Norsecofriedelanes as Spasmolytics, Advances of Structure-Activity Relationships

González-Cortazar, Manasés; Tortoriello, Jaime; Álvarez, Laura

doi:10.1055/s-2005-871224

Cited by 25 publications

(37 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…(Malpighiaceae) is a plant species native to Mexico, where traditional medicine employs it as a tranquilizer for mental disorders [17]. Diverse studies have indicated that the plantʼs methanolic extract possesses anxiolytic activity, which is attributed to a group of compounds that are found chiefly in G. glauca, denominated galphimines A, B, and E, the most active of which is G-B [18][19][20]. G-B is a nor-seco-triterpene compound, and its chemical name is (4R)-trihydroxy-13α-methoxycarbonyl-30-nor-3,4-seco-7α,18β-fridela-1,20-dien-3,24-olide.…”

mentioning

confidence: 99%

Therapeutic Effectiveness of Galphimia glauca vs. Lorazepam in Generalized Anxiety Disorder. A Controlled 15-Week Clinical Trial

et al. 2012

Self Cite

View full text Add to dashboard Cite

tolerability and safety. One hundred ninety-one patients initiated the study with 94 in the experimental group. One hundred four patients concluded the study, 51 of these in the experimental group. Anxiolytic effectiveness, measured as 0 in a negative case and as 1 in a positive case, was assessed 593 times in the experimental group and 631 in the control; the mean effectiveness observed was 0.686 ± 0.019 vs. 0.588 ± 0.019 (repeated-measures ANOVA; p = 0.0003). In the same way, G. glauca-herbal medicinal product diminished the score in the Hamilton anxiety scale to 11.51 ± 8.27 points and lorazepam to 12.40 ± 8.07 points (repeated-measures ANOVA; p = 0.05). The tolerability analysis, which comprised patients who concluded the treatment plus 11 patients who withdrew due to adverse reactions did not show differences between treatments (p = 0.35), nor did therapeutic safety demonstrate differences between groups (p = 0.21). There were no cases of tolerance, intoxication, dependence, or suppression syndrome. We concluded that G. glauca herbal medicinal product, standardized in 0.175 mg of galphimine-B and administered for 15 weeks to patients with generalized anxiety disorder, showed greater anxiolytic effectiveness than that obtained with lorazepam, with high percentages of therapeutic tolerability and safety.

show abstract

mentioning

confidence: 99%

Therapeutic Effectiveness of Galphimia glauca vs. Lorazepam in Generalized Anxiety Disorder. A Controlled 15-Week Clinical Trial

et al. 2012

Self Cite

View full text Add to dashboard Cite

show abstract

“…Extract preparation: For obtaining the galphimines, the ground plant material (aerial parts) (7.26 kg) was macerated with n-hexane (16.8 L, 3 times) for its degreasing and later was submitted to extraction with a mixture of ethyl acetate and methanol (50:50, 3 times) (Gonzalez-Cortazar et al, 2005). The extract obtained (310.8 g, 4.27%) was resuspended in solvents with ascending polarity as follows: n-hexane (600 mL, Merck), chloroform (500 mL, Merck), ethyl acetate (500 mL, Merck) and methanol (500 mL, Merck).…”

Section: Methodsmentioning

confidence: 99%

Pharmacological Interaction between Galphimine-A, a Natural Anxiolytic Compound and Gabaergic Drugs

