acute and subacute toxicity studies on rutin-rich tartary ... · rutin, a type of flavonol, is...

7
175 J Nutr Sci Vitaminol, 61, 175–181, 2015 Rutin, a type of flavonol, is widely distributed in the plant kingdom (14). Some reports have shown that rutin strengthens fragile blood capillaries (5, 6), and has antioxidative (7, 8), antihypertensive (9) and a-glu- cosidase inhibitory activities (10). The clinical effects of rutin-rich food have also been reported; administra- tion leads to reductions in serum myeloperoxidase and cholesterol levels (11), mucosal symptoms, headache and tiredness (11). Among cereals, Tartary buckwheat is known to contain large amounts of rutin (approxi- mately 1–2% [w/w]) in its seeds (12). For this reason, buckwheat has gained attention as a rutin-rich material for food products (13, 14). However, Tartary buckwheat seeds contain markedly higher rutinosidase activity (Fig. 1) (1517). Rutinosidase is a b-glycosidase that releases the disaccharide rutinose from rutin, and Tar- tary buckwheat seeds contain at least two rutinosidase isozymes (1517). The rutinosidase activity in Tartary buckwheat seeds is sufficient to hydrolyze rutin in the flour within a few minutes after the addition of water. Recently, we developed a new variety of Tartary buck- wheat designated ‘Manten-Kirari.’ The rutinosidase activity of ‘Manten-Kirari’ is about two or three orders of magnitude less than that of other Tartary buckwheat varieties (18, 19). Therefore, most of the rutin in ‘Man- ten-Kirari’ will remain present without hydrolysis. As a result, rutin concentration in ‘Manten-Kirari’ dough is much higher when compared to dough from other vari- eties. Wilson et al. (20) reported that intravenous and intraperitoneal injections of 30 to 50 mg/kg in rats and guinea pigs, and intravenous injections in rabbits of 100 to 200 mg/kg, were innocuous. However, to date, foods containing large amounts of rutin, such as ‘Man- ten-Kirari,’ have not been eaten very widely. Therefore, to ensure the safety of ‘Manten-Kirari,’ it is necessary to evaluate its toxicity. In this paper, we assessed the acute and subacute toxicity of ‘Manten-Kirari’ dough. MATERIALS AND METHODS Preparation of flour and investigation of rutin concentra- tion. ‘Manten-Kirari’ flour and common buckwheat flour were obtained using a test mill machine with a flour milling percentage of 63%. Rutin in the flour was extracted three times using methanol containing 0.1% phosphoric acid at 80˚C for 8 h, followed by analysis using HPLC (17). In addition, rutinosidase isozymes in ‘Manten-Kirari’ flour were investigated using the in-gel detection method (21) to confirm the absence of con- taminating rutinosidase in the normal variety, which possesses large amounts of rutinosidase. Acute and Subacute Toxicity Studies on Rutin-Rich Tartary Buckwheat Dough in Experimental Animals Tatsuro SUZUKI 1 , Toshikazu MORISHITA 2 , Takahiro NODA 2 and Koji ISHIGURO 2 1 National Agriculture and Food Research Organization Hokkaido Agricultural Research Center, Hitsujigaoka, Toyohira, Sapporo, Hokkaido 062–8555, Japan 2 National Agriculture and Food Research Organization Hokkaido Agricultural Research Center, Memuro Upland Farming Research Station, Shinsei, Memuro, Kasai-gun, Hokkaido 082–0081, Japan (Received August 4, 2014) Summary In order to investigate the toxicity of rutin-rich dough from the Tartary buck- wheat variety ‘Manten-Kirari,’ acute and subacute toxicity studies (10,000 and 5,000 mg/ kg flour, respectively) were performed using rats. In the acute toxicity study, no toxic symp- toms were observed and no rats died during the test. Body weight in the ‘Manten-Kirari’- treated group was not significantly different when compared with that of the control group. On pathologico-anatomic observation, no unusual symptoms were observed in the ‘Manten- Kirari’-treated group when compared with the control group. In the subacute toxicity study, no toxic symptoms were observed and no rats died during the test. Body weight and food intake in the ‘Manten-Kirari’-treated and common buckwheat groups were not significantly different when compared with the control group. However, some investigated properties, such as urine protein and serum albumin, were significantly different in the ‘Manten-Kirari’ and common buckwheat groups when compared with the control group. However, these changes were not caused by toxicity, but by transient changes. On pathologico-anatomic observation, some abnormalities were observed in the liver, kidneys, heart, lung, bronchi and pituitary gland in some rats. However, the incidental rates in the ’Manten-Kirari’ and common buckwheat groups did not differ when compared to controls. Therefore, these abnormalities may be caused by natural generation. Based on these results, we concluded that dough at a dose of 5,000 mg flour/kg is at a non effect level. Key Words acute toxicity, subacute toxicity, Tartary buckwheat, rutin, food E-mail: [email protected]

