A Complete Review of Mexican Plants with Teratogenic Effects.

In Mexico, the use of medicinal plants is the first alternative to treat the diseases of the most economically vulnerable population. Therefore, this review offers a list of Mexican plants (native and introduced) with teratogenic effects and describes their main alterations, teratogenic compounds, and the models and doses used. Our results identified 63 species with teratogenic effects (19 native) and the main alterations that were found in the nervous system and axial skeleton, induced by compounds such as alkaloids, terpenes, and flavonoids. Additionally, a group of hallucinogenic plants rich in alkaloids employed by indigenous groups without teratogenic studies were identified. Our conclusion shows that several of the identified species are employed in Mexican traditional medicine and that the teratogenic species most distributed in Mexico are Astragalus mollissimus, Astragalus lentiginosus, and Lupinus formosus. Considering the total number of plants in Mexico (≈29,000 total vascular plants), to date, existing research in the area shows that Mexican plants with teratogenic effects represent ≈0.22% of the total species of these in the country. This indicates a clear need to intensify the evaluation of the teratogenic effect of Mexican plants.

Myristic acid reduces skin inflammation and nociception.

This study evaluated the inhibitory effect of myristic acid (MA) on models of inflammation and nociception. The in vitro anti-inflammatory activities of MA were assessed on LPS-stimulated macrophages, membrane stabilization assay, and inhibition of protein denaturation, whereas the inhibitory activity of MA on in vivo inflammation was assessed on TPA-induced ear edema using acute and chronic assays in mice. The inhibitory effect of MA on nociception was assessed using three in vivo models. MA exerted in vitro anti-inflammatory activity by the increase (58%) in the production of IL-10 in LPS-stimulated macrophages. In the in vivo assay, MA showed good anti-inflammatory effects on the acute (ED50 = 62 mg/kg) and chronic (ED50 = 77 mg/kg) TPA-induced ear edema. The antinociceptive activity of MA was related to the participation of the nitrergic system in the formalin-induced paw licking test. PRACTICAL APPLICATIONS: Previous studies with different plant extracts containing MA, as one of their major components, have demonstrated anti-inflammatory and antinociceptive actions. However, the anti-inflammatory and antinociceptive actions of myristic acid have not been previously reported. The results suggest that MA induced anti-inflammatory effects in LPS-stimulated macrophages through the participation of IL-10. The antinociceptive effects of MA are attributed to the participation of the nitrergic system.

Anti-inflammatory activity of Jefea gnaphalioides (a. gray), Astereaceae.

BACKGROUND: Inflammation is a symptom associated with many diseases. This symptom is treated with steroidal and non-steroidal anti-inflammatory drugs, which can cause severe side effects when used as long-term treatments. Natural products are an alternative source of new compounds with anti-inflammatory activity. Jefea gnaphalioides (Astereaceae) (A. Gray) is a plant species used to treat inflammatory problems, in Mexico. This study determined the anti-inflammatory activity and the composition of the methanol extract of Jefea gnaphalioides (MEJG). METHODS: The extract was obtained by heating the plant in methanol at boiling point for 4 h, and then the solvent was evaporated under vacuum (MEJG). The derivatization of the extract was performed using Bis-(trimethylsilyl) trifluoroacetamide, and the composition was determined by GC-MS. Total Phenols and flavonoids were determined by Folin-Ciocalteu AlCl3 reaction respectively. The antioxidant activity of MEJG was determined by DPPH method. The acute and chronic anti-inflammatory effects were evaluated on a mouse ear edema induced with 12-O-Tetradecanoylphorbol-13-acetate (TPA). Acute oral toxicity was tested in mice at doses of MEJG of 5000, 2500 and 1250 mg/kg. The levels of NO, TNF-α, IL-1ß and IL-6 were determinate in J774A.1 macrophages stimulated by Lipopolysaccharide. The production of inflammatory interleukins was measured using commercial kits, and nitric oxide was measured by the Griess reaction. RESULTS: The anti-inflammatory activity of MEJG in acute TPA-induced ear edema was 80.7 ± 2.8%. This result was similar to the value obtained with indomethacin (IND) at the same dose (74.3 ± 2.8%). In chronic TPA-induced edema at doses of 200 mg/kg, the inhibition was 45.7%, which was similar to that obtained with IND (47.4%). MEJG have not toxic effects even at a dose of 5000 mg/kg. MEJG at 25, 50, 100 and 200 µg/mL decreased NO, TNF-α, IL-1ß and IL-6 production in macrophages stimulated with LPS. The major compounds in MEJG were α-D-Glucopyranose (6.71%), Palmitic acid (5.59%), D-(+)-Trehalose (11.91%), Quininic acid (4.29%) and Aucubin (1.17%). Total phenolic content was 57.01 mg GAE/g and total flavonoid content was 35.26 mg QE/g MEJG had antioxidant activity. CONCLUSIONS: MEJG has anti-inflammatory activity.

