ABSTRACT
Angiogenesis, formation of new blood vessels, play an important role in some diseases such as cancer and its metastasis. Using angiogenesis inhibitors, therefore, is one of the ways for cancer treatment and prevention of metastasis. Medicinal plants have been shown to play a major role in the treatment of a variety of cancers. In this direction, cytotoxic and angiogenic effects of oleo gum resin extracts of Rhus coriaria, Pistacia vera and Pistacia khinjuk from Anacardiaceae family were studied. For IC50 values, cytotoxic effects of the plant extracts were evaluated at different concentrations (1, 10, 20, 40, 80,100 µg/ml) against human umbilical vein endothelial normal cell (HUVEC) and Y79 cell lines using 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. In vitro tube formation on matrigel base was used to evaluate angiogenic effects in the presence of increasing concentrations (50, 100, 250 µg/ml) of the extracts. Vascular endothelium growth factor was used as angiogenesis stimulator. Gas chromatography results showed that α-pinene and ß-pinene were the major essential oils constituents of all plant extracts. According to the MTT assay results, the R. coriaria resin extract was more cytotoxic than those of P. vera and P. khinjuk extracts (IC50, 9.1 ± 1.6 vs 9.8 ± 2.1 and 12.0 ± 1.9, respectively; P<0.05). Cytotoxic effects of all extracts against Y79 cell line was significantly higher than those of HUVEC used as a normal cell line (P<0.05). Tube formation assay also showed that extract of R. coriaria resin inhibited angiogenesis more significantly than other tested extracts (P<0.05). It could be concluded that R. coriaria resin extract possess cytotoxic effect and antiangiogenesis against cancer cells and as an anticancer natural product has a good potential for future studies.
ABSTRACT
Bioassay monitoring of hydroalcoholic extract from the aerial part of Pyconcycla spinosa revealed that it contains components with spasmolytic activity in vitro. In addition, P. spinosa extract at oral dose of 1-5 mg/kg inhibits diarrhoea in animal models. Pharmacological screening of pure compounds isolated from P. spinosa hydroalcoholic extract led to the identification of 3,7,10,14,15-pentaacetyl-5-butanoyl-13,17-epoxy-8-myrsinene (PABEM) which is a new diterpene. In this research, we have investigated antispasmodic and antidiarrheal effects of PABEM for comparison with P. spinosa extract. Aerial parts of P. spinosa were extracted with ethanol. For antispasmodic studies, rat isolated ileum was suspended in Tyrode's solution in an organ bath. The ileum was contracted by acetylcholine (ACh, 0.5 µM), serotonin (5-HT, 5 µM) or electrical field stimulation (EFS). P. spinosa extract in a concentration dependent manner (10-640 µg/ml) inhibited ileum contractions induced by ACh, 5-HT or EFS. The new compound isolated form P. spinosa extract "PABEM" in a similar manner inhibited the contractile response to ACh, 5-HT and EFS. However, the inhibitory effects of PABEM were observed at much lower bath concentrations. The relaxation effect of PABEM was started at 40 ng/ml bath concentration and with 2.5 µg/ml PABEM in the bath, the contractile responses of ileum were completely abolished. Both hydroalcoholic extract of P. spinosa and PABEM reduced intestinal meal transit and castor oil and MgSO4 induced diarrhoea in mice. However, PABEM was about 10 times more potent than its parent extract. This research shows that PABEM is probably the main component responsible for antispasmodic and antidiarrheal actions of P. spinosa extract.
ABSTRACT
Isovanillin and iso-acetovanillon are two phenolic components isolated from a number of plants including Pycnocycla spinosa. P. spinosa extract has antispasmodic and antidiarrheal activities. However, no comparative study has been done on antidiarrheal action of isovanillin and iso- acetovanillon, so far. The aim of this study was to investigate antidiarrheal action of isovanillin and iso-acetovanillon and their effects on small intestinal transit, for comparison with propantheline. Male mice (25-30 g), fasted over night with free access to water, were treated with test compounds or control (p.o.). Thirty min later castor oil (0.5 ml) was given orally to the animals. In another groups of animals MgSO4 (0.5 ml of 10% solution) was given first and half an hour later the test drugs were administered. Onset and number of wet defecations were recorded for each animal over 3.5 h after treatment with diarrhoea inducing agents. In another groups, intestinal transit of charcoal meal was determined following administration of the compounds. Isovanillin (2 mg/kg & 5 mg/kg), iso-acetovanillon (2 mg/kg & 5 mg/kg) and P. spinosa extract (5 mg/kg) delayed onset of diarrhoea and significantly reduced wet defecation induced by castor oil and MgSO4. They all had antidiarrheal effect similar to propantheline (5 mg/kg). Isovanillin, iso-acetovanillon and P. spinosa extract compared to control groups, significantly reduced small intestinal transit of charcoal meal. This study shows that antidiarrheal effect of P. spinosa extract is at least partially due to presence of two active compounds isovanillin and iso-acetovanillon.
