Pacific Nights™

1. Ursolic acid mediates the vasorelaxant activity of Lepechinia caulescens via NO release in isolated rat thoracic aorta.
Aguirre-Crespo F, Vergara-Galicia J, Villalobos-Molina R, Javier Lopez-Guerrero J, Navarrete-Vazquez G, Estrada-Soto S. Facultad de Farmacia, Universidad Autonoma del Estado de Morelos, Avenida Universidad 1001, Colonia Chamilpa, 62210, Cuernavaca, Morelos, Mexico.
PMID: 16630635 [PubMed - in process]

2. Pharmacologic and toxicologic effects of two Maytenus species in laboratory animals.
Oliveira MG; Monteiro MG; Macaúúbas C; Barbosa VP; Carlini EA
J Ethnopharmacol, 34: 1, 1991 Aug, 29-41

3. In vitro Effects of Two Extracts and Two Pure Alkaloid Preparations of Uncaria tomentosa on Peripheral Blood Mononuclear Cells.
Winkler C, Wirleitner B, Schroecksnadel K, Schennach H, Mur E, Fuchs D.
Institute of Medical Chemistry and Biochemistry, University of Innsbruck, Innsbruck, Austria.
Planta Med. 2004 Mar;70(3):205-10.
PMID: 15114496 [PubMed - in process]

4. Effect of acute treatment with a water-alcohol extract of Erythrina mulungu on anxiety-related responses in rats.
Onusic GM, Nogueira RL, Pereira AM, Viana MB.
PMID: 11960198 [PubMed - indexed for MEDLINE]

5. Antinociceptive activities of the hydroalcoholic extracts from Erythrina velutina and Erythrina mulungu in mice.
Vasconcelos SM, Reboucas Oliveira G, Mohana de Carvalho M, Rodrigues AC, Rocha Silveira E, Maria Franca Fonteles M, Florenco Sousa FC, Barros Viana GS.

6. Central activity of hydroalcoholic extracts from Erythrina velutina and Erythrina mulungu in mice.
Vasconcelos SM, Macedo DS, de Melo CT, Paiva Monteiro A, Rodrigues AC, Silveira ER, Cunha GM, Sousa FC, Viana

7. Effects of chronic treatment with a water-alcohol extract from Erythrina mulungu on anxiety related responses in rats.
Onusic GM, Nogueira RL, Pereira AM, Flausino Junior OA, Viana Mde B.
Biol Pharm Bull. 2003 Nov;26(11):1538-42.
PMID: 14600397 [PubMed - in process]

8. Analgesic and sedative activities of lactucin and some lactucin-like guaianolides in mice.
Wesolowska A, Nikiforuk A, Michalska K, Kisiel W, Chojnacka-Wojcik E.
PMID: 16621374 [PubMed - in process]

9. Research on the preparation of lactucin and lactucopicrin from Lactuca virosa plants. On the enzymatic and non-enzymatic oxidation of therapeutically active plant substances.
[Article in German] SCHENCK G, LOTH H, REUBERT W.
PMID: 13747469 [PubMed - indexed for MEDLINE]