Anti-inflammatory activity of standardized dichloromethane extract of Salvia connivens on macrophages stimulated by LPS.

CONTEXT: A previous study demonstrated that the chloroform extract of Salvia connivens Epling (Lamiaceae) has anti-inflammatory activity. OBJECTIVE: Identification of the active components in the dicholorometane extract (DESC), and, standardization of the extract based in ursolic acid. MATERIAL AND METHODS: DESC was prepared by percolation with dichlromethane and after washed with hot hexane, its composition was determined by CG-MS and NMR, and standardized by HPLC. The anti-inflammatory activity was tested on acute TPA-induced mouse ear oedema at doses of 2.0 mg/ear. The cell viability of macrophages was evaluated by MTT method, and pro- and anti-inflammatory interleukin levels were measured using an ELISA kit. RESULTS: Ursolic acid, oleanolic acid, dihydroursolic acid and eupatorin were identified in DESC, which was standardized based on the ursolic acid concentration (126 mg/g). The anti-inflammatory activities of DESC, the acid mixture, and eupatorin (2 mg/ear) were 60.55, 57.20 and 56.40% inhibition, respectively, on TPA-induced ear oedema. The IC50 of DESC on macrophages was 149.4 µg/mL. DESC (25 µg/mL) significantly reduced TNF-α (2.0-fold), IL-1ß (2.2-fold) and IL-6 (2.0-fold) in macrophages stimulated with LPS and increased the production of IL-10 (1.9-fold). DISCUSSION: Inflammation is a basic response to injuries, and macrophages are involved in triggering inflammation. Macrophage cells exhibit a response to LPS, inducing inflammatory mediators, and DESC inhibits the biosynthesis of the pro-inflammatory and promote anti-inflammatory cytokines. CONCLUSION: DESC has an anti-inflammatory effect; reduced the levels of IL-1ß, Il-6 and TNF-α; and increases IL-10 in macrophages stimulated with LPS. Ursolic acid is a good phytochemical marker.

Antigiardial Effect of Kramecyne in Experimental Giardiasis.

A variety of drugs are used in giardiasis treatment with different levels of efficiency, presence of side effects, and even formation of resistant strains, so that it is important to search new only-one-dose treatments with high efficiency and less side effects. Kramecyne, an anti-inflammatory compound isolated from methanolic extract of Krameria cytisoides, does not present toxicity, even at doses of 5,000 mg/kg. The objective was to determine the antigiardial effect of kramecyne over Giardia intestinalis in vitro and in vivo and analyze the expression of genes ERK1, ERK2, and AK on kramecyne treated trophozoites by Real Time Polymerase Chain Reaction (RTPCR). The median lethal dose (LD50) was 40 µg/mL and no morphological changes were observed by staining with blue trypan and light microscopy; experimental gerbil infection was eliminated with 320 µg/Kg of weight. After treatment there were no differences between intestines from treated and untreated gerbils. Kramecyne did not have significant effect over ERK1 and AK, but there are differences in ERK2 expression (p = 0.04). Results show antigiardial activity of kramecyne; however the mode of action is still unclear and the evaluation of ultrastructural damage and expressed proteins is an alternative of study to understand the action mechanism.

Antispasmodic Effects and Action Mechanism of Essential Oil of Chrysactinia mexicana A. Gray on Rabbit Ileum.

