8 research outputs found
Hypoglycaemic effect of quinolizidine alkaloids - lupanine and 2-thionosparteine on non-diabetic and streptozotocin-induced diabetic rats
The hypoglycaemic effects of two quinolizidine alkaloids: lupanine and 2-thionosparteine were examined in non-diabetic and in streptozotocin-induced diabetic rats. The model of experimental diabetes can be considered to be related to diabetes mellitus type 2 with regards to the impairment of beta-cells' secretory function. A single intraperitoneal injection of 2-thionosparteine at a dose of 8.6\ua0mg/kg lowered the blood glucose levels in diabetic rats at 90 and 120\ua0min after administration and showed similar hypoglycaemic effects to glibenclamide and sparteine, which were used as reference substances. In contrast to glibenclamide, 2-thionosparteine did not result in a significant increase in plasma insulin levels in diabetic rats; an increase was only observed in the non-diabetic group. It was found that lupanine did not exert hypoglycaemic potency in diabetic and in non-diabetic animals and did not significantly increase plasma insulin concentration independent of the group examined. From this study we can state that 2-thionosparteine, but not lupanine, is confirmed to be a possible plasma glucose lowering agent. It is possible that 2-thionosparteine-dependent decrease in blood glucose level is not the only result of this drug's related insulin secretion. © 2007 Elsevier B.V. All rights reserved
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The hypoglycaemic effects of two quinolizidine alkaloids: lupanine and 2-thionosparteine were examined in non-diabetic and in streptozotocin-induced diabetic rats. The model of experimental diabetes can be considered to be related to diabetes mellitus type 2 with regards to the impairment of beta-cells' secretory function. A single intraperitoneal injection of 2-thionosparteine at a dose of 8.6 mg/kg lowered the blood glucose levels in diabetic rats at 90 and 120 min after administration and showed similar hypoglycaemic effects to glibenclamide and sparteine, which were used as reference substances. In contrast to glibenclamide, 2-thionosparteine did not result in a significant increase in plasma insulin levels in diabetic rats; an increase was only observed in the non-diabetic group. It was found that lupanine did not exert hypoglycaemic potency in diabetic and in non-diabetic animals and did not significantly increase plasma insulin concentration independent of the group examined. From this study we can state that 2-thionosparteine, but not lupanine, is confirmed to be a possible plasma glucose lowering agent. It is possible that 2-thionosparteine-dependent decrease in blood glucose level is not the only result of this drug's related insulin secretion. " 2007 Elsevier B.V. All rights reserved.",,,,,,"10.1016/j.ejphar.2007.02.032",,,"http://hdl.handle.net/20.500.12104/42020","http://www.scopus.com/inward/record.url?eid=2-s2.0-34249004601&partnerID=40&md5=7011c5f67be003bfacb0bf2c4a6a2963",,,,,,"01-mar",,"European Journal of Pharmacology",,"24
Wpływ ekstraktów z Epilobium angustifolium i Serenoa repens na poziom ekspresji cytohromów 2D2 i 3A1 w modelu szczurzym
Benign prostatic hyperplasia (BPH) is a common disease affecting aging males. In recent
years, as alternative strategy for the prevention and therapy of BPH, there is an growing
interest in usage of plant derived remedies i.e. from Serenoa repens (sabal palm) and some
plants from the Epilobium genus. The aim of this study was to investigate the influence of
standardized Epilobium angustifolium L. and Serenoa repens extracts on expression level of
CYP3A1 and CYP2D2 mRNAs in rats. Testosterone and standardized Epilobium angustifolium
or commercial Serenoa repens extracts were given for 21 days to castrated male Wistar rats.
The levels of CYP2D2 and CYP3A1 mRNAs expression were analyzed by real-time quantitative
PCR using specific target primers.
