Diester type diterpenoid alkaloid with analgesic effect as well as preparation method and application of diester type diterpenoid alkaloid
A diterpene alkaloid and diester-type technology, which is applied in the field of diester-type diterpene alkaloid preparation, can solve problems such as slow progress, and achieve significant economic benefits and huge clinical application value
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Embodiment 1
[0024] Embodiment 1, the LD50 of the aconitine A of the diester type diterpene alkaloid is obtained as follows:
[0025] (1) Grouping of animals: Take 80 Kunming mice, half male and half female, and divide them into 8 groups. kg, 7.14mg / kg, 10.10mg / kg, 14.58mg / kg, 20mg / kg groups, 10 rats in each group;
[0026] (2) Experimental method: The equal volumes of different concentration and dosage groups were given by intragastric administration once, and the vehicle control group was given normal saline. The acute toxic reaction and death of animals in each group were observed after administration for 14 consecutive days. Animals that died during the observation period and animals that were sacrificed after the observation period were dissected, and the volume, color, and texture of various tissues and organs were checked with naked eyes for abnormalities. According to the death rate of animals in each group, the LD50 of aconitine A was calculated by Bliss method;
[0027] (3) Ca...
Embodiment 2
[0028] Example 2, the analgesic effect of the diester-type diterpene alkaloid Aconitine A (VA) on the formalin-induced pain model in rats was specifically verified by the following process:
[0029] (1) Animal grouping: 18 Wistar male rats were randomly divided into 3 groups, vehicle control group (Vehicle), aconitine A group (BAA), and aconitine A (VA) group, 6 rats in each group;
[0030](2) Model construction: Administered by intraperitoneal injection, the dose of BAA group was 59 μg / kg, the dose of VA group was 21 μg / kg, and the vehicle group was given the configuration vehicle of aconitine A (VA). 50 μl of 5% formalin solution was subcutaneously injected into the right foot of the rat; immediately after the injection, the rat was placed in a plexiglass box, and the rats were recorded at 0, 10, 20, 30, 40, The number of pain behaviors at 50, 60, 70, 80 and 90 minutes; the two-phase pain after injection of 5% formalin can be divided into acute phase (0-10min phase I) and ch...
Embodiment 3
[0032] Example 3, the analgesic effect of the aconitine A (VA) in the neuropathic pain model caused by nerve ligation in rats, specifically verified by the following process:
[0033] (1) Grouping of animals: Wistar male rats, 24 animals with mechanical pain threshold <10 g were selected to be included in the experiment on the 14th day after nerve ligation, and were randomly divided into 4 groups, vehicle control group (Vehicle) and aconitin group (BAA), aconitine A (VA) group and morphine (Morphine)+VA group, 6 rats in each group;
[0034] (2) Model construction: Except for morphine administered by subcutaneous injection, other compounds and vehicles were administered by intraperitoneal injection, the dose of BAA group was 21 μg / kg, the dose of VA group was 15 μg / kg, and the dose of Morphine+VA group was 7 mg / kg, injected once a day, the vehicle group was given the preparation vehicle of aconitine A (VA), and the other drugs except morphine were injected twice a day, with an...
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