A new steroidal glycoside from the seeds of Hyoscyamus niger
A new steroidal glycoside hyoscyamoside G (1), together with two known analogues hyoscyamoside E (2) and hyoscyamoside F1 (3), was isolated from the seeds of Hyoscyamus niger. The structure of 1 was established as (22R,24Z)-1α,3β,7β,22,26-pentakishydroxylergost-22-O-β-d-gulcopyranosyl-5,24-diene-26-O-β-d-glucopyranoside, by means of chemical and spectroscopic methods including HRESI-MS, 1D and 2D NMR. In vitro, compound 2 showed cytotoxicity against human lung cancer cell H460 with IC50 value of 66 μg/mL.
Hyoscyamus niger L. (Solanaceae)
A biennial or annual herb found in Asia, northwest China, Europe, and North Africa. Its name is derived from the Anglo-Saxon Hen (chicken) and Bana (murderer), because when fowls eat the seeds of this plant, they become paralyzed and die. All parts of the plant are poisonous, even small amounts cause from dizziness to delirium along with other anticholinergic effects. Seeds are also poisonous to children, rodents, pigs, and fish. Three kinds were known to the Greeks: black, white and yellow. Pliny mentioned four kinds, first with black seeds (H. reticulatus), the second with brownish-gray seeds (H. niger), the third with reddish seeds (H. aureus), and the fourth with white seeds (H. albus), which is medicinally preferred. The white variety was also the only one recommended by Dioscorides and Galen. Henbane is described as intoxicating, narcotic and anodyne. Its uses include a poultice made of leaf juice with barley flour to relieve pain of inflammatory swellings. Seeds increase blood clotting, and are used in a dose of 15 mg in bleeding conditions. Ibn Jazlah did not recommend its use due to its toxicity, and Razi called it Saykarān al-Dūr, which indicates in Arabic a person who is drunk. It is one of the four plants that are used in Ayurveda for the treatment of Parkinson’s disease. It has peculiarly sedative effect beneficial in irritable affections of the lungs, bowels, and genitourinary tract, such as cystitis. Leaves contain about 0.04% alkaloids (mainly hyoscyamine and scopolamine), the glycoside hyoscypicrin, and choline. Withanolide class steroids, lignanamides, rutin, hyoscyamide, β-sitosterol, daucosterol, coumarinolignans, tetrahydrofuranolignan, and steroidal glycosides, have been isolated from seeds. Methanol seed extract produced significant analgesic, anti-inflammatory and antipyretic activities; cleomiscosin A is suggested to play a role in anti-inflammatory effect. Methanol seed extract also exhibited anticonvulsant activity against picrotoxin-induced seizures in mice.
Multiple-dose pharmacokinetics of moxisylyte after oral administration to healthy volunteers.
The pharmacokinetics of moxisylyte in plasma and urine was investigated after oral administration. Twelve subjects were treated orally, twice daily with 240 mg of the drug for 6 days; on day 7, the subjects received a last dose of 240 mg of moxisylyte. Moxisylyte was assayed in plasma and urine by a specific HPLC method with fluorimetric detection. Moxisylyte was absorbed rapidly and changed to its metabolites immediately after drug administration; unchanged moxisylyte was not found in plasma. Two metabolites were found in plasma and urine: conjugated desacetylmoxisylyte (DAM) and the conjugate of desmethylated DAM (MDAM). The pharmacokinetic parameters determined after the first oral administration were not modified on multiple dosing. The apparent elimination half-lives of conjugated DAM and MDAM were 2.3 and 3.5 h, respectively. Elimination of these two metabolites in urine averaged 50 and 10%, respectively.