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Page 1: Acute and Subacute Toxicity Studies on Rutin-Rich Tartary ... · Rutin, a type of flavonol, is widely distributed in the ... with a positive urine protein test was significantly higher

175

J Nutr Sci Vitaminol, 61, 175–181, 2015

Rutin, a type of flavonol, is widely distributed in the plant kingdom (1–4). Some reports have shown that rutin strengthens fragile blood capillaries (5, 6), and has antioxidative (7, 8), antihypertensive (9) and a-glu-cosidase inhibitory activities (10). The clinical effects of rutin-rich food have also been reported; administra-tion leads to reductions in serum myeloperoxidase and cholesterol levels (11), mucosal symptoms, headache and tiredness (11). Among cereals, Tartary buckwheat is known to contain large amounts of rutin (approxi-mately 1–2% [w/w]) in its seeds (12). For this reason, buckwheat has gained attention as a rutin-rich material for food products (13, 14). However, Tartary buckwheat seeds contain markedly higher rutinosidase activity (Fig. 1) (15–17). Rutinosidase is a b-glycosidase that releases the disaccharide rutinose from rutin, and Tar-tary buckwheat seeds contain at least two rutinosidase isozymes (15–17). The rutinosidase activity in Tartary buckwheat seeds is sufficient to hydrolyze rutin in the flour within a few minutes after the addition of water.

Recently, we developed a new variety of Tartary buck-wheat designated ‘Manten-Kirari.’ The rutinosidase activity of ‘Manten-Kirari’ is about two or three orders of magnitude less than that of other Tartary buckwheat

varieties (18, 19). Therefore, most of the rutin in ‘Man-ten-Kirari’ will remain present without hydrolysis. As a result, rutin concentration in ‘Manten-Kirari’ dough is much higher when compared to dough from other vari-eties. Wilson et al. (20) reported that intravenous and intraperitoneal injections of 30 to 50 mg/kg in rats and guinea pigs, and intravenous injections in rabbits of 100 to 200 mg/kg, were innocuous. However, to date, foods containing large amounts of rutin, such as ‘Man-ten-Kirari,’ have not been eaten very widely. Therefore, to ensure the safety of ‘Manten-Kirari,’ it is necessary to evaluate its toxicity. In this paper, we assessed the acute and subacute toxicity of ‘Manten-Kirari’ dough.

MATERIALS AND METHODS

Preparation of flour and investigation of rutin concentra-tion. ‘Manten-Kirari’ flour and common buckwheat flour were obtained using a test mill machine with a flour milling percentage of 63%. Rutin in the flour was extracted three times using methanol containing 0.1% phosphoric acid at 80˚C for 8 h, followed by analysis using HPLC (17). In addition, rutinosidase isozymes in ‘Manten-Kirari’ flour were investigated using the in-gel detection method (21) to confirm the absence of con-taminating rutinosidase in the normal variety, which possesses large amounts of rutinosidase.

Acute and Subacute Toxicity Studies on Rutin-Rich Tartary Buckwheat Dough in Experimental Animals

Tatsuro Suzuki1, Toshikazu Morishita2, Takahiro Noda2 and Koji Ishiguro2

1 National Agriculture and Food Research Organization Hokkaido Agricultural Research Center, Hitsujigaoka, Toyohira, Sapporo, Hokkaido 062–8555, Japan

2 National Agriculture and Food Research Organization Hokkaido Agricultural Research Center, Memuro Upland Farming Research Station, Shinsei, Memuro, Kasai-gun, Hokkaido 082–0081, Japan

(Received August 4, 2014)