Salvinol™ ~ Lepechinia meyenii

1. Ursolic acid mediates the vasorelaxant activity of Lepechinia caulescens via NO release in isolated rat thoracic aorta.
Aguirre-Crespo F, Vergara-Galicia J, Villalobos-Molina R, Javier Lopez-Guerrero J, Navarrete-Vazquez G,
Estrada-Soto S. Facultad de Farmacia, Universidad Autonoma del Estado de Morelos, Avenida Universidad 1001, Colonia Chamilpa, 62210, Cuernavaca, Morelos, Mexico.
We have determined that the methanolic extract of L. caulescens (MELc) produced a significant vasodilator effect in a concentration-dependent and endothelium-dependent manner. This relaxation was blocked by N(omega)-nitro-l-arginine methylester (l-NAME), indicating that MELc vasodilator properties are endothelium mediated due to liberation of nitric oxide (NO). In this paper we aimed to corroborate its mode of action. MELc effects on noradrenaline (NA)-induced contraction in isolated rat aortic thoracic rings with endothelium (+E), in the presence of atropine (0.1 muM) and 1-H-[1,2,4]-oxadiazolo-[4,3a]-quinoxalin-1-one (ODQ, 1 muM) were conducted. MELc relaxation curve was significantly shifted to the right in the presence of ODQ and atropine, thus confirming that its mode of action is related with activation of nitric oxide synthase (NOS) and the consequent increment in NO formation. Bio-guided study of MELc allowed the isolation of ursolic acid (UA, 50 mg) and ursolic-oleanolic acids mixture [UA/OA (7:3), 450 mg]. The relaxant effect of UA (0.038-110 muM) was evaluated in functional experiments. UA induced a significant relaxation in a concentration- and endothelium-dependent manner (IC(50)=44.15 muM) and did not produce a vasorelaxant effect on ontraction evoked by KCl (80 mM). In addition, NA-induced contraction was significantly displaced to the right by UA (30 muM). In order to determine its mode of action, UA-induced relaxant effect was evaluated in the presence of atropine (0.1 muM), indomethacin (10 muM), l-NAME (100 muM) and ODQ (1 muM). Relaxation was blocked by l-NAME and ODQ. On the other hand, UA (3 muM) provoked a significant displacement to the left in the relaxation curve induced by sodium nitroprusside (SNP, 0.32 nM to 0.1 muM), but it was not significant in the presence of Carbamoyl choline (carbachol, 1 nM to 10 muM). These results indicate that UA-mediated relaxation is endothelium dependent, probably due to NO release, and the consequent activation of vascular smooth muscle soluble guanylate cyclase (sGC), a signal transduction enzyme that forms the second messenger cGMP.
Life Sci. 2006 Aug. 8; 79(11): 1062-8.Epub 2006 April 21
PMID: 16630635 [PubMed - in process]

2. Pharmacologic and toxicologic effects of two Maytenus species in laboratory animals.
Oliveira MG; Monteiro MG; Macaúúbas C; Barbosa VP; Carlini EA
Leaves of Maytenus species are used in the popular medicine of Brazil for their reported antacid and antiulcerogenic activity. The present work examined the effects of a boiling water extract of equal parts of M. aquifolium and M. ilicifolia leaves on acute administration in rats and mice, in an attempt to detect any general depressant, hypnotic, anticonvulsant and analgesic effects. General depressant and hypnotic effects were seen only after intraperitoneal administration. After chronic administration, the overall behavior of animals did not change and they continued to gain weight at the same rate as controls. Several biochemical and hematological parameters as well as pathological examination of different organs did not show any significant alterations after 3 months of treatment. A search for the potential effects of the extract on the fertility of female and male rats and on the course of pregnancy as well as a search for potential teratogenic effects did not reveal any significant differences from controls. Taken together, the results indicate that these Maytenus species may be safe for human use and deserve further investigation.
J Ethnopharmacol, 34: 1, 1991 Aug, 29-41

3. Chuchuhuasha - a drug used in folk medicine in the Amazonian and Andean areas. A chemical study of Maytenus laevis.
Gonzalez JG; delle Monache G; delle Monache F; Marini-Bettol GB
In the high Amazonian basin a plant named chuchuasha, (or chuchuaso) is used in traditional medicine for several purposes in the form of an alcoholic extract. This plant, a Maytenus species, most probably Maytenus laevis, grows in the subandean region of the Amazonian basin (Peru, Ecuador, Colombia). Antitumor and anti-inflammatory properties were recently attributed to the extracts of the root bark of the plant. The composition of the extract of M. laevis from the Putumayo area of Colombia was studied in order to establish the active principle responsible for these activities. The presence of phenoldienones (tingenone, 22-hydroxytingenone), a catechin (4’-methyl-(--epigallocatechin) and proanthocyanidins (Ouratea-proanthocyanidins A and B) was established. The biological activities of these compounds confirm the properties of the extracts of the plant claimed by traditional medicine.
J Ethnopharmacol, 5: 1, 1982 Jan, 73-7

