Research on Semen Hyoscyami

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[b:6e87b50ffc]Semen Hyoscyami[/b:6e87b50ffc]

Pin Yin：Tian Xian Zi
Common Name：Henbane Seed
Latin Name：Semen Hyoscyami

Chemical Composition： The material contains 0.06% to 0.2% of alkaloid among most of which are Hyoscyamine, atropine, and anisodamine, and 25% of fatty oil and sterol. [1-3] The fatty acid contained in the material includes myristic acid (0.3%), palmitic acid (6.5%), stearic acid (1.6%), oleic acid (35.2%), and linoleic acid (56.4%).

Pharmacological Effects:
1. The effect to the glands and smooth muscles: It has remarkable inhibiting effect on the secretary functions and could also relieve the gastrointestinal spasm, ureteral spasm, irritation of the bladder, and pyloric spasm. To treat gastric and duodenal ulcer, it could be combined with antacids.
2. The effect to the cardiovascular system: The atropine could release the inhibition of the vagus nerve to the heart so as to speed up the heart rate. Either the abdominal injection 5 or 10 mg/kg or intravenous injection 2 or 4 mg/kg, scopolamine has certain antagonizing effect for the disordered heart rate of mice induced by aconitine, ouabin, BaCl2, CaCl2, adrenalin, chloroform, and Ach-CaCl2. [5] 0.4 ml or 0.8 ml of Tiaowei II (2 ml for each ampule, containing 0.6 mg of scopolamine and 0.2 mg of atropine) was injected into the abdominal cavity of mice, the result by means of the detection with radioactive 86 Rb showed that the effect of Tiaowei II for influencing the nutritional myocardic blood flow of mice is just a little slower than that of persantine and its peak value is a little lower, however the lasting time of the effect is longer. The dosage increase of Tiaowei II could potentiate the intensity of the effect but has nothing to do with its lasting time.
3. The effect to the central nerve system: The therapeutic dosage could excite the vagus and respiratory center but the scopolamine acts as the sedative effect. “The radioactive immune determination found that the abdominal injection of both atropine and scopolamine, each of 25 mg/kg, could make the content of acetylcholine in the cerebral cortex of rats remarkably reduced and the reduction by the two was respectively as 46% and 42%. Probably this is related to the fact that they can block the presynaptic receptor M, thus can enable the release of the acetylcholine to be increased. While atropine block the inhibiting receptor M2, the functions of receptor M1 will be predominant and acts as the excitation, and at this moment the release of acetylcholine increases, stimulating the receptor M1 and intensifying its excitation. The scopolamine could block the exciting receptor M1, enabling the receptor M2 to be predominant, so there will be manifestations of inhibition. If both of them are overdosed, there may appear the bi-directional functions and as the result patients may have the manifestations such as unconsciousness, delirium, restlessness, contraction of limbs, and convulsion.”
4. The antiplatelet-aggregation effect: “Born” and “Brien” methods were performed for the platelet aggregation test and it was found that atropine of the concentration of 10-6-10-3 mol/L has the effect of counteracting the platelet-aggregation of human blood induced by adenosine diphosphate (ADP), adrenalin, and the endotoxin of Bacillus coli, and there appears the dosage-dependence. Besides, its antiplatelet-aggregation effect becomes lessened and intensified in pace with the rise and fall of the extracellular calcium ion concentration, suggesting the antiplatelet-aggregation effect of atropine may be in relations with its calcium-antagonistic effect.
5. The effect to the bio-membrane: The differential scanning calorimetry was used to compare the influence of several agents of Hyoscyamus on the phase transition of acid phospholipid (DPPA) membrane and it was proved that they did change the phase status of the membrane.
6. The other effect: Atropine has the other effects e.g. mydriasis, elevating the intraocular pressure, and regulating the paralysis.

Toxicity
To take the scopolamine up to the clinical therapeutic dosage for adults (approximately 0.5μg/1 ml) as the initial dosage and to make altogether 6 groups of crescendo dosage (i.e. 0.5、1.0、2.0、5.0、10、and 20μg/1 ml), the agent acted directly on the culture fluid of the blood lymphatic cells in the peripheral veins of the healthy human subjects, the result showed that the chromosomal aberration rate and the sister chromatid exchange (SCE) rate are much higher that those of the control group. From the 6th day of pregnancy of mice, the scopolamine was given via abdominal injection, respectively 4.6 and 5.9 mg/kg daily until the 16th day of the pregnancy, as the result the teratism of the fetus mice is respectively 3.8% and 8.2%, much higher figures than those in the control group. It was demonstrated that scopolamine has the mutagenic and teratogenic effect. When the hyoscyamine poisoning occurs, the chief pathology process is that the exciting effect to the central nerve system turns to the inhibition, so it could block the M-choline reacting system, antagonizing the effect of acetylcholine. When the brain is stimulated, there could appear the manifestations of delirium and involuntary cry and laugh; when the spinal cord is stimulated, there could be contraction of limbs and convulsion; when the gland secretion is inhibited, there may be dryness in mouth, mydriasis, and dull or even lost light reflex; when the cardiovagus nerve becomes paralyzed, there will be tachycardia, rapid pulse; and when the vasodilatory center is excited, there will be flushed skin.

HPLC
The reverse ion-pair HPLC method was used to identify the content of the hyoscyamine and scopolamine in Semen Hyoscyami. The linear range of the sample size and that of the integral value of the peak area were respectively 0.2445-0.7332μg，r=0.9995 and 0.1864-0.5592μg，r=0.9999；the average rate of recovery was 98.82%，RSD=3.41%(ｎ=5) and 97.86%，RSD＝1.85% (ｎ=5).

Dosage: 0.2 to 1.2 grams for the oral administration with decoction; and 0.06 to 0.6 grams is taken as the fine powder. Externally, it could be used by means of grinding it into powder for applying on the local area, decoction for washing, and burning the fire for fumigation.

Precautions: Since this material is greatly poisonous, so it must be taken per os with caution. It can never be administered for overdose, neither taken successively. It is contraindicated to patients of heart disease and glaucoma, likewise to gravida. Clinically there are reports about the Semen Hyoscyami poisoning taken by mistake.

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Posted: Mon Jan 24, 2005 5:33 pm    Post subject: Research on Semen Hyoscyami