Summary In order to investigate the toxicity of rutin-rich dough from the Tartary buck-wheat variety ‘Manten-Kirari,’ acute and subacute toxicity studies (10,000 and 5,000 mg/kg flour, respectively) were performed using rats. In the acute toxicity study, no toxic symp-toms were observed and no rats died during the test. Body weight in the ‘Manten-Kirari’-treated group was not significantly different when compared with that of the control group. On pathologico-anatomic observation, no unusual symptoms were observed in the ‘Manten-Kirari’-treated group when compared with the control group. In the subacute toxicity study, no toxic symptoms were observed and no rats died during the test. Body weight and food intake in the ‘Manten-Kirari’-treated and common buckwheat groups were not significantly different when compared with the control group. However, some investigated properties, such as urine protein and serum albumin, were significantly different in the ‘Manten-Kirari’ and common buckwheat groups when compared with the control group. However, these changes were not caused by toxicity, but by transient changes. On pathologico-anatomic observation, some abnormalities were observed in the liver, kidneys, heart, lung, bronchi and pituitary gland in some rats. However, the incidental rates in the ’Manten-Kirari’ and common buckwheat groups did not differ when compared to controls. Therefore, these abnormalities may be caused by natural generation. Based on these results, we concluded that dough at a dose of 5,000 mg flour/kg is at a non effect level.Key Words acute toxicity, subacute toxicity, Tartary buckwheat, rutin, food

E-mail: [email protected]

Page 2: Acute and Subacute Toxicity Studies on Rutin-Rich Tartary ... · Rutin, a type of flavonol, is widely distributed in the ... with a positive urine protein test was significantly higher

Suzuki T et al.176

Animals. Crl:CD(SD)(SPF) rats (male and female) were purchased from Charles River Laboratories Japan, Inc. (Yokohama, Japan). Animals were maintained in a room at 2263˚C under a relative humidity of 50620% with a 12 h/12 h light-dark cycle with 13–17 air purges per day. Rats were housed in steel cages. Animal experiments in this study were performed at New Drug Research Center, Inc. (Eniwa, Japan). In addition, all experiments conformed to the relevant laws, and were approved by the Animal Experimental Committee (Nos. 130122A and 130117A).

Acute toxicity. Rats were acclimated for 7 d before the acute test. Healthy rats were randomly divided into two groups (‘Manten-Kirari’ flour and control) with 10 animals (5 males and 5 females in each group). Animals subjected to this test were aged 6 wk, and weighed 184–196 g (males) and 136–154 g (females). Animals were fasted for 15 h. To make dough, the ‘Manten-Kirari’ flour was mixed with 0.5% sodium carboxymethyl cellulose at 250 mg/mL, which was then administrated orally at a dose level of 10,000 mg flour/kg body weight using a gavage. As a control, 0.5% sodium carboxymethyl cellu-lose was administrated. Administration was divided into two doses at 2-h intervals in order to reduce the harm to animals. Clinical signs of the animals were closely observed for the first 4 h, and were observed more than once per day up to 14 d after administration. Animals were weighed just after administration, and at 1, 3, 7, 10 and 14 d after administration. At 14 d after admin-istration, surviving rats were subjected to euthanasia under isoflurane anesthesia with death from exsangui-nation, and were then subjected to pathologico-ana-tomic observation.

Subacute toxicity. Rats were acclimated for 13 d before the subacute test. Healthy rats were randomly divided into three groups (‘Manten-Kirari’ flour, common buckwheat flour and control) with 12 animals (6 males and 6 females in each group). Animals subjected to this test were aged 6 wk. To make dough, ‘Manten-Kirari’ flour was mixed with 0.5% sodium carboxymethyl cellu-lose at 250 mg/mL, and was then administrated orally at a dose of 5,000 mg flour/kg of body weight using a gavage. As a control, 0.5% sodium carboxymethyl cellu-lose was administrated. Administration was performed once per day. Clinical signs of animals were observed more than once per day for 28 d after the beginning of the test. Animals were weighed three times per week in the first week, and twice per week after that. In the final week, 3 h feces and urine were collected individually under fasted conditions. Collected samples were inves-tigated for pH, protein, glucose, occult blood, Ketone

