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Uterine stimulants
Published in Michael J. O’Dowd, The History of Medications for Women, 2020
Sparteine sulfate, first isolated by Stenhouse in 1851, had been employed as a corrective for cardiac irregularities since 1873. Its atropine-like action was investigated by Tamba in 1921 and he deduced that it caused uterine contractions in experimental animals. Kleine of Germany introduced sparteine to obstetrics in 1939 and, although initial studies were disappointing, the drug became popular for the induction of labor (Moir, 1964; Clarke, 1975). Introduced to America in 1958, sparteine became widely used there until the mid-1960s when a number of adverse reports of its safety were published.
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Two prototypical substrates of CYP2D6 are sparteine (Ebner et al. 1995; Eichelbaum et al. 1979, 1986b; Tyndale et al. 1990) and debrisoquine (Boobis et al. 1983; Distlerath and Guengerich 1984; Gonzalez et al. 1988; Woolhouse et al. 1979), which are widely used to determine the phenotype of CYP2D6-mediated metabolism. Sparteine, a class la antiarrhythmic and oxytocic agent (not approved by the Food and Drug Administration [FDA] for human use), is initially identified as a natural quinolizidine alkaloid, which is extracted from Scotch broom (Cytisus scoparius) (Haferkamp 1950).
Catalog of Herbs
Published in James A. Duke, Handbook of Medicinal Herbs, 2018
The alkaloid sparteine was used as a cardiac depressant, cathartic, diuretic, and as an oxytocic to induce labor,17 stimulating uterine contractions.37 Sparteine is occasionally used as a quinidine substitute in stubborn cases of atrial fibrillation. Derivatives like anagyrine, lupanine, and oxysparteine have similar actions. Scoparoside, present largely in the flowers, is diuretic.37 Ornamental, used to hold steep, barren banks, even in the salt spray zone. Wood has been used in veneer for cabinetry; also for thatch. Bark has been used in tanning leather. Before the advent of hops, the tender green tops were used to impart bitterness to beer and make it more intoxicating. Leaves and young tops give a green dye. Seeds have served as a dangerous coffee substitute. Flowers used in hair rinses, supposed to brighten and lighten the hair.29 Moldy blossoms, aged about 10 days in a sealed jar, are pulverized and smoked like marijuana, for relaxation and hallucination or at least color enhancement.37
Role of amino acids at positions 34, 296, and 486 of cytochrome P450 2D6 in the stimulatory and inhibitory effects of psychotropic agents on dopamine formation from p-tyramine
Published in Xenobiotica, 2021
Toshiro Niwa, Juri Arima, Yurina Michihiro
In the present study, we found that Km values for CYP2D6.39-catalysed dopamine formation from p-tyramine increased with increasing concentrations of all investigated psychotropic agents (fluvoxamine, fluoxetine, paroxetine, milnacipran, and fluphenazine). By contrast, kcat values only increased with increasing concentrations of fluvoxamine, fluoxetine, and milnacipran, but not of paroxetine and fluphenazine. These results are similar to those obtained for CYP2D6.1 (Table 2) (Niwa et al. 2018; Niwa and Sugimoto 2019), suggesting that the substitution of serine to threonine at 486 position would be of minor importance for the activation, i.e. the increase in affinity and/or catalytic activity, of CYP2D6 variants. Fluoxetine, fluvoxamine and fluphenazine, but not paroxetine and milnacipran, have a trifluoromethylphenyl group in their chemical structure (Figure 1). However, only fluoxetine, fluvoxamine, and milnacipran-activated CYP2D6-catalysed dopamine formation, suggesting that this functional moiety may not be essential for activation. In contrast, fluoxetine, in addition to paroxetine, was reported to inhibit CYP2D6-catalysed sparteine oxidation in human liver microsomes (Crewe et al. 1992; Liu et al. 2001).
Fragment-based screening with natural products for novel anti-parasitic disease drug discovery
Published in Expert Opinion on Drug Discovery, 2019
The Dictionary of Natural Products database has been computationally divided into 64,650 fragment sized (MW 100–300 Da) and 145,623 natural products with an MW > 300. SPiDER software [27] predicted the targets of 23,340 (36%) of the low MW natural products compared to 31,556 (22% of the 145,623 larger natural products). The concept of target prediction for fragment-like natural products through a comparison with drug-like small molecules was undertaken with sparteine for a prospective experiment. In addition to weakly inhibiting p38α mitogen-activated protein kinase, sparteine was previously shown to bind to the muscarinic and nicotinic receptors [28]. SPiDER predicted these two targets among the top three predictions. The kappa opioid receptor was listed as the second-most-confidently predicted target. Binding and functional assays confirmed the prediction and revealed sparteine as a ligand-efficient fragment for further development (ligand efficiency = 0.30) [29].
Nutrient and Antioxidant Properties of Oils from Bagasses, Agricultural Residues, Medicinal Plants, and Fodders
Published in Journal of the American College of Nutrition, 2019
Agomuo Emmanuel Nnabugwu, Amadi Peter Uchenna
The phytochemical composition of oils from bagasse, agricultural residues, medicinal plants, and forages are shown in Table 4. Sparteine occurred in minute quantities between 0.030 and 0.038 µg/ml, while ribalinidine and lunamarine were in a range of 0 to 51.94 and 0.69 to 22.61 µg/ml, respectively. For the flavonoids, rutin, anthocyanin, and kaempferol were found within the range of 0 to 61.74, 0 to 3.52, and 0 to 87.32 µg/ml, respectively, while in the case of phenols, the catechin and epicatechin were respectively between 0 and 67.67 and 0 and 9.01 µg/ml. CS, SJ, and CC oils contained comparable sapogenin contents, while TB and PM oils contained equivalent phytate contents with GH oil containing the highest phytate levels. The occurrence of oxalates and tannins were found between 0 and 11.37 and 0.03 and 59.51 µg/ml, respectively. From the results, oils from the forage crops collectively produced more alkaloids than other oils, which agrees with the wide reports of immunomodulatory, antioxidant, and anticancer potentials of these fodders (43–45). TB, CS, and SJ oils contained the highest amount of the flavonoids rutin and kaempferol. From the reports of Koçanci et al. (46), SJ and TB oils in this study contain enough rutins to produce anti-inflammatory properties, while the reports of Asgary et al. (47) and Lv-Ying et al. (48) provide enough scientific backing for the investigation of both CS and SJ oils for possible anticancer and anti-HIV potential. Of the phenols evaluated, catechin was more abundant in the oils from the medicinal plants. Catechin is a potent antioxidant (49) that could be connected to the antioxidant potentials of SJ (50) and CS (51). The excessive content of sapogenins, especially in PM, CC, SJ, and CS oils, necessitate more extensive scrutiny in applying these oils as possible medicaments. Further, GH oils produced very high amounts of the antinutrients; phytate and oxalate, implying that the consumption of the GH oil could decrease the bioavailabilities of divalent minerals, as well as potentially cause the formation of oxalate crystals. In addition, the high tannin levels of the oils from the fodders and medicinal plants provides a clue as to astrigent taste of these plants.