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Cirsium Japonicum
Lipolysis/Fat Burning
For the sake of space, I’ll post the links for this segment and you can read them on your own time.
Cirsium japonicum is one of few plants to contain the flavone glycoside known as cirsimarin (Link: S&T Papers | Asia Science and Technology Portal)
Cirsimarin is an exceptionally lipolytic compound, meaning it contributes to fat burning quite a bit. In fact, researchers found that cirsimarin was 20 times stronger than caffeine for stimulating lipolysis (Link: Lipolytic activity of cirsimarin extracted from M... [Planta Med. 2005] - PubMed - NCBI).
A follow-up published in the “gold standard” Nature magazine found that a low dose of cirsimarin in the murine model was enough to reduce fat mass substantially (Link: http://www.nature.com/ijo/journal/v34/n11/extref/ijo201085x3.doc). This is important because the primary fat lost was white adipose tissue (WAT), which is the main form of fat found in humans. They found that the region of weight loss was visceral adipose tissue (VAT). This is in contrast to Cirsium Oligophyllum, which caused fat loss primarily in subcutaneous adipose tissue (SAT). A combination of the two may be highly preferable for total systemic fat loss. A final effect of cirsimarin was that it was anti-lipogenic. This means that it not only stimulated fat loss but also prevented fat gain, as would be observed in a caloric surplus.
But how did cirsimarin fare in the human model? Almost exactly the same (Link: Total synthesis of cirsimarin and evidence of its lipolytic and antilipogenic activities on human adipocytes). Fat loss was stimulated and fat gain was inhibited. This led the authors to conclude: “Cirsimarin could therefore be considered as an efficient tool in the struggle against excessive adipose tissue deposition and as a potential candidate in the treatment of obesity.”
Cirsimarin isn’t just more lipolytic than caffeine though. It shares the same mechanism as caffeine: adenosine receptor antagonism. It also shares a second mechanism with caffeine: phosphodiesterase inhibition. The difference is that cirsimarin appears to be more potent in these regards where fat loss is concerned (Link: Adenosine-1 active ligands: cirsimarin, a flavone... [J Nat Prod. 1997] - PubMed - NCBI ; Cirsimarin and cirsimaritin, flavonoids of... [J Pharm Pharmacol. 1997] - PubMed - NCBI).
Glucose Disposal Agent (GDA)
Antidiabetic effect of flavones from Cirsium ... [Arch Pharm Res. 2010] - PubMed - NCBI
[h=1]Antidiabetic effect of flavones from Cirsium japonicum DC in diabetic rats.[/h]Liao Z, Chen X, Wu M.
[h=3]Author information[/h][h=3]Abstract[/h]Cirsium japonicum DC is a traditional Chinese herb used along with other herbs to treat hypertension, traumatic hemorrhage, inflammation, and renal cellular injury. Here, we isolated two flavones from Cirsium japonicum DC, pectolinarin and 5,7-dihydroxy-6,4'-dimethoxy flavone (DDMF), and investigated their antidiabetic effect in diabetic rats established by intravenous injection with streptozotocin followed by feeding with high-carbohydrate/high-fat diet. Both pectolinarin and DDMF showed antidiabetic effect in diabetic rats. However, FECJ, a mixture of pectolinarin and DDMF, is more effective than pectolinarin and DDMF in improving the plasma glucose, cholesterol and triglycerides levels in diabetic rats. The altered activities of glucose metabolism-related enzymes in diabetic rats were well reversed after flavone treatment. The plasma adiponectin level was greatly increased in diabetic rats treated with FECJ, while no obvious effect of the flavones on the dysregulated plasma insulin level and expressions of leptin and glucose transporter 4 (GLUT4) was observed. Our data indicated that the flavones improved adiponectin expression, accompanied by restoring of the dysregulated activities of the glucose metabolism-related enzymes, ultimately resulting in well improved glucose and lipid homeostasis. Thus, an antidiabetic effect of Cirsium japonicum DC was revealed in diabetic rats, suggesting the potential benefit of the Cirsium japonicum DC as an alternative in treating diabetes mellitus.
