Phytochemical composition and biological screening of two Lophophytum species / Composición fitoquímica y cribado biológico de dos especies de Lophophytum

Lophophytum species are holoparasites that grow on tree roots. The objectives of the work were to explore the chemical composition of the tubers of two Lophophytum species and to analyze the antioxidant, anti-inflammatory and antilithiatic activity of their extracts using in vitro methods. The chemical composition was determined by histochemical, phytochemical and TLC tests. In addition, the profile of phenolic compounds was determined by HPLC-MS. The presence of secondary metabolites of recognized activity was demonstrated. The results of the HPLC-MS/MS allowed the tentative identification of catechin, luteolin and glycosides of eriodictyol, naringenin and luteolin in the extract of Lophophytum leandriand eriodictyol, naringenin, luteolin and their glycosylated derivatives in Lophophytum mirabile. The extracts showed promising antioxidant (DPPH, ABTS and ß-carotene-linoleic acid), anti-inflammatory (inhibition of 5-LOX) and anti-urolytic (by bioautographic TLC) activity. It is noteworthy that these are the first results of the phytochemical composition and biological activity of L. mirabile. However, in vivo studies are required to corroborate these activities.

Las especies de Lophophytumson holoparásitas que crecen en raíces de árboles. Los objetivos del trabajo fueron explorar la composición química del túber de dos especies de Lophophytum y analizar la actividad antioxidante, antiinflamatoria y antilitiásica de sus extractos usando métodos in vitro. La composición química se determinó mediante pruebas histoquímicas, fitoquímicas y por TLC. Además, se determinó el perfil de compuestos fenólicos por HPLC-MS/MS. Se demostró presencia de metabolitos secundarios de reconocida actividad. Los resultados del HPLC-MS/MS permitieron identificar tentativamente catequina, luteolina y glucósidos de eriodictiol, naringenina y luteolina en el extracto de Lophophytum leandriy eriodictiol, naringenina, luteolina y sus derivados glicosilados en Lophophytum mirabile. Los extractos mostraron prometedora actividad antioxidante (DPPH, ABTS y ß-caroteno-ácido linoleico), antiinflammatoria (inhibición de la 5-LOX) y antiurolitiásica (por TLC bioautográfica). Es de destacar que estos son los primeros resultados de composición fitoquímica y actividad biológica de L. mirabile. Sin embargo, se requieren estudios in vivo para corroborar dichas actividades.

Efecto del extracto de Corynaea crassa y selenio en la disfunción sexual inducida en Rattus norvegicus albinus / Effect of Corynaea crassa and Selenium extract on sexual dysfunction induced in rats

Introducción. Corynaea crassa es una planta hemiparásita usada como afrodisíaco en la medicina tradicional. Objetivo. Determinar el efecto erectógeno del extracto etanólico de las raíces de Corynaea crassa (EECC) y selenio en la disfunción sexual inducidas en roedores. Materiales y métodos. Investigación de diseño experimental, preclínico, in vivo, llevado a cabo en el Laboratorio de Farmacología Experimental de la Facultad de Medicina Humana-UNMSM, Lima, Perú. Se emplearon raíces de «viagra macho¼ colectada en el departamento de Cajamarca; ratas machos de dos meses, de 150 ­ 200 g; 42 animales se dividieron al azar en siete grupos: 1). SSF 5 mL/kg; 2). Sildenafilo 5 mg/kg/día; 3). EECC 100mg/kg; grupo 4 EECC 200 mg/kg; grupo 5 EECC 400 mg/kg; grupo 6 EECC 200mg/kg + Se 1 ug/kg y grupo 7 EECC 400 mg/kg + Se 1 ug/kg. Se evaluaron los parámetros del comportamiento sexual, reflejos del pene y nivel de testosterona. Resultados. Por análisis cualitativo se identificaron alcaloides, compuestos fenólicos, esteroides/terpenoides, flavonoides, lactonas, saponinas y taninos. El comportamiento sexual fue dosis dependiente; la administración de 400 mg/kg de EECC + Se 1 ug/kg por vía oral incrementó la frecuencia de monta, en tanto que la dosis de 100 mg/kg aumentó la frecuencia de intromisión (p<0,05), así como los parámetros de los reflejos del pene e incremento significativo de los niveles de testosterona. Conclusiones. Se ha demostrado efecto erectógeno del extracto etanólico de las raíces de Corynaea crassa más selenio en la disfunción sexual inducidas en ratas.