The Chrysactinia mexicana A. Gray (C. mexicana) plant is used in folk medicine to treat fever and rheumatism; it is used as a diuretic, antispasmodic; and it is used for its aphrodisiac properties. This study investigates the effects of the essential oil of C. mexicana (EOCM) on the contractility of rabbit ileum and the mechanisms of action involved. Muscle contractility studies in vitro in an organ bath to evaluate the response to EOCM were performed in the rabbit ileum. EOCM (1-100 µg·mL(-1)) reduced the amplitude and area under the curve of spontaneous contractions of the ileum. The contractions induced by carbachol 1 µM, potassium chloride (KCl) 60 mM or Bay K8644 1 µM were reduced by EOCM (30 µg·mL(-1)). Apamin 1 µM and charybdotoxin 0.01 µM decreased the inhibition induced by EOCM. The d-cAMP 1 µM decreased the inhibition induced by EOCM. l-NNA 10 µM, Rp-8-Br-PET-cGMPS 1 µM, d,l-propargylglycine 2 mM, or aminooxyacetic acid hemihydrochloride 2 mM did not modify the EOCM effect. In conclusion, EOCM induces an antispasmodic effect and could be used in the treatment of intestinal spasms or diarrhea processes. This effect would be mediated by Ca(2+), Ca(2+)-activated K⁺ channels and cAMP.

In Vivo Antiprotozoal Activity of the Chloroform Extract from Carica papaya Seeds against Amastigote Stage of Trypanosoma cruzi during Indeterminate and Chronic Phase of Infection.

In order to evaluate the antiprotozoal activity of the chloroform extract of Carica papaya seeds during the subacute and chronic phase of infection of Trypanosoma cruzi, doses of 50 and 75 mg/kg were evaluated during the subacute phase, including a mixture of their main components (oleic, palmitic, and stearic acids). Subsequently, doses of 50 and 75 mg/kg in mice during the chronic phase of infection (100 dpi) were also evaluated. It was found that chloroform extract was able to reduce the amastigote nests numbers during the subacute phase in 55.5 and 69.7% (P > 0.05) as well as in 56.45% in animals treated with the mixture of fatty acids. Moreover, the experimental groups treated with 50 and 75 mg/kg during the chronic phase of the infection showed a significant reduction of 46.8 and 53.13% respectively (P < 0.05). It is recommended to carry out more studies to determine if higher doses of chloroformic extract or its administration in combination with other antichagasic drugs allows a better response over the intracellular stage of T. cruzi in infected animal models and determine if the chloroform extract of C. papaya could be considered as an alternative for treatment during the indeterminate and chronic phase of the infection.

Bioassay-guided chemical study of the anti-inflammatory effect of Senna villosa (Miller) H.S. Irwin & Barneby (Leguminosae) in TPA-induced ear edema.

Senna villosa (Miller) is a plant that grows in México. In traditional Mexican medicine, it is used topically to treat skin infections, pustules and eruptions and to heal wounds by scar formation. However, studies of its potential anti-inflammatory effects have not been performed. The aim of the present study was to determine the anti-inflammatory effect of extracts from the leaves of Senna villosa and to perform a bioassay-guided chemical study of the extract with major activity in a model of ear edema induced by 12-O-tetradecanoylphorbol 13-acetate (TPA). The results reveal that the chloroform extract from Senna villosa leaves has anti-inflammatory and anti-proliferative properties. Nine fractions were obtained from the bioassay-guided chemical study, including a white precipitate from fractions 2 and 3. Although none of the nine fractions presented anti-inflammatory activity, the white precipitate exhibited pharmacological activity. It was chemically characterized using mass spectrometry and infrared and nuclear magnetic resonance spectroscopy, resulting in a mixture of three aliphatic esters, which were identified as the principal constituents: hexyl tetradecanoate (C20H40O2), heptyl tetradecanoate (C21H42O2) and octyl tetradecanoate (C22H44O2). This research provides, for the first time, evidence of the anti-inflammatory and anti-proliferative properties of compounds isolated from Senna villosa.

Evaluation of the anti-diarrheal activity of Salvia connivens.