Cirsium Japonicum provides “FECJ,” the mixture of two bioactive flavones that most effectively improves blood glucose and lipids. The primary mechanism of action was through a very large increase in adiponectin expression. Adiponectin is a hormone usually found in high levels in lean individuals and regulates fat loss and glucose disposal.
Antioxidant and antidiabetic activities of ex... [Nutr Res Pract. 2008] - PubMed - NCBI
[h=1]Antioxidant and antidiabetic activities of extracts from Cirsium japonicum roots.[/h]Yin J, Heo SI, Wang MH.
[h=3]Author information[/h][h=3]Abstract[/h]This study investigated the antioxidant activity of methanol (MeOH) and water extracts from roots of Cirsium japonicumin vitro. MeOH extract showed a stronger free radical scavenging activity than water extract. However, both of extracts showed a concentration dependent hydroxyl radical scavenging activity, reducing power and metal chelating ability. MeOH extract had greater phenolic and flavonoid contents than water extract. The antidiabetic activity of these two extracts was evaluated by the alpha-glucosidase inhibition assay. The water extract showed a considerable alpha-glucosidase inhibitory activity. To our knowledge, this may be the first time to report the antioxidant and antidiabetic activities in Cirsium japonicum roots.
This study shows a second method of reduction of plasma glucose: alpha-glucosidase inhibition. This means that if you consume carbohydrates, they will be absorbed at a slower rate (or even blocked to a degree), resulting in an effective lowering of the glycemic index of co-ingested food.
Liver Health
Effects of methanol extract of Cirsium japonic... [Phytother Res. 2004] - PubMed - NCBI
[h=1]Effects of methanol extract of Cirsium japonicum var. ussuriense and its principle, hispidulin-7-O-neohesperidoside on hepatic alcohol-metabolizing enzymes and lipid peroxidation in ethanol-treated rats.[/h]Park JC, Hur JM, Park JG, Kim SC, Park JR, Choi SH, Choi JW.
[h=3]Author information[/h][h=3]Abstract[/h]Effects of the methanol extract of Cirsium japonicum var. ussuriense and hispidulin 7-O-neohesperidoside isolated from the plant on hepatic alcohol-metabolizing enzymes and lipid peroxidation were studied in rats treated with ethanol. Rats treated with 10% alcohol solution for 6 weeks were orally administered with 250 or 500 mg of methanol extract or 10 or 20 mg of hispidulin 7-O-neohesperidoside per kg body weight daily during the last week of ethanol treatment. The administration of the methanol extract of herbal plant and hispidulin 7-O-neohesperidoside in ethanol-treated rats significantly enhanced the activities of hepatic alcohol dehydrogenase, microsomal ethanol-oxidizing system and aldehyde dehydrogenase in a dose-dependent manner. The extract and the compound decreased hepatic lipid peroxidation along with an increase in hepatic content of reduced glutathione. The methanol extract and hispidulin 7-O-neohesperidoside of C. japonicum var. ussuriense also increased the activity of glutathione reductase, but had no effect on gamma-glutamylcysteine synthase. The results suggest that C. japonicum var. ussuriense may alleviate alcoholic toxicity by enhancing ethanol oxidation as well as inhibiting lipid peroxidation, and hispidulin 7-O-neohesperidoside is one of the active substances responsible for the protective effects of this plant.
Interestingly, cirsium japonicum reduces liver stress through enzymatic upregulation but also increases metabolism of alcohol, resulting in less alcoholic toxicity on the liver.
Pectolinarin and Pectolinarigenin of Cirsium... [Biol Pharm Bull. 2008] - PubMed - NCBI
[h=1]Pectolinarin and Pectolinarigenin of Cirsium setidens Prevent the Hepatic Injury in Rats Caused by D-Galactosamine via an Antioxidant Mechanism.[/h]Yoo YM, Nam JH, Kim MY, Choi J, Park HJ.