ABSTRACT
Isovanillin and isoacetovanillon are two components found in P. spinosa Decne.exBoiss extract with no previously reported effect on ileum contractions. Spasmolytic effect of isovanillin and isoacetovanillon were examined on response to electrical field stimulation (EFS), acetylcholine (ACh) and 5-HT in strips of rat ileum. Longitudinal ileum strips were set up in an organ bath containing oxygenated Tyrode's solution. All strips that was contracted in response to EFS, acetylcholine or 5-HT showed relaxation in the presence of isovanillin (5-320 µg/ml), or isoacetovanillon (5-320 µg/ml). Isovanillin and isoacetovanillon inhibited the response to 5-HT with IC50 values of 356±50µM and 622±110µM respectively. They reduced the response to EFS without significantly affecting the acetylcholine response. P. spinosa extract (5-160 µg/ml) in a concentration dependent manner reduced the response to 5-HT, acetylcholine and EFS. This study demonstrated that isovanillin and isoacetovanillon are relaxant of ileum contractions induced by 5-HT and EFS and they have contribution to the relaxant effect of P. spinosa extract but other components are responsible for the inhibition of acetylcholine by the extract.
ABSTRACT
Pharmacological activities of 6-(4-hydroxy-3-methoxyphenyl)-hexanonic acid (HMPHA), a phenolic compound, isolated from the extract of Pycnocycla spinosa was investigated on ileum motility in vivo and in vitro. Ileum motility was examined by measuring charcoal movement through the gut in mice. In addition, antidiarrhoeal activity of HMPHA was assessed and compared with standard drug; loperamide (2 mg/kg) and the hydroalcoholic extract of P. spinosa (2 mg/kg). Furthermore, concentration response curve to contraction induced by acetylcholine (ACh), 5-hydroxy triptamine (5-HT) and electrical field stimulation (EFS) were obtained after incubation of ileum segment with various concentrations of HMPHA or hydroalcoholic extract of P. spinosa. HMPHA (2 mg/kg and 5 mg/kg, orally) significantly inhibited gut movements in vivo and reduced diarrhoea induced by castor oil or sulphate magnesium. In addition, HMPHA reduced ileum contraction induced by ACh (IC50=33 ± 6 µg/ml), 5-HT (IC50=87 ± 12 µg/ml) and EFS (IC50=36 ± 3 µg/ml) in vitro in a concentration-dependent manner. The inhibitory effect was reversible following washing off the drug. These studies indicate that HMPHA as an active component of P. spinosa extract has significant antispasmodic and antidiarrhoeal activities and therefore, has the potential as a lead compound for further development of a new spasmolytic remedy.
ABSTRACT
The cytotoxic chloroform fraction of Euphorbia aellenii Rech. F. (Euphorbiaceae) afforded two new phorbol diterpenoids: 4-deoxy-4α-phorbol-12-(2,3-dimethyl) butyrate-13-isobutyrate and 17-hydroxy-4-deoxy-4α-phorbol-12-(2,3-dimethyl) butyrate-13-isobutyrate. Their structures were elucidated by NMR and other spectroscopic methods. The immunomodulating potentials of the isolated compounds were tested using standard proliferation and chemiluminescence assays. Compound 2 showed moderate inhibitory activity against both T-cell proliferation and reactive oxygen species (ROS) production in whole blood with IC50 of 14.0 ± 0.57 and 44.1 ± 3.8 µg/ml, respectively, while compound 1 was relatively inactive with IC50 >50 µg/mL for T-cell proliferation, and >100 µg/mL for ROS.