We have observed a slightly increased level of CYP2D2 mRNA in animals treated with testosterone
and both plant extracts (by 4.6% in rats receiving Epilobium angustifolium extract
and by 25.29% in animals treated with extract from Serenoa repens) and the CYP3A1 mRNA
level by 11.02% in rats treated with Serenoa repens extract. In rats receiving E. angustifolium
extract a 20.22% decrease of CYP3A1 mRNA expression level was observed.
Results from our work showed that standardized plant extracts from Epilobium angustifolium
and Serenoa repens have differentially influenced on CYP3A1 and CYP2D2 mRNA expression
level in a rat liver.Łagodny rozrost gruczołu krokowego jest powszechnym schorzeniem występującym
u starzejących się mężczyzn. W ostatnich latach wzrosło zainteresowanie roślinami leczniczymi
należącymi do gatunku boczni piłkowanej (Serenoa repens) i rodzaju wierzbownica
(Epilobium sp.), które mogą stać się alternatywną strategią profilaktyki i leczenia BPH.
Celem pracy było ustalenie wpływu standaryzowanych wyciągów z Epilobium angustifolium
i Serenoa repens na ekspresję cytochromów CYP3A1 i 2D2 u szczurów. Kastrowanym samcom
szczurów rasy Wistar podawano przez okres 21 dni testosteron i badane, standaryzowane
wyciągi roślinne. Zmiany poziomu ekspresji mRNA CYP3A1 i 2D2 mierzono techniką
PCR w czasie rzeczywistym z użyciem starterów specyficznych dla cytochromów. Stwierdzono
nieznaczne podwyższenie poziomu ekspresji mRNA CYP2D2 u zwierząt otrzymujących
testosteron i oba wyciągi roślinne (podwyższenie o 4,6% u szczurów otrzymujących
wyciąg z Epilobium angustifolium i o 25,29% u zwierząt otrzymujących wyciąg z Serenoa repens)
i wzrost poziomu ekspresji mRNA CYP3A1 o 11,02% u zwierząt otrzymujących wyciąg
z Serenoa repens. U szczurów otrzymujących wyciąg z Epilobium angustifolium stwierdzono
obniżenie poziomu ekspresji mRNA CYP3A1 o 20,22%. Wyniki naszej pracy wykazały, że
standaryzowane wyciągi z Epilobium angustifolium i Serenoa repens w zróżnicowany sposób
wpływają na poziom transkrypcji CYP3A1 i CYP2D2 mRNA w wątrobie szczura
Effect of camellia sinensis extract on the expression level of transcription factors and cytochrome p450 genes coding phase i drug-metabolizing enzymes
Green tea (Camellia sinensis) is widely used as a popular beverage and dietary supplement
that can significantly reduce the risk of many diseases. Despite the widespread
use of green tea, the data regarding the safety as well as herb-drug interactions are
limited. Therefore, the aim of our study was to assess the influence of standardized
green tea extract (GTE) containing 61% catechins and 0.1% caffeine on the expression
level of rat CYP genes and the corresponding transcription factors expression by realtime
PCR. The findings showed that GTE resulted in a significant decrease of CYP2C6
expression level by 68% (p<0.001). In case of CYP3A1 and CYP3A2, the mRNA levels
were also reduced by extract but in a lesser degree compared to CYP2C6. Simultaneously
the significant increase in the mRNA level of CAR, RXR and GR factors was observed
by 54% (p<0.05), 79% (p<0.001) and 23% (p<0.05), respectively after 10 days
of green tea extract administration. In addition, there was noted a small increase of
CYP1A1 expression level by 21% (p>0.05) was noted. No statistically significant differences
were observed for CYP1A2 and CYP2D1/2. In the same study we observed
an increase in amount of ARNT gene transcript by 27% (p<0.05) in the long-term use.