[h=3]Author information[/h][h=3]Abstract[/h]To identify the hepatoprotective component from the leaves of Cirsium setidens (Compositae), the methanolic extract was divided into two fractions, chloroform and butanol fractions, and their hepatoprotective efficacy was evaluated in a rat model of hepatic injury caused by D-galactosamine (GalN). Hepatoprotective activity was measured by the activity of serum aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), and lactate dehydrogenase (LDH). Glutathione metabolism was measured via biochemical parameters such as glutathione (GSH), glutathione reductase (GR), gamma-glutamylcysteine synthetase (GCS), glutathione S-transferase (GST), and superoxide dismutase (SOD) levels. We subjected the butanol fraction, which had higher activity, to column chromatography to yield pectolinarin, which was further hydrolyzed to yield pectolinarigenin. Administration (10, 20 mg/kg, p.o.) of the main flavonoid glycoside component, pectolinarin, and its aglycone, pectolinarigenin, for 2 weeks significantly decreased the activity levels of AST, ALT, ALP and LDH, indicating that the two compounds have hepatoprotective activity. Pectolinarin and pectolinarigenin also increased activity levels of GSH, GR, GCS, and GST, as well as SOD. The significant effect was only seen in SOD activity. This suggests that the two components exhibit hepatoprotective activity mainly via SOD antioxidant mechanism.
These constituents, also found in Cirsium Japonicum, lowered liver enzymes and markers of damage through multiple mechanisms.
Nitric Oxide Booster
Cirsium japonicum elicits endothelium-depen... [J Ethnopharmacol. 2008] - PubMed - NCBI
[h=1]Cirsium japonicum elicits endothelium-dependent relaxation via histamine H(1)-receptor in rat thoracic aorta.[/h]Kim EY, Jho HK, Kim DI, Rhyu MR.
[h=3]Author information[/h][h=3]Abstract[/h]Cirsium japonicum De Candole is widely used in traditional herbal medicine for the treatment of hemorrhage, hypertension or blood circulation in Korea. In this work, we investigated the vasorelaxant activity of an aqueous extract of C. japonicum whole plant (CjEx) and its possible mechanism in isolated rat thoracic aortic rings constricted with norepinephrine (NE; 300 nmol/l). CjEx elicited an acute relaxation in endothelium-intact rings in a concentration-dependent manner (0.1-1.0 mg/ml). This relaxation was eliminated by the removal of the endothelium and pretreatment with N(G)-nitro-L-arginine (10 micromol/l), methylene blue (1 micromol/l) or diphenylhydramine (10 micromol/l), but indomethacin (10 micromol/l) atropine (100 nmol/l), [D-Pro(2), D-Trp(7,9)] substance P (5 micromol/l) or HOE-140 (10 nmol/l) did not affect the relaxation. The results indicate that the response to CjEx involves enhancement of the nitric oxide-cyclic guanosine monophosphate system, and that it occurs via histamine H(1)-receptor. Our findings may contribute to better understanding of the potential link between the clinical use and its beneficial effects on vascular health.
Cirsium japonicum elevated nitric oxide and may promote both vasodilation and improvements in vascular health.
Anxiety/Depression
A common effect with stimulant consumption, e.g. yohimbine, is increases in anxiety. Thankfully, cirsium japonicum exerts anti-anxiety effects in vivo as well as anti-depressant effects via modulation of the GABA-A receptor.
The ethanol extract of Cirsium japonicum in... [Drug Discov Ther. 2013] - PubMed - NCBI
Luteolin mediates the antidepressant-like eff... [Arch Pharm Res. 2013] - PubMed - NCBI
Cognition
Secondary to inhibition of acetylcholinesterase (same MOA as galantamine) plus reduction of oxidative stress induced by high blood glucose, Cirsium japonicum improved cognition in the murine model.
Luteolin attenuates diabetes-associated cogni... [Brain Res Bull. 2013] - PubMed - NCBI
Bonus for Women: Pre-Menstrual Syndrome
The effects of cirsium japonicum on anxiety and depression, as mentioned above, where confirmed in humans. Females were given cirsium japonicum and they noted lower anxiety and depression associated with PMS.