Introduction. Corynaea crassa, a hemiparasitic plant used as an aphrodisiac in traditional medicine. Objective. To determine the erectógeno effect of the ethanolic extract of the roots of Corynaea crassa (EECC) and Selenio in the sexual dysfunction induced in rats. Design. Experimental, Pre-clinical, "In vivo". Setting. Laboratory of Experimental Pharmacology, Faculty of Human Medicine-UNMSM, Lima, Peru. Biological material. Roots of "male Viagra", male rats of 2 months, 150-200 g. Interventions. The plant was collected in the department of Cajamarca; 42 animals divided randomly into 7 groups: 1) SSF 5 mL / kg; 2) Sildenafil 5 mg / kg / day; 3) EECC 100 mg / kg; groups 4 EECC 200mg / kg; groups 5 EECC 400 mg/kg; groups 6 EECC 200 mg / kg + Se 1ug / kg and groups 7 EECC 400 mg / kg + Se 1ug/kg. Main outcome measures. The parameters of sexual behavior, penile reflexes and testosterone level were evaluated. Results. For qualitative analysis, alkaloids, phenolic compounds, steroids / terpenoids, flavonoids, lactones, saponins and tannins were identified. The sexual behavior was dose dependent; the administration of 400 mg / kg of EECC + Se 1ug / kg orally increased the frequency of mounting, while the dose of 100 mg / kg increased the frequency of intrusion (p <0.05), as well as the parameters of the reflexes of the penis and significant increase in testosterone levels. Conclusions. The best results were observed in the doses of 200 mg / kg and 400 mg / kg of the EECC in combination with Selenium.

1,3,4-tri-O-galloyl-6-O-caffeoyl-β-D-glucopyranose, a new anti-proliferative ellagitannin, regulates the expression of microRNAs in HepG(2) cancer cells / 南方医科大学学报

<p><b>OBJECTIVE</b>MicroRNAs (miRNAs) play important roles in cell proliferation, differentiation and apoptosis. 1, 3, 4-tri-O-galloyl-6-O-caffeoyl-β-D-glucopyranose (BJA32515) is a new natural ellagitannin compound extracted from Balanophora Japonica MAKINO. The effect of BJA32515 on the expression of miRNAs in cancer cells has not yet been explored. Objective The present study was carried out to examine the changes in miRNA expression profiles in human HepG(2) hepatocarcinoma cells following BJA32515 exposure.</p><p><b>METHODS</b>The proliferation of BJA32515-exposed HepG(2) cells was assessed using a colorimetric assay (cell counting kit-8). The miRNA expression profile of the cancer cells was analyzed using a miRNA array and quantitative real-time PCR. Apoptosis was assessed by annexin V and propidium iodide staining.</p><p><b>RESULTS</b>BJA32515 inhibited the cell proliferation and increased apoptosis in HepG(2) cancer cells. The exposure to BJA32515 also caused alterations in the miRNA expression profile in the cells, with 33 miRNAs upregulated and 59 down-regulated. The up-regulation of let-7a and miR-29a and the down-regulation of miR-373 and miR-197 were verified by quantitative real-time PCR. CONCLSION: BJA32515-modifed miRNA expression may mediate the antiproliferative effect of this compound in HepG(2) cancer cells.</p>