However, green tea extract showed the ability to stimulate HNF-1α both after 3 and
10 days of treatment by 30% (p<0.05) and 80% (p<0.001), respectively. In contrast,
no change was observed in the concentration of HNF-4α cDNA. These results suggest
that GTE may change the expression of CYP enzymes, especially CYP2C6 (homologue
to human CYP2C9) and may participate in clinically significant interactions with drugs
metabolized by these enzymes.Zielona herbata (Camellia sinensis) jest powszechnie stosowana jako napój i suplement diety
i może istotnie zmniejszać ryzyko wystąpienia wielu chorób. Pomimo powszechnego
59
Effect of Camellia sinensis extract on the expression level of transcription factors and cytochrome P450 genes coding...
Vol. 59 No. 4 2013
zastosowania zielonej herbaty, dane dotyczące bezpieczeństwa jak i interakcji preparatu
roślinnego i leku syntetycznego są bardzo ograniczone. Celem badania była ocena wpływu
standaryzowanego ekstraktu z zielonej herbaty (GTE) zawierającego 61% katechin i 0,1%
kofeiny na poziom ekspresji szczurzych genów CYP i czynników transkrypcyjnych stosując
technikę real-time PCR. Wyniki wykazały, że GTE znacznie obniża poziom ekspresji
CYP2C6 o 68% (p<0,001). W przypadku CYP3A1 i CYP3A2 poziom mRNA tych genów był
również redukowany przez ekstrakt, ale w mniejszym stopniu w porównaniu do CYP2C6.
Istotny wzrost w poziomie mRNA obserwowano dla czynników CAR, RXR i GR odpowiednio
o 54% (p<0,05), 79% (p<0,001) i 23% (p<0,05) po 10 dniach stosowania ekstraktu. Dodatkowo,
zanotowano niewielki wzrost poziomu ekspresji CYP1A1 o 21% (p>0,05). Brak
istotnych różnic zaobserwowano dla CYP1A2 i CYP2D1/2. W badaniu wykazano również
wzrost ilości transkryptu genu ARNT o 27% (p<0,05) podczas dłuższego stosowania. Ponadto,
ekstrakt z zielonej herbaty wykazał zdolność do stymulacji HNF-1α zarówno po
3, jak i 10 dniach trwania eksperymentu odpowiednio o 30% (p<0,05) i 80% (p<0,001).
Brak zmian obserwowano w przypadku stężenia cDNA dla HNF-4α. Wyniki te sugerują, że
GTE może zmieniać ekspresję enzymów CYP, szczególnie w przypadku CYP2C6 (homolog
ludzki CYP2C9) i może uczestniczyć w klinicznie istotnych reakcjach z lekami metabolizowanymi
przez te enzymy
Wpływ ekstraktu z Camellia sinensis na poziom ekspresji czynników transkrypcyjnych i genów cytochromu P450 kodujących enzymy I fazy metabolizmu leków
Green tea (Camellia sinensis) is widely used as a popular beverage and dietary supplement
that can significantly reduce the risk of many diseases. Despite the widespread
use of green tea, the data regarding the safety as well as herb-drug interactions are
limited. Therefore, the aim of our study was to assess the influence of standardized
green tea extract (GTE) containing 61% catechins and 0.1% caffeine on the expression
level of rat CYP genes and the corresponding transcription factors expression by realtime
PCR. The findings showed that GTE resulted in a significant decrease of CYP2C6
expression level by 68% (p<0.001). In case of CYP3A1 and CYP3A2, the mRNA levels
were also reduced by extract but in a lesser degree compared to CYP2C6. Simultaneously
the significant increase in the mRNA level of CAR, RXR and GR factors was observed
by 54% (p<0.05), 79% (p<0.001) and 23% (p<0.05), respectively after 10 days
of green tea extract administration. In addition, there was noted a small increase of
CYP1A1 expression level by 21% (p>0.05) was noted. No statistically significant differences
were observed for CYP1A2 and CYP2D1/2. In the same study we observed
an increase in amount of ARNT gene transcript by 27% (p<0.05) in the long-term use.