Luteolin attenuates diabetes-associated cogni... [Brain Res Bull. 2013] - PubMed - NCBI
Lipolysis/Fat Burning
For the sake of space, I’ll post the links for this segment and you can read them on your own time.
Cirsium japonicum is one of few plants to contain the flavone glycoside known as cirsimarin (Link: S&T Papers | Asia Science and Technology Portal)
Cirsimarin is an exceptionally lipolytic compound, meaning it contributes to fat burning quite a bit. In fact, researchers found that cirsimarin was 20 times stronger than caffeine for stimulating lipolysis (Link: Lipolytic activity of cirsimarin extracted from M... [Planta Med. 2005] - PubMed - NCBI).
A follow-up published in the “gold standard” Nature magazine found that a low dose of cirsimarin in the murine model was enough to reduce fat mass substantially (Link: http://www.nature.com/ijo/journal/v34/n11/extref/ijo201085x3.doc). This is important because the primary fat lost was white adipose tissue (WAT), which is the main form of fat found in humans. They found that the region of weight loss was visceral adipose tissue (VAT). This is in contrast to Cirsium Oligophyllum, which caused fat loss primarily in subcutaneous adipose tissue (SAT). A combination of the two may be highly preferable for total systemic fat loss. A final effect of cirsimarin was that it was anti-lipogenic. This means that it not only stimulated fat loss but also prevented fat gain, as would be observed in a caloric surplus.
But how did cirsimarin fare in the human model? Almost exactly the same (Link: Total synthesis of cirsimarin and evidence of its lipolytic and antilipogenic activities on human adipocytes). Fat loss was stimulated and fat gain was inhibited. This led the authors to conclude: “Cirsimarin could therefore be considered as an efficient tool in the struggle against excessive adipose tissue deposition and as a potential candidate in the treatment of obesity.”
Cirsimarin isn’t just more lipolytic than caffeine though. It shares the same mechanism as caffeine: adenosine receptor antagonism. It also shares a second mechanism with caffeine: phosphodiesterase inhibition. The difference is that cirsimarin appears to be more potent in these regards where fat loss is concerned (Link: Adenosine-1 active ligands: cirsimarin, a flavone... [J Nat Prod. 1997] - PubMed - NCBI ; Cirsimarin and cirsimaritin, flavonoids of... [J Pharm Pharmacol. 1997] - PubMed - NCBI).
Glucose Disposal Agent (GDA)
Antidiabetic effect of flavones from Cirsium ... [Arch Pharm Res. 2010] - PubMed - NCBI
[h=1]Antidiabetic effect of flavones from Cirsium japonicum DC in diabetic rats.[/h]Liao Z, Chen X, Wu M.
[h=3]Author information[/h][h=3]Abstract[/h]Cirsium japonicum DC is a traditional Chinese herb used along with other herbs to treat hypertension, traumatic hemorrhage, inflammation, and renal cellular injury. Here, we isolated two flavones from Cirsium japonicum DC, pectolinarin and 5,7-dihydroxy-6,4'-dimethoxy flavone (DDMF), and investigated their antidiabetic effect in diabetic rats established by intravenous injection with streptozotocin followed by feeding with high-carbohydrate/high-fat diet. Both pectolinarin and DDMF showed antidiabetic effect in diabetic rats. However, FECJ, a mixture of pectolinarin and DDMF, is more effective than pectolinarin and DDMF in improving the plasma glucose, cholesterol and triglycerides levels in diabetic rats. The altered activities of glucose metabolism-related enzymes in diabetic rats were well reversed after flavone treatment. The plasma adiponectin level was greatly increased in diabetic rats treated with FECJ, while no obvious effect of the flavones on the dysregulated plasma insulin level and expressions of leptin and glucose transporter 4 (GLUT4) was observed. Our data indicated that the flavones improved adiponectin expression, accompanied by restoring of the dysregulated activities of the glucose metabolism-related enzymes, ultimately resulting in well improved glucose and lipid homeostasis. Thus, an antidiabetic effect of Cirsium japonicum DC was revealed in diabetic rats, suggesting the potential benefit of the Cirsium japonicum DC as an alternative in treating diabetes mellitus.