Study of the mechanism of caffeoyl glucopyranoses in inhibiting HIV-1 entry using pseudotyped virus system / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the inhibitory activities of caffeoyl glucopyranoses purified from Balanophora japonica Makino on HIV entry and their mechanism.</p><p><b>METHODS</b>HIV-1 Env pseudovirus was used to evaluate the anti-HIV-1 activity of those compounds. ELISA and molecular docking were used to study the mechanism of the actions of the active compounds.</p><p><b>RESULTS</b>We used the HIV-1 Env pseudovirus to test the anti-HIV-1 activity of the six phenolic compounds (final concentration 25 microg/ml), and found that only 1,2,6-Tri-O-caffeoyl-beta-D-glucopyranose (TCGP) and 1,3-Di-O-caffeoyl-4-O-galloyl-beta-D- glucopyranose (DCGGP) could effectively inhibit the entry of HIV-1 Env pseudovirus into the target cells in a dose-dependent manner, with IC(50) values of 5.5-/+0.2 and 5.3-/+0.1 microg/ml, respectively. These two compounds could also blocked the gp41 six-helix bundle formation. Molecular docking analysis suggested that they might bind to the hydrophobic cavity of the gp41 N-trimeric coiled-coil.</p><p><b>CONCLUSION</b>TCGP and DCGGP are potent HIV-1 entry inhibitors targeting gp41 and can serve as lead compounds for developing novel anti-HIV-1 microbicides for prevention of sexual HIV-1 transmission.</p>

Antibacterial Activity of Thonningia sanguinea against some Multi-Drug Resistant Strains of Salmonella enterica

Background : The emergence of strains of S.enterica with multiple drug resistance (MDR) is of great concern worldwide.The extracts of flowers of Thonningia sanguinea are used in traditional medicine in Ivory Coast to treat diarrhoeal diseases including salmonellosis. Previous studies had shown inhibition of the MDR strain Salmonella Enteritidis lysotype 6. Objectives: The present study focused to investigate the effect of the extract of the flowers of Thonningia sanguinea on some clinical MDR strains of Salmonella namely S.Tyhpi; S. Typhimurium; S. Hadar and a sensitive strain (S.Enteritidis). Methods : The antimicrobial parameters were determined by double dilution with agar slant method. This method led us to determine MIC; IC 50 and MBC. Results: The MDR strain of S.Typhimurium presented the highest MIC (2.5 mg/ml) whereas the other two MDR strains (S.Hadar; S.Typhi) and the sensitive one (S.Enteritidis) had the same MIC (1.25 mg/ml). The four strains presented the same MBC (2.5 mg/ml). The MDR strain of S.Typhi is the most susceptible strain to the aqueous extract of the flowers of Thonningia sanguinea according to The IC 50 values. Conclusions: The aqueous extract of Thonningia sanguinea can provide an alternative therapy for the treatment of salmonellosis; mainly for typhoid fever caused by MDR strains of S Typhi. The extract also inhibits S.Hadar a MDR emerging strain in Ivory Coast

Antibacterial activities of four Thai medicinal plants.

Medicinal plants have long been used and prescribed in Thailand for centuries. Some of them have been used for treating various diseases including infectious diseases. Pouzolzia pentandra Benn., Gelonium multiflorum A. Juss., Erycibe elliptilimba Merr. and Chun., Balanophora abbreviate Bl. are Thai medicinal plants from the Thai pharmacopoeia that have been prescribed for treating unknown fevers including some specific infectious diseases. This investigation demonstrated the effects of these Thai medicinal plants for their antibacterial activities by using the macrodilution assay. Based on the present study, the water methanol fraction (fraction 2) of Balanophora abbreviate Bl. showed the antibacterial activity at the MIC level of 250 microg/ml but the activity was bacteriostatic in its effects. Therefore, the use of these medicinal plants in controlling fever and infectious diseases appears to be justified and further investigations may be required to obtain more information.

Studies on chemical constituents of Balanophora spicata / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents of Balanophora spicata.</p><p><b>METHOD</b>Various chromatographic and spectral techniques were used to isolate the constituents and elucidate their structures.</p><p><b>RESULT</b>Eight compounds were isolated from whole plant of B. spicata and elucidated as balanophorin A (1), balanophorin B (2), beta-amyrin acetate (3), monogynol A (4), lupeone (5), caffeic acid ethyl ester (6), catechin (7), 1-O-(E)-caffeoyl-3-O-galloyl-beta-D-glucopyranose (8), respectively.</p><p><b>CONCLUSION</b>Compounds of 1-8 were obtained from B. spicata for the first time and the compound 4 was isolated from this genus for the first time.</p>