However, green tea extract showed the ability to stimulate HNF-1α both after 3 and
10 days of treatment by 30% (p<0.05) and 80% (p<0.001), respectively. In contrast,
no change was observed in the concentration of HNF-4α cDNA. These results suggest
that GTE may change the expression of CYP enzymes, especially CYP2C6 (homologue
to human CYP2C9) and may participate in clinically significant interactions with drugs
metabolized by these enzymes.Zielona herbata (Camellia sinensis) jest powszechnie stosowana jako napój i suplement diety
i może istotnie zmniejszać ryzyko wystąpienia wielu chorób. Pomimo powszechnego
59
Effect of Camellia sinensis extract on the expression level of transcription factors and cytochrome P450 genes coding...
Vol. 59 No. 4 2013
zastosowania zielonej herbaty, dane dotyczące bezpieczeństwa jak i interakcji preparatu
roślinnego i leku syntetycznego są bardzo ograniczone. Celem badania była ocena wpływu
standaryzowanego ekstraktu z zielonej herbaty (GTE) zawierającego 61% katechin i 0,1%
kofeiny na poziom ekspresji szczurzych genów CYP i czynników transkrypcyjnych stosując
technikę real-time PCR. Wyniki wykazały, że GTE znacznie obniża poziom ekspresji
CYP2C6 o 68% (p<0,001). W przypadku CYP3A1 i CYP3A2 poziom mRNA tych genów był
również redukowany przez ekstrakt, ale w mniejszym stopniu w porównaniu do CYP2C6.
Istotny wzrost w poziomie mRNA obserwowano dla czynników CAR, RXR i GR odpowiednio
o 54% (p<0,05), 79% (p<0,001) i 23% (p<0,05) po 10 dniach stosowania ekstraktu. Dodatkowo,
zanotowano niewielki wzrost poziomu ekspresji CYP1A1 o 21% (p>0,05). Brak
istotnych różnic zaobserwowano dla CYP1A2 i CYP2D1/2. W badaniu wykazano również
wzrost ilości transkryptu genu ARNT o 27% (p<0,05) podczas dłuższego stosowania. Ponadto,
ekstrakt z zielonej herbaty wykazał zdolność do stymulacji HNF-1α zarówno po
3, jak i 10 dniach trwania eksperymentu odpowiednio o 30% (p<0,05) i 80% (p<0,001).
Brak zmian obserwowano w przypadku stężenia cDNA dla HNF-4α. Wyniki te sugerują, że
GTE może zmieniać ekspresję enzymów CYP, szczególnie w przypadku CYP2C6 (homolog
ludzki CYP2C9) i może uczestniczyć w klinicznie istotnych reakcjach z lekami metabolizowanymi
przez te enzymy
Involvement of the different extracts from roots of Salvia miltiorrhiza Bunge on acute hypobaric hypoxia-induced cardiovascular effects in rats – preliminary report
The present study was carried out to investigate the protective effects of roots of Salvia miltiorrhiza Bunge on hypobaric hypoxia. Two extracts of S. miltiorrhiza (extract 1: ethanol : water - 50 : 50; extract 2: 96% ethanol) were used. The experiments were performed after 7 consecutive days of administration of the extracts (200 mg/kg b.w., intragastrically) to male Wistar rats. Next, after placing animals for 60 min in the controlled acute hypobaric hypoxia (500 mm Hg) the systolic arterial blood pressure (SAP) in conscious rats, bioelectric heart activity in unconscious rats and analysis of oxidative stress parameters in the blood of rats: malonyldialdehyde (MDA) and lipid peroxidase (LPO) concentration, activity of superoxide dismutase (SOD) or glutathione peroxidase (GPX) were assayed. It was found out that the extract 1 augmented the lowering of SAP shown in hypoxia affected control rats. On the contrary the extract 2 reversed SAP to values obtained in control animals. Moreover, both extracts led to the normalization of hypoxia-induced tachycardia and levels of MDA, LPO and SOD. It seems that the above-mentioned effects are coupled with different active compounds content in the extracts, however more studies are needed to confirm this hypothesis