Cirsium Japonicum provides “FECJ,” the mixture of two bioactive flavones that most effectively improves blood glucose and lipids. The primary mechanism of action was through a very large increase in adiponectin expression. Adiponectin is a hormone usually found in high levels in lean individuals and regulates fat loss and glucose disposal.
Antioxidant and antidiabetic activities of ex... [Nutr Res Pract. 2008] - PubMed - NCBI
[h=1]Antioxidant and antidiabetic activities of extracts from Cirsium japonicum roots.[/h]Yin J, Heo SI, Wang MH.
[h=3]Author information[/h][h=3]Abstract[/h]This study investigated the antioxidant activity of methanol (MeOH) and water extracts from roots of Cirsium japonicumin vitro. MeOH extract showed a stronger free radical scavenging activity than water extract. However, both of extracts showed a concentration dependent hydroxyl radical scavenging activity, reducing power and metal chelating ability. MeOH extract had greater phenolic and flavonoid contents than water extract. The antidiabetic activity of these two extracts was evaluated by the alpha-glucosidase inhibition assay. The water extract showed a considerable alpha-glucosidase inhibitory activity. To our knowledge, this may be the first time to report the antioxidant and antidiabetic activities in Cirsium japonicum roots.
This study shows a second method of reduction of plasma glucose: alpha-glucosidase inhibition. This means that if you consume carbohydrates, they will be absorbed at a slower rate (or even blocked to a degree), resulting in an effective lowering of the glycemic index of co-ingested food.
Liver Health
Effects of methanol extract of Cirsium japonic... [Phytother Res. 2004] - PubMed - NCBI
[h=1]Effects of methanol extract of Cirsium japonicum var. ussuriense and its principle, hispidulin-7-O-neohesperidoside on hepatic alcohol-metabolizing enzymes and lipid peroxidation in ethanol-treated rats.[/h]Park JC, Hur JM, Park JG, Kim SC, Park JR, Choi SH, Choi JW.
[h=3]Author information[/h][h=3]Abstract[/h]Effects of the methanol extract of Cirsium japonicum var. ussuriense and hispidulin 7-O-neohesperidoside isolated from the plant on hepatic alcohol-metabolizing enzymes and lipid peroxidation were studied in rats treated with ethanol. Rats treated with 10% alcohol solution for 6 weeks were orally administered with 250 or 500 mg of methanol extract or 10 or 20 mg of hispidulin 7-O-neohesperidoside per kg body weight daily during the last week of ethanol treatment. The administration of the methanol extract of herbal plant and hispidulin 7-O-neohesperidoside in ethanol-treated rats significantly enhanced the activities of hepatic alcohol dehydrogenase, microsomal ethanol-oxidizing system and aldehyde dehydrogenase in a dose-dependent manner. The extract and the compound decreased hepatic lipid peroxidation along with an increase in hepatic content of reduced glutathione. The methanol extract and hispidulin 7-O-neohesperidoside of C. japonicum var. ussuriense also increased the activity of glutathione reductase, but had no effect on gamma-glutamylcysteine synthase. The results suggest that C. japonicum var. ussuriense may alleviate alcoholic toxicity by enhancing ethanol oxidation as well as inhibiting lipid peroxidation, and hispidulin 7-O-neohesperidoside is one of the active substances responsible for the protective effects of this plant.
Interestingly, cirsium japonicum reduces liver stress through enzymatic upregulation but also increases metabolism of alcohol, resulting in less alcoholic toxicity on the liver.
Pectolinarin and Pectolinarigenin of Cirsium... [Biol Pharm Bull. 2008] - PubMed - NCBI
[h=1]Pectolinarin and Pectolinarigenin of Cirsium setidens Prevent the Hepatic Injury in Rats Caused by D-Galactosamine via an Antioxidant Mechanism.[/h]Yoo YM, Nam JH, Kim MY, Choi J, Park HJ.