CONTEXT: Diarrheal disease is a leading cause of mortality and morbidity and accounts for 5-8 million deaths worldwide each year. Salvia connivens Epling (Lamiaceae) is used to treat sore throat, fevers, diarrhea, malaria, and also is used as an antipyretic. OBJECTIVE: The present study evaluates the efficacy of S. connivens in the treatment of diarrhea using animal models. MATERIALS AND METHODS: The anti-diarrheal effect of methanol extract of S. connivens was investigated on mice with castor oil, arachidonic acid (AA) or prostaglandin E2 (PGE2)-induced diarrhea. On Wistar rats, the activity was evaluated on the intestinal transit and Castor oil-induced enteropooling. RESULTS: The methanol extract at doses of 6.25, 12.5, 25, 50, 100, and 200 mg/kg on castor oil-induced diarrhea reduced the diarrhea by 32.3, 41.9, 67.7, 74.2, 83.3, and 100%, respectively. Additionally, this extract, at doses of 200 mg/kg, inhibited AA-induced diarrhea by 100%. The methanol extract produced no effect on PGE2-induced diarrhea at the same doses. In Wistar rats, at dose of 200 mg/kg, the methanol extract inhibited intestinal transit and decreased the volume of intestinal secretion induced by castor oil. DISCUSSION: The methanol extract showed anti-diarrheal effect on the animal models used. Phytochemical screening revealed the presence of alkaloids, tannins, and saponins which may be responsible for this effect. The extract did not cause any mortality or any visible signs of toxicity or differences in food and water uptake were seen. CONCLUSIONS: These results justify the use of S. connivens as an anti-diarrheal agent.

Composition and Antidiarrheal Activity of Bidens odorata Cav.

The antidiarrheal effects of chloroform, methanol, and aqueous extracts of Bidens odorata Cav. were investigated at doses of 200 mg/kg on castor-oil-induced diarrhea. The chloroform extract of B. odorata (CBO) reduced diarrhea by 72.72%. The effect of CBO was evaluated on mice with diarrhea induced by castor oil, MgSO4, arachidonic acid, or prostaglandin E2. CBO inhibited the contraction induced by carbachol chloride on ileum (100 µg/mL) and intestinal transit (200 mg/kg) in Wistar rats. The active fraction of CBO (F4) at doses of 100 mg/kg inhibited the diarrhea induced by castor oil (90.1%) or arachidonic acid (72.9%) but did not inhibit the diarrhea induced by PGE2. The active fraction of F4 (FR5) only was tested on diarrhea induced with castor oil and inhibited this diarrhea by 92.1%. The compositions of F4 and FR5 were determined by GC-MS, and oleic, palmitic, linoleic, and stearic acids were found. F4 and a mixture of the four fatty acids inhibited diarrhea at doses of 100 mg/kg (90.1% and 70.6%, resp.). The results of this study show that B. odorata has antidiarrheal effects, as is claimed by folk medicine, and could possibly be used for the production of a phytomedicine.

Assessment of the anti-protozoal activity of crude Carica papaya seed extract against Trypanosoma cruzi.

In order to determine the in vivo activity against the protozoan Trypanosoma cruzi, two doses (50 and 75 mg/kg) of a chloroform extract of Carica papaya seeds were evaluated compared with a control group of allopurinol. The activity of a mixture of the three main compounds (oleic, palmitic and stearic acids in a proportion of 45.9% of oleic acid, 24.1% of palmitic and 8.52% of stearic acid previously identified in the crude extract of C. papaya was evaluated at doses of 100, 200 and 300 mg/kg. Both doses of the extracts were orally administered for 28 days. A significant reduction (p < 0.05) in the number of blood trypomastigotes was observed in animals treated with the evaluated doses of the C. papaya extract in comparison with the positive control group (allopurinol 8.5 mg/kg). Parasitemia in animals treated with the fatty acids mixture was also significantly reduced (p < 0.05), compared to negative control animals. These results demonstrate that the fatty acids identified in the seed extracts of C. papaya (from ripe fruit) are able to reduce the number of parasites from both parasite stages, blood trypomastigote and amastigote (intracellular stage).

Antidiarrheal activity of 19-deoxyicetexone isolated from Salvia ballotiflora Benth in mice and rats.

The antidiarrheal properties of 19-deoxyicetexone, a diterpenoid isolated from Salvia ballotiflora were evaluated on castor oil-, arachidonic acid (AA)- and prostaglandin (PGE2)-induced diarrhea in rodent models. The structure of 19-deoxyicetexone was determined by X-ray crystallography, mass spectrometry (EI-MS), as well as ultraviolet (UV-Vis), infrared (FT-IR) and nuclear magnetic resonance (NMR) spectroscopies. This compound significantly and dose-dependently reduced frequency of stooling in castor oil-induced diarrhea, and at dose of 25 mg/kg it also inhibited diarrhea induced with AA, while it had no effect on PGE2-induced diarrhea. This compound at doses of 25 mg/kg also diminished castor oil-induced enteropooling and intestinal motility, and inhibited the contraction of the rats' ileum induced by carbachol chloride at a concentration of 100 µg/mL. 19-Deoxyicetexone did not present acute toxicity at doses of 625 mg/kg. Its antidiarrheal activity may be due to increased reabsorption of NaCl and water and inhibition of the release of prostaglandins, gastrointestinal motility and fluid accumulation in the intestinal tracts of rats. These findings suggest that 19-deoxyicetexone may be used in the treatment of diarrhea, although more studies must be carried out to confirm this.

Kramecyne--a new anti-inflammatory compound isolated from Krameria cytisoides.

In the present work we describe the structure and anti-inflammatory activity of a new compound, kramecyne, isolated from a methanol extract of Krameria cytisoides (Krameriaceae). The structure of kramecyne was determined by IR, NMR, MS, and elemental analysis, which indicated that the structure corresponded to a hexamer of cyclic peroxide monomers. This compound exhibited good anti-inflammatory activity in the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema (51.8 ± 6.9% inhibition) and carrageenan-induced rat paw edema models at doses of 50 mg/kg. The compound significantly reduced edema to 63.1% after 1.0 h, and the effect was unchanged for 5 h. Kramecyne did not present acute toxicity, even at doses of 5,000 mg/kg.

Bioactivity of Carica papaya (Caricaceae) against Spodoptera frugiperda (Lepidoptera: Noctuidae).

The composition of a chloroform seed extract of C. papaya was determined by GC-MS. Nineteen compounds were identified, with oleic (45.97%), palmitic (24.1%) and stearic (8.52%) acids being the main components. The insecticidal and insectistatic activities of the extract and the three main constituents were tested. Larval duration increased by 3.4 d and 2.5 d when the extract was used at 16,000 and 9,600 ppm, respectively, whereas the pupal period increased by 2.2 d and 1.1 d at the same concentrations. Larval viability values were 0%, 29.2%, and 50% when the extract was applied at 24,000, 16,000, and 9,600 ppm, respectively; pupal viability was 42.9% and 66.7% at 16,000 and 9,600 ppm; and pupal weight decreased by 25.4% and 11.5% at 16,000 and 9,600 ppm. The larval viability of the main compounds was 33.3%, 48.5%, and 62.5% when exposed to 1,600 ppm of palmitic acid, oleic acid, or stearic acid, respectively.

Anti-inflammatory evaluation and antioxidant potential of Senna crotalarioides and Penstemon roseus / Evaluación anti-inflamatoria y potencial antioxidante de Senna crotalarioides y Penstemon roseus

Chloroform, methanol and aqueous extracts of Penstemon roseus and Senna crotalarioides were investigated for their anti-inflammatory and antioxidant properties. The aqueous extract had no activity on TPA-induced ear edema, but the chloroform and methanol extracts of both plants caused a significant inhibition of the edema. The chloroform extracts showed activity on carrageenan-induced paw edema and mouse ear edema induced by multiple topical applications of TPA, and only P. roseus (dose of 100 mg/kg) exhibited anti-arthritic activity. The methanol extracts of P. roseus and S. crotalarioides had the most activity in the DPPH and reducing power tests. The LD50 values in mice of both chloroform extracts were considerate as slight acute toxic and higher than the doses used in this study.