bodies and urobilinogen using test paper (SIMENS Mul-tisticks; Siemens Healthcare Diagnostics Ltd., Malvern, PA). Bilirubin was also investigated using a microscope with Sternheimer-Malbin staining. Subsequently, 21 h urine was also collected individually. Collected samples were subjected to investigation for specific gravity, color and ion concentration (Na, K and Cl). On the final day of administration, after a 15-h fast, we took blood samples under isoflurane anesthesia. Collected blood was sub-jected to investigation for number of leukocytes, num-ber of red cells, hemoglobin content, hematocrit, blood platelet count, neutropenia rate, lymphocyte rate, mono-cyte rate, eosinophile rate, basophil rate and reticulocyte rate using a Sysmex XT-2000iV Automated Hematology Analyzer (Sysmex Corporation, Hyogo, Japan). Plasma was subjected to investigation for prothrombin time and activated partial thromboplastin time using a CA-530 (Sysmex Corporation). In addition, plasma was sub-jected to investigation of total protein concentration, albumin concentration, globulin concentration, glucose concentration, total cholesterol concentration, triglycer-ide concentration, total bilirubin, blood urea nitrogen, creatinine concentration, AST, ALT, g-GTP and ion con-centration (Ca P, Na, K and Cl) using a Hitachi Model 7070 Automated Analyzer (Hitachi, Ltd., Tokyo, Japan). After blood samples were obtained, animals were sub-jected to anesthesia before being sacrificed by exsangui-nation, and then heart, spleen, thymus, lung, salivary glands, liver, kidneys, brain, pituitary gland, adrenal gland, uterus, ovaries and testes were weighed and fixed in 10% formalin solution. In addition, heart, spleen, lung, bronchi, stomach, duodenum, liver, pancreas, kidneys, brain, pituitary gland, adrenal gland, uterus, ovaries and testes were embedded in paraffin, and were subjected to pathologico-anatomic observation using a microscope after staining with hematoxylin-eosin.

Statistical analysis. Statistical analyses were per-formed by the Dunnett test or Kruskal-Wallis H test. p,0.05 was considered to be significant on the Kruskal-Wallis H test, and p,0.05 and ,0.01 were considered to be significant on the Dunnett test.

RESULTS

Rutin concentration in flourRutin concentration of ‘Manten-Kirari’ flour and

common buckwheat flour was 1,570 mg/100 g flour and 18.2 mg/100 g flour, respectively. These rutin con-centrations are usual for each species. In addition, we confirmed that rutin in this dough was not hydrolyzed during administration.

Fig. 1. Rutinosidase activity.

Page 3: Acute and Subacute Toxicity Studies on Rutin-Rich Tartary ... · Rutin, a type of flavonol, is widely distributed in the ... with a positive urine protein test was significantly higher

Toxicity in Rutin-Rich Tartary Buckwheat Dough 177

Acute toxicityIn the acute toxicity study, no rats died. In addition,

no toxic symptoms were observed during the test. The body weight of the ‘Manten-Kirari’-treated group was not significantly different when compared with that of the control group (Fig. 2). On pathologico-anatomic observation, no unusual symptoms were observed in the ‘Manten-Kirari’-treated group when compared with the control group.Subacute toxicity

In the subacute toxicity study, no rats died. In addi-tion, no toxic symptoms were observed during the test. Body weight and food intake in the ‘Manten-Kirari’-treated and common buckwheat groups were not sig-nificantly different when compared with those of the control group (Fig. 3). Food intake in the ‘Manten-Kira-ri’-treated group and common buckwheat group were not significantly different when compared with that of the control group (data not shown). The number of rats with a positive urine protein test was significantly higher in male rats of the ‘Manten-Kirari’ group and female

Fig. 2. Changes in rat body weight in acute toxicity test. A: male, B: female, Bars indicate SD.

Fig. 3. Changes in rat body weight in subacute toxicity test. A: male, B: female, Bars indicate SD.

Tabl

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Page 4: Acute and Subacute Toxicity Studies on Rutin-Rich Tartary ... · Rutin, a type of flavonol, is widely distributed in the ... with a positive urine protein test was significantly higher

Suzuki T et al.178

Tabl

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Page 5: Acute and Subacute Toxicity Studies on Rutin-Rich Tartary ... · Rutin, a type of flavonol, is widely distributed in the ... with a positive urine protein test was significantly higher

Toxicity in Rutin-Rich Tartary Buckwheat Dough 179Ta

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1.5

68

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62

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43

46

12

4.8

0.8

36

0.4

15

.95

60

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2.7

86

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96

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36

61

8.6

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mon

bu

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62

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79

64

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0.8

36

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16

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60

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36

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3.3

36

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Na

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Ca

(mg/

dL)