[h=3]Author information[/h][h=3]Abstract[/h]To identify the hepatoprotective component from the leaves of Cirsium setidens (Compositae), the methanolic extract was divided into two fractions, chloroform and butanol fractions, and their hepatoprotective efficacy was evaluated in a rat model of hepatic injury caused by D-galactosamine (GalN). Hepatoprotective activity was measured by the activity of serum aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), and lactate dehydrogenase (LDH). Glutathione metabolism was measured via biochemical parameters such as glutathione (GSH), glutathione reductase (GR), gamma-glutamylcysteine synthetase (GCS), glutathione S-transferase (GST), and superoxide dismutase (SOD) levels. We subjected the butanol fraction, which had higher activity, to column chromatography to yield pectolinarin, which was further hydrolyzed to yield pectolinarigenin. Administration (10, 20 mg/kg, p.o.) of the main flavonoid glycoside component, pectolinarin, and its aglycone, pectolinarigenin, for 2 weeks significantly decreased the activity levels of AST, ALT, ALP and LDH, indicating that the two compounds have hepatoprotective activity. Pectolinarin and pectolinarigenin also increased activity levels of GSH, GR, GCS, and GST, as well as SOD. The significant effect was only seen in SOD activity. This suggests that the two components exhibit hepatoprotective activity mainly via SOD antioxidant mechanism.
These constituents, also found in Cirsium Japonicum, lowered liver enzymes and markers of damage through multiple mechanisms.
Nitric Oxide Booster
Cirsium japonicum elicits endothelium-depen... [J Ethnopharmacol. 2008] - PubMed - NCBI
[h=1]Cirsium japonicum elicits endothelium-dependent relaxation via histamine H(1)-receptor in rat thoracic aorta.[/h]Kim EY, Jho HK, Kim DI, Rhyu MR.
[h=3]Author information[/h][h=3]Abstract[/h]Cirsium japonicum De Candole is widely used in traditional herbal medicine for the treatment of hemorrhage, hypertension or blood circulation in Korea. In this work, we investigated the vasorelaxant activity of an aqueous extract of C. japonicum whole plant (CjEx) and its possible mechanism in isolated rat thoracic aortic rings constricted with norepinephrine (NE; 300 nmol/l). CjEx elicited an acute relaxation in endothelium-intact rings in a concentration-dependent manner (0.1-1.0 mg/ml). This relaxation was eliminated by the removal of the endothelium and pretreatment with N(G)-nitro-L-arginine (10 micromol/l), methylene blue (1 micromol/l) or diphenylhydramine (10 micromol/l), but indomethacin (10 micromol/l) atropine (100 nmol/l), [D-Pro(2), D-Trp(7,9)] substance P (5 micromol/l) or HOE-140 (10 nmol/l) did not affect the relaxation. The results indicate that the response to CjEx involves enhancement of the nitric oxide-cyclic guanosine monophosphate system, and that it occurs via histamine H(1)-receptor. Our findings may contribute to better understanding of the potential link between the clinical use and its beneficial effects on vascular health.
Cirsium japonicum elevated nitric oxide and may promote both vasodilation and improvements in vascular health.
Anxiety/Depression
A common effect with stimulant consumption, e.g. yohimbine, is increases in anxiety. Thankfully, cirsium japonicum exerts anti-anxiety effects in vivo as well as anti-depressant effects via modulation of the GABA-A receptor.
The ethanol extract of Cirsium japonicum in... [Drug Discov Ther. 2013] - PubMed - NCBI
Luteolin mediates the antidepressant-like eff... [Arch Pharm Res. 2013] - PubMed - NCBI
Cognition
Secondary to inhibition of acetylcholinesterase (same MOA as galantamine) plus reduction of oxidative stress induced by high blood glucose, Cirsium japonicum improved cognition in the murine model.
Luteolin attenuates diabetes-associated cogni... [Brain Res Bull. 2013] - PubMed - NCBI
Bonus for Women: Pre-Menstrual Syndrome
The effects of cirsium japonicum on anxiety and depression, as mentioned above, where confirmed in humans. Females were given cirsium japonicum and they noted lower anxiety and depression associated with PMS.
Luteolin attenuates diabetes-associated cogni... [Brain Res Bull. 2013] - PubMed - NCBI
