Abstract:Course treatment with diterpene alkaloids of Aconitum baicalense in mice reduced the time of immobilization in the tail suspension test and produced an antiexudative effect in mouse model of serotonin-induced edema. In the open field test, application of alkaloids did not change the total motor activity, orientation and exploratory behavior, and emotional reactions of animals. Experimental data suggest that diterpene alkaloids of Aconitum baicalensis exhibit antidepressant properties, possibly due to modulatio… Show more
“…Alkaloids are endowed with diverse biological activities, being already used in therapy as pharmacological tools. Among the reported biological effects (Awaad et al 2007), antidepressant (Nesterova et al 2011), antimicrobial (Karou et al 2006), antiemetic (Bulbul et al 2013), and anti-inflammatory (Vijayalakshmi et al 2011) properties. Nonetheless, there are also reports of toxic effects to humans; thus, the use of different experimental models to understand the exact mechanism of the molecules under study is necessary, in order to have the real knowledge of their effect (Nascimento et al 2015).…”
Background: The purpose of this study is to determine the effect of in vitro anticancer activity and cytotoxicity of 13 Papaver alkaloids (amurine, armepavine, berberine, isocorydine, isothebaine, macranthine, mecambrine, mecambridine, narkotine, orientalidine, oripavine, salutaridine and thebaine) against the human cervical cancer cell line (HeLa) compared to the normal African green monkey kidney epithelial cell line (Vero) using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.
Materials and Methods:The Vero and HeLa cell lines were treated with various concentrations (1-300 μg/mL) of alkaloids for 48 h. Values for cytotoxicity measured by MTT assay were expressed as the concentration that causes a 50% decrease in cell viability (IC 50 ) (μg/mL). Results: Berberine and macranthine were the most active alkaloids. Salutaridine exhibited no cytotoxic activity against two types of cell lines. Dose-dependent studies presented IC 50 of 12.08 μg/mL and IC 50 of 71.14 μg/mL for berberine and IC 50 of 24.16 μg/mL and IC 50 of >300 μg/mL for macranthine on the HeLa cells and the Vero cells respectively.
Conclusion:The degree of selectivity of the compounds can be expressed by its Selectivity Index (SI) value. High SI value (>2) of a compound gives a selective toxicity towards cancer cells (SI = IC 50 for normal cells/IC 50 for cancer cells). Two alkaloids showed significant SI values, which are 12.42 for macranthine and 5.89 for berberine. Hence, macranthine and berberine display potential to be further exploited in the discovery and development of new anticancer agents.
“…Alkaloids are endowed with diverse biological activities, being already used in therapy as pharmacological tools. Among the reported biological effects (Awaad et al 2007), antidepressant (Nesterova et al 2011), antimicrobial (Karou et al 2006), antiemetic (Bulbul et al 2013), and anti-inflammatory (Vijayalakshmi et al 2011) properties. Nonetheless, there are also reports of toxic effects to humans; thus, the use of different experimental models to understand the exact mechanism of the molecules under study is necessary, in order to have the real knowledge of their effect (Nascimento et al 2015).…”
Background: The purpose of this study is to determine the effect of in vitro anticancer activity and cytotoxicity of 13 Papaver alkaloids (amurine, armepavine, berberine, isocorydine, isothebaine, macranthine, mecambrine, mecambridine, narkotine, orientalidine, oripavine, salutaridine and thebaine) against the human cervical cancer cell line (HeLa) compared to the normal African green monkey kidney epithelial cell line (Vero) using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.
Materials and Methods:The Vero and HeLa cell lines were treated with various concentrations (1-300 μg/mL) of alkaloids for 48 h. Values for cytotoxicity measured by MTT assay were expressed as the concentration that causes a 50% decrease in cell viability (IC 50 ) (μg/mL). Results: Berberine and macranthine were the most active alkaloids. Salutaridine exhibited no cytotoxic activity against two types of cell lines. Dose-dependent studies presented IC 50 of 12.08 μg/mL and IC 50 of 71.14 μg/mL for berberine and IC 50 of 24.16 μg/mL and IC 50 of >300 μg/mL for macranthine on the HeLa cells and the Vero cells respectively.
Conclusion:The degree of selectivity of the compounds can be expressed by its Selectivity Index (SI) value. High SI value (>2) of a compound gives a selective toxicity towards cancer cells (SI = IC 50 for normal cells/IC 50 for cancer cells). Two alkaloids showed significant SI values, which are 12.42 for macranthine and 5.89 for berberine. Hence, macranthine and berberine display potential to be further exploited in the discovery and development of new anticancer agents.
“…Since pain induced by acetic acid is primarily mediated by endogenous kinins forming under conditions of low pH and to other algogenic compounds (histamine, serotonin, acetylcholine, prostaglandins [13], the pain-relieving effects of the studied alkaloids were most likely due to inhibition of these algogenic compounds. Our previous studies confi rmed this hypothesis: treatment of animals with Baikal aconite diterpene alkaloids prevented the development of edema caused by injection of arachidonic acid, histamine, and serotonin [5,11]. In modeled adjuvant disease, the analgesic effects of Aconitum baikalensis alkaloids were observed on days 6, 7, and 8 (Table 1).…”
Section: Resultsmentioning
confidence: 68%
“…Our studies detected various physiological activities in diterpene alkaloids extracted from Aconitum baikalensis: stress-protective [8], antimetastatic [7], regeneratory [12,14], antidepressant [11], anti-infl ammatory [3,5,6], antihypoxic, antipyretic [4].…”
We compared analgesic activities of individual alkaloids extracted from Baikal aconite (Aconitum baikalensis): napelline, hypaconitine, songorine, mesaconitine, 12-epinapelline N-oxide. The detected analgesic activity was comparable to that of sodium metamizole. The mechanisms of analgesia were different in diterpene alkaloids of different structure. The antinociceptive effect of atisine alkaloids (12-epinapelline N-oxide, songorine) was naloxonedependent and realized via opioid receptor modulation.
“…Locomotor activity was studied using an open-field test which was performed on mice using a slightly modified method (18,19). Briefly, the locomotor activity of the mice was measured using a box (30×30×15 cm) with the floor divided into 25 squares illuminated with light from the ceiling.…”
Peony is often used in Chinese herbal medicine for the treatment of depression-like disorders. Our previous studies have demonstrated that the total glycosides of peony exert antidepressant-like effects in animal models. Paeoniflorin is the main active glycoside of peony. The aim of this study was to evaluate the antidepressant-like effects of paeoniflorin in mice, as well as its active mechanisms. The results revealed that intraperitoneally injected paeoniflorin significantly reduced the duration of immobility in forced swimming and tail suspension tests. The doses that affected the immobility response did not affect locomotor activity. Furthermore, paeoniflorin antagonized reserpine-induced ptosis, akinesia and hypothermia. Paeoniflorin also significantly increased the levels of serotonin (5-HT) and its metabolite 5-hydroxyindoleacetic acid (5-HIAA) in the hippocampus. These results suggest that the upregulation of serotonergic systems may be an important mechanism for the antidepressant-like effects of paeoniflorin in mice.
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