4. In vitro Effects of Two Extracts and Two Pure Alkaloid Preparations of Uncaria tomentosa on Peripheral Blood Mononuclear Cells.
Winkler C, Wirleitner B, Schroecksnadel K, Schennach H, Mur E, Fuchs D.
Institute of Medical Chemistry and Biochemistry, University of Innsbruck, Innsbruck, Austria.
In the traditional Peruvian medicine, hot aqueous extracts of Uncaria tomentosa have been used for the treatment of a wide range of health problems, particularly digestive complaints and arthritis. Some of the beneficial effects observed in patients suggest an immunomodulatory capacity of Uncaria tomentosa extracts. In this study, the effects of two extracts and two mixtures of tetracyclic and pentacyclic oxindole alkaloids of Uncaria tomentosa were investigated in freshly isolated human peripheral blood mononuclear cells (PBMC) stimulated with the mitogens phytohaemagglutinin (PHA) and concanavalin A (Con A) in vitro. Neopterin production and tryptophan degradation were monitored in culture supernatants to determine the effects of the test substances on immunobiochemical pathways induced by interferon-gamma. Compared to unstimulated cells PHA and Con A increased the production of neopterin and degradation of tryptophan (p < 0.01). HCl and ethanol extracts and mixtures of alkaloids of Uncaria tomentosa inhibited both effects in a dose-dependent manner, the lowest effective concentrations of the extracts were 500 - 1000 microg/mL and of the alkaloid mixtures 100 - 175 microg/mL (p < 0.05 and < 0.01). With the highest concentrations of extracts and mixtures complete suppression of mitogen-induced neopterin production and tryptophan degradation was observed. These data demonstrate that Uncaria tomentosa extracts and mixtures of alkaloids modulate the immunobiochemical pathways induced by interferon-gamma. The findings imply a potential application of the extracts as immunoregulators and would be in line with observations in patients using these extracts. Abbreviations. Con A:concanavalin A EDTA:ethylenediaminetetraacetic acid, Titriplex III IDO:indoleamine (2,3)-dioxygenase IFN-gamma:interferon-gamma kyn:kynurenine MTT:3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide PBMC:peripheral blood mononuclear cells PHA:phytohaemagglutinin POA:pentacyclic oxindole alkaloids ROS:reactive oxygen species TOA:tetracyclic oxindole alkaloids trp:tryptophan
Planta Med. 2004 Mar;70(3):205-10.
PMID: 15114496 [PubMed - in process]

5. Effect of acute treatment with a water-alcohol extract of Erythrina mulungu on anxiety-related responses in rats.
Onusic GM, Nogueira RL, Pereira AM, Viana MB.
Laboratorio de Psicofarmacologia, Faculdade de Filosofia, Ciencias e Letras de Ribeirao Preto, Universidade de Sao Paulo, Ribeirao Preto, SP, Brasil.
We investigated the effect of acute oral treatment with a water-alcohol extract of the inflorescence of Erythrina mulungu (EM, Leguminosae-Papilionaceae) (100, 200 and 400 mg/kg) on rats submitted to different anxiety models: the elevated T-maze (for inhibitory avoidance and escape measurements), the light/dark transition, and the cat odor test. These models were selected for their presumed capacity to demonstrate specific subtypes of anxiety disorders as recognized in clinical practice. Treatment with 200 mg/kg EM impaired avoidance latencies (avoidance 1 - 200 mg/kg EM: 18 +/- 7 s, control group: 40 +/- 9 s; avoidance 2 - 200 mg/kg EM: 15 +/- 4 s, control group: 110.33 +/- 38 s) in a way similar to the reference drug diazepam (avoidance 1: 3 +/- 0.79 s; avoidance 2: 3 +/- 0.76 s), without altering escape. Additionally, the same treatments increased the number of transitions (200 mg/kg EM: 6.33 +/- 0.90, diazepam: 10 +/- 1.54, control group: 2.78 +/- 0.60) between the two compartments and the time spent in the lighted compartment in the light/dark transition model (200 mg/kg EM: 39 +/- 7 s; diazepam: 61 +/- 9 s; control group: 14 +/- 4 s). The dose of 400 mg/kg EM also increased this last measurement (38 +/- 8 s). These results were not due to motor alterations since no significant effects were detected in the number of crossings or rearings in the arena. Furthermore, neither EM nor diazepam altered the behavioral responses of rats to a cloth impregnated with cat odor. These observations suggest that EM exerts anxiolytic-like effects on a specific subset of defensive behaviors, particularly those that have been shown to be sensitive to low doses of benzodiazepines.
Braz J Med Biol Res. 2002 Apr;35(4):473-7.
PMID: 11960198 [PubMed - indexed for MEDLINE]

6. Antinociceptive activities of the hydroalcoholic extracts from Erythrina velutina and Erythrina mulungu in mice.
Vasconcelos SM, Reboucas Oliveira G, Mohana de Carvalho M, Rodrigues AC, Rocha Silveira E, Maria Franca Fonteles M, Florenco Sousa FC, Barros Viana GS.
Department of Physiology and Pharmacology, Federal University of Ceara, Brazil.
This work studied the antinociceptive effects of the hydroalcoholic extracts (HAEs) from Erythrina velutina (Ev) and Erythrina mulungu (Em) in three experimental models of nociception in mice. The extract was administered intraperitoneally to female mice at the doses of 200 and 400 mg/kg. Inhibitions of abdominal contractions were observed with the doses of 200 (88.6%; 86.8%) and 400 (95.5%; 83.5%) mg/kg of E. velutina and E. mulungu, respectively, as compared to controls. E. velutina and E. mulungu, at both doses, reduced the nociception produced by formalin in the 1st and 2nd phases and this effect was not reversed by the pretreatment with naloxone. In the hot plate test an increase of the reaction time was observed only at 60 (Ev=18.0+/-2.2; Em=20.8+/-2.52) and 90 min (Ev=20.4+/-1.71; Em=23.7+/-2.32) after the treatment with E. velutina and E. mulungu at the dose of 400 mg/kg as compared to controls (T60=11.1+/-0.74; T90=11.9+/-0.86). This effect was not reversed by naloxone. We conclude that E. velutina and E. mulungu presents antinociceptive effects, which are independent of the opioid system.
Biol Pharm Bull. 2003 Jul;26(7):946-9
PMID: 12843615 [PubMed - indexed for MEDLINE]

7. Central activity of hydroalcoholic extracts from Erythrina velutina and Erythrina mulungu in mice.
Vasconcelos SM, Macedo DS, de Melo CT, Paiva Monteiro A, Rodrigues AC, Silveira ER, Cunha GM, Sousa FC, Viana GS.Department of Physiology and Pharmacology, Federal University of Ceara, Rua Cel. Nunes de Melo 1127, CEP 60431-270, Fortaleza, Brazil. claussil@bol.com.br
This work studied the central behavioural effects of hydroalcoholic extracts from the stem bark of Erythrina velutina and Erythrina mulungu on the elevated plus maze, open field, and rota rod tests in mice. These medicinal plants belong to the Fabaceae family and are popularly used in Brazil for their effects on the central nervous system. Single doses of the extracts were administered orally (200, 400 or 800 mg kg(-1)) or intraperitoneally (200 or 400 mg kg(-1)) to female mice. A reduction of the locomotor activity was observed in the open field test with both hydroalcoholic extracts after intraperitoneal treatment with all doses, but only with the highest dose after oral administration. In addition, oral and intraperitoneal administration of the extracts decreased the incidence of rearing and grooming. Decreases in the number of entries in the open (NEOA) and closed (NECA) arms of the elevated plus maze were observed after the administration of the highest dose (800 mg kg(-1), p.o.) of both hydroalcoholic extracts, and this effect may be due to the decrease in locomotor activity. These hydroalcoholic extracts failed to affect the motor coordination in the rota rod test. In conclusion, we showed that the hydroalcoholic extracts of E. velutina and E. mulungu have depressant effects on the central nervous system, which, at least partially, corroborates the popular use of these species as tranquilizers in Brazilian popular medicine.
J Pharm Pharmacol. 2004 Mar;56(3):389-93.
PMID: 15025865 [PubMed - in process]

8. Effects of chronic treatment with a water-alcohol extract from Erythrina mulungu on anxiety related responses in rats.
Onusic GM, Nogueira RL, Pereira AM, Flausino Junior OA, Viana Mde B.
Laboratory of Psychopharmacology, FFCLRP, University of Sao Paulo, Sao Paulo, Brazil.
We investigated the effects of chronic oral treatment with a water-alcohol extract from the inflorescence of Erythrina mulungu (Leguminosae-Papilionaceae) (EM, 50, 100, 200 mg/kg) in rats submitted to different anxiety models: the elevated T-maze (ETM, for inhibitory avoidance and escape measurements), the light/dark transition, and the cat odor test. These models were selected for their capacity to elicit specific subtypes of anxiety disorders as recognized in clinical practice. Treatment with EM impaired inhibitory avoidance latencies in a way similar to the reference drug, diazepam (DZP). Additionally, both EM and DZP increased the number of transitions and the time spent in the lighted compartment of the light/dark transition model. Furthermore, neither EM nor DZP altered behavioral responses of rats to a cloth impregnated with cat odor. In contrast to DZP, however, EM also altered ETM one-way escape. These results were not due to motor alterations since no significant effects were detected in the number of crossings or rearings in the arena. The present observations suggest that chronic EM exerts anxiolytic-like effects in defensive behaviors related to generalized anxiety and panic disorder. Although alkaloids appear to be one of the main constituents of EM, the possible mechanisms through which the extract exerts its anxiolytic action should be further investigated.
Biol Pharm Bull. 2003 Nov;26(11):1538-42.
PMID: 14600397 [PubMed - in process]

9. Amazon Medicines of Brazil, Columbia, Bolivia, Peru and Ecuador
by J. River Jones.
Amazon Therapeutic Laboratories, unpublished field journals 1994-2005. 46 pg 38

10. Analgesic and sedative activities of lactucin and some lactucin-like guaianolides in mice.
Wesolowska A, Nikiforuk A, Michalska K, Kisiel W, Chojnacka-Wojcik E.
Department of New Drugs Research, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Str., 31-343 Krakow, Poland.
Lactucin (1) and its derivatives lactucopicrin (2) and 11beta,13-dihydrolactucin (3), which are characteristic bitter sesquiterpene lactones of Lactuca virosa and Cichorium intybus, were evaluated for analgesic and sedative properties in mice. The compounds showed analgesic effects at doses of 15 and 30 mg/kg in the hot plate test similar to that of ibuprofen, used as a standard drug, at a dose of 30 mg/kg. The analgesic activities of the compounds at a dose of 30 mg/kg in the tail-flick test were comparable to that of ibuprofen given at a dose of 60 mg/kg. Lactucopicrin appeared to be the most potent analgesic of the three tested compounds. Lactucin and lactucopicrin, but not 11beta,13-dihydrolactucin, also showed sedative properties in the spontaneous locomotor activity test.
PMID: 16621374 [PubMed - in process]

11. Research on the preparation of lactucin and lactucopicrin from Lactuca virosa plants. On the enzymatic and non-enzymatic oxidation of therapeutically active plant substances.
[Article in German] SCHENCK G, LOTH H, REUBERT W.
PMID: 13747469 [PubMed - indexed for MEDLINE]