(mg/

dL)

(mg/

dL)

(mg/

dL)

(mg/

dL)

(mEq

/L)

(mEq

/L)

(mEq

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(mg/

dL)

(mg/

dL)

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67

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91

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19

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57

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Tabl

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66

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0.1

76

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49

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92

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66

0.1

64

Com

mon

bu

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d gr

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0.4

78

60

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2.5

56

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20

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06

0.0

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66

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60

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86

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6

Fem

ale

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trol

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up

0.8

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60

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86

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1‘M

ante

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0.7

99

60

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20

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96

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71

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00

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5C

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61

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60

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60

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30

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76

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46

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0.7

51

60

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11

7.6

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0.8

26

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0.1

73

60

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70

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46

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14

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0.7

89

60

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08

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23

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ante

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29

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Page 6: Acute and Subacute Toxicity Studies on Rutin-Rich Tartary ... · Rutin, a type of flavonol, is widely distributed in the ... with a positive urine protein test was significantly higher

Suzuki T et al.180

Fig. 4. Slight or trace abnormalities on pathologico-anatomic observation. A–D: liver; E–G: kidneys; H: heart; I, J: lung and bronchi; K: pituitary gland; A, C, E, F and J: Common buckwheat-treated group; B, D, G, H, I and K: ‘Manten-Kirari’-treated group. Bar indicates 100 mm.

rats of the common buckwheat group, when compared with the control group (Table 1). The number of rats in which serum albumin was significantly higher in female rats of the common buckwheat group when compared with the control group (Tables 2 and 3). In the common buckwheat group, relative adrenal gland weight was sig-nificantly lower when compared with that of the control group (Table 4). There were no significant differences in the absolute organ weight in the ‘Manten-Kirari’ group and common buckwheat group when compared with the control group (data not shown). There were no sig-nificant differences in other parameters in the ‘Manten-

Kirari’ group and common buckwheat group when compared with the control group (Tables 1–4). Histo-pathologic examination revealed the following minimal or mild findings: minimal cell aggregation in the liver (Fig. 4A), minimal localized cellular infiltration of Glis-son’s capsule in the liver (Fig. 4B), minimal peripheral lobular vacuolation in the liver (lipid droplets) (Fig. 4C), minimal fibrosis near the membrane in the liver (Fig. 4D), minimal localized basophilic changes/atrophy in the renal tubules (Fig. 4E), minimal localized intersti-tial cellular infiltration in the kidneys (Fig. 4F), minimal hyaline cast in the kidneys (Fig. 4G), minimal localized myocardial degeneration/cell aggregation in the heart (Fig. 4H), minimal localized foam cell aggregation in the lungs and bronchi (Fig. 4I), mild localized mineraliza-tion in arterial walls in the lungs and bronchi (Fig. 4J), and minimal cyst in the anterior lobe of the pituitary (Fig. 4K). Figures 4A, C, E, F and J show the common buckwheat treated group, and 4B, D, G, H, I and K show the ‘Manten-Kirari’-treated group. However, we found no important or critical abnormalities on pathologico-anatomic observation.

DISCUSSION

In the subacute toxicity test, the number of rats that were positive for urine protein was significantly higher. However, on pathologico-anatomic observation, there were no important or critical abnormalities in the glom-erulus or renal tubules of the kidneys. This was there-fore regarded as a transient change, and not sample tox-icity. Although a significant increase in serum albumin was observed, the variation was minimal in comparison with physiological variability (Table 3). The incidence of some abnormalities on pathologico-anatomic obser-vation did not differ between the sample and control groups. These findings are considered to be attribut-able to natural occurrences. Based on these results, we concluded that a dose of 5,000 mg flour/kg is at a non effect level.

Common buckwheat has been utilized as a food since the Jomon period, and it is recognized to be safe. In the acute and subacute tests, there were no critical differ-ences between ‘Manten-Kirari’ flour and common buck-wheat flour. In this study, the dose was 10,000 mg/kg for the acute toxicity test and 5,000 mg/kg for the sub-acute toxicity test; in general, this is the maximum limit of this test. In addition, there were no critical differences between the common buckwheat group and the ‘Man-ten-Kirari’ group. Therefore, ‘Manten-Kirari’ flour may be safