhythmia model.
Noteworthy results were obtained for the complex with composition 8:1, which ensured full pro-
tection of animals when administered preventively and after the development of calcium chloride
arrhythmia. In the calcium chloride arrhythmia model the complex with composition 16:1 retains
high activity (80%) only when administered preventively.
The data of Table 11.9 on the quantitative characteristics of the complexes indicate that complex-
ation of lappaconitine with stevioside, like in the case of glycyrrhizic acid, allows decreasing the
therapeutic dose of the pharmacon signiicantly.
It should be noted that the molecule of stevioside, unlike GA, has no free carboxyl groups.
Association of glycoside is likely to occur only due to the bonding of carbohydrate fragments.
However, it is not impossible that in vivo ester bonds hydrolysis takes place with the formation of
acid diglucoside capable of forming associates acting as pharmacon complexing agents.
Complexation of stevioside with luoxetine allows decreasing the pharmacon toxicity by 32
times. For example, at intragastrical administration LD 50 of luoxetine is 248 mg/kg, while LD 50 of
complex 4:1 is higher than 8000 mg/kg.
The study of pharmacological properties of complexes of luoxetine with stevioside ST:FL with
composition 1:1 and 4:1 demonstrated a reduction of depressive effect of l-DOPA on emotional and
motor activity in mice, similar to that of luoxetine. The effect of complexes was shown to depend
on the dose. Both complexes act on the dopaminergic system in the same way as luoxetine.
TABLE 11.9
Quantitative Characteristics of Stevioside-Lappaconitine Complexes
Lappacontine Content 
in the Dose (mg)
Decrease in Therapeutic 
Dose (Times)
Molecular Composition
Dose (mg/kg)
Complex 1:1
0.150
0.063
4.6
Complex 4:1
0.150
0.023
12.0
Complex 8:1
0.135
0.011
16.0
Complex 16:1
0.128
0.006
48.0
 
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