Las propiedades antiinflamatorias y antioxidantes de los extractos de cloroformo, metanol y agua de Penstemon roseus y Senna crotalarioides fueron investigadas. El extracto acuoso no tuvo actividad sobre el edema auricular inducido con TPA, pero el extracto de cloroformo y etanol de ambas plantas inhibieron significativamente el edema. El extracto de cloroformo mostró actividad sobre el edema plantar inducido con carragenina y el edema auricular en ratón inducido por múltiples aplicaciones de TPA, y solo P. roseus y S. crotalarioides tuvieron la mejor actividad en las pruebas de DPPH y poder reductor. Los valores de la DL50 en ratón de ambos extractos de cloroformo son considerados con ligera toxicidad aguda y mayores que las dosis empleadas en el estudio.

Antitrypanosomal activity of Senna villosa in infected BALB/c mice with Trypanosoma cruzi during the sub acute phase of infection.

Antitrypanosomal activity of chloroform extract of Senna villosa leaves was evaluated in the sub acute phase of mice infected with Trypanosoma cruzi. Oral doses of 3.3, 6.6 and 13.2 µg/g were tested during 15 days on infected mice BALB/c, beginning treatment 40 days after infection to evaluate specifically the antitrypanosomal activity over the amastigote form of the parasite. Two different amount of parasites (100 and 500) were inoculated to 25 mice for each doses tested. At the end of the assay the animals were sacrificed and cardiac and skeletal tissue sections were stained with hematoxylin-eosin (HE) for identification and quantification of amastigote nest. In mice infected with 100 parasites, a significant reduction in the number of amastigote nest was observed in cardiac tissue of treated animals at all doses evaluated (p<0.05). An important reduction of amastigote nest was also observed in treated animals and infected with 500 parasites in comparison with no treated mice or treated with allopurinol.

Chemical composition and antifungal activity of essential oil of Chrysactinia mexicana gray.

The chemical composition of the essential oil of Chysactinia mexicana was analyzed by gas chromatography-mass spectrometry. Seventeen compounds were characterized; eucalyptol (41.3%), piperitone (37.7%), and linalyl acetate (9.1%) were found as the major components. The essential oil of leaves and piperitone completely inhibited Aspergillus flavus growth at relatively low concentrations (1.25 and 0.6 mg/mL, respectively).

Anti-hyperglycemic effect of Psacalium peltatum.

The purpose of this research was to study the anti-hyperglycemic effect of Psacalium peltatum, a folk medicinal plant used in treatment of diabetes mellitus. This plant was processed in the traditional way (water decoction) and administered i.p. to normoglycemic and diabetic mice. Hexane, chloroform, methanol and water extracts were administered to fasting healthy mice. The results showed that the water decoction, methanolic extract and aqueous extracts exhibit hypoglycemic activity in the studied mice. The methanolic extract was submitted to a separation process by chromatographic column from which seven fractions were obtained. Each fraction was administered to healthy mice and hypoglycemic activity was found in fraction VII. A second chromatographic separation was performed on this fraction, to yield seven subfractions. The results of the biological trials showed that the subfractions SFII and SFIII significantly reduce blood glucose levels in healthy mice.

Actividad hipoglucemiante de Bouvardia terniflora, Brickellia veronicaefolia y parmentiera edulis / Hypoglycemic activity of Bouvardia terniflora, Brickellia veronicaefolia and parmentiera edulis

Objetivo. Evaluar la actividad hipoglucemiante de los extractos de hexano, cloroformo y metanol de Brickellia veronicaefolia, Bouvardia terniflora y Parmentiera edulis. Material y métodos. Se probaron los extractos de las plantas (100, 200 y 300 mg/kg, vía intraperitoneal) en ratones normoglucémicos y con diabetes inducida con aloxana. Resultados. La administración de 300 mg/kg de los extractos clorofórmicos de P. edulis, B. terniflora y hexánico de B. veronicaefolia en ratones diabéticos disminuye el nivel de glucosa sanguínea en 43.75, 58.56 y 72.13 por ciento, respectivamente. Estos extractos (300 mg/kg), administrados en ratones normoglucémicos, reducen la glucosa sanguínea en 29.61, 33.42 y 39.84 por ciento, respectivamente. Conclusiones. Con este estudio se confirma la actividad hipoglucemiante de estas plantas usadas en la medicina tradicional para el tratamiento de las diabetes