Montes¹,

Ruiz²,

Ramos³

et al. 2015

International J. of Pharmacology

View full text Add to dashboard Cite

Galphimia glauca is a plant species that has been used in mexican traditional Medicine for the treatment of central nervous system disorders. It was demonstrated that the standardized extract of G. glauca, by means of double-blind, controlled and randomized clinical studies, possesses therapeutic effectiveness in patients with generalized anxiety disorder. In the active extract, nor-secotriterpenes Galphimines, Galphimine-A (G-A) and Galphimine-B (G-B) are prominent for their anxiolytic effect. In the present work, the oral administration of different doses of G-A in ICR male mice submitted to the Elevated Plus Maze (EPM) test was capable of inducing a significant anxiolytic effect, while any of the doses modified the spontaneous motor activity of the mice in the Open Field Test (OFT). The administration of G-A (30 mg kgG 1 , p.o.) in mice inhibited the anxiogenic effect of picrotoxin (PTX, 2 mg kgG 1 , i.p.), but not of bicuculline (BCC, 5 mg kgG 1 , i.p.) and pentylenetetrazole (PTZ, 10 mg kgG 1 , i.p.) in the EPM. The combination of G-A with these drugs was evaluated by means of in vivo extracellular recordings in basolateral amygdala (BLA). A dose-dependent increase of the firing rate on BLA neurons was induced by the administration (i.v.) of different doses of G-A, while diazepam (DZP) decreased the firing rate. The co-administration of G-A with DZP or flumazenil (FMZ) did not modify the effect produced by these drugs on the firing rate. However, the co-administration of G-A modified the effect produced by PTX. The G-A was able to produce an anxiolytic effect when administered at different doses orally in mice, without inducing an associated sedative effect. Electrophysiological recordings showed that the effect produced by G-A is different of that of DZP and suggest that G-A do not interact directly with the GABAergic system (transmission mechanism for the g-aminobutyric acid-GABA), while it was able to modify the effect produced by PTX, BCC and Phaclofen evidencing a different action mechanism.

show abstract

“…The natural galphimines utilized as standards were previously isolated from the aerial parts of the plant . Different concentrations of G‐B (15, 31, 62, 125, and 250 μg/mL), G‐A (12.5, 25, 50, 200, and μg/mL), and G‐E (12.5, 25, 50, and 200 μg/mL) were prepared and injected (50 μL) into the HPLC method to determine the corresponding calibration curves.…”

Section: Methodsmentioning

confidence: 99%

“…The natural galphimines utilized as standards were previously isolated from the aerial parts of the plant [14]. [6].…”

Section: Quantitative Analysis Of G-b and Related Galphiminesmentioning

confidence: 99%

Biosynthesis stimulation of nor‐secotriterpene anxiolytics in cell suspension cultures of Galphimia glaucaCav

Osuna

Tapia

Zamilpa

et al. 2013

Engineering in Life Sciences

Self Cite

View full text Add to dashboard Cite

Galphimia glauca produces compounds denominated galphimines (galphimine‐A, galphimine‐B and galphimine‐E). Due to their important anxiolytic activity, we initiated in vitro cultures of the species with the purpose of developing a biotechnological process for obtaining galphimines. In this work, we stimulated the biosynthesis and excretion of galphimines with two‐phase batch‐type cell suspension cultures of G. glauca. The effect of nutritional variation and the 2,4‐dichlorophenoxy acetic acid added to Murashige & Skoog(MS) culture medium was evaluated. Later, we evaluated the effect of the stimulation with calcium and methyl jasmonate (MeJ). The greatest production of galphimine‐B (3.39 × 10−5 g/L day−1) was obtained on day 40 of kinetics, and induced by a treatment containing concentrations of nitrates and phosphate that are double of those normally used in MS medium, without sucrose but with added 2,4‐dichlorophenoxy acetic acid (4 mg/L). Time of galphimine‐B biosynthesis diminished due to the effect of MeJ in combination with calcium, and induced the excretion (100%) of galphimine‐B (6.35 × 10−5 g/L day−1) into the culture medium. Thus, the use of calcium and MeJ comprises a viable alternative to stimulate the production and excretion of galphimine‐B and galphimine‐A in batch‐type cultures of G. glauca in modified MS medium. Once optimized, the production of the anxiolytic compounds can be scaled up to the industrial level.

show abstract

Norsecofriedelanes as Spasmolytics, Advances of Structure-Activity Relationships

Cited by 25 publications

References 11 publications

Therapeutic Effectiveness of Galphimia glauca vs. Lorazepam in Generalized Anxiety Disorder. A Controlled 15-Week Clinical Trial

Therapeutic Effectiveness of Galphimia glauca vs. Lorazepam in Generalized Anxiety Disorder. A Controlled 15-Week Clinical Trial

Pharmacological Interaction between Galphimine-A, a Natural Anxiolytic Compound and Gabaergic Drugs

Biosynthesis stimulation of nor‐secotriterpene anxiolytics in cell suspension cultures of Galphimia glaucaCav

Contact Info

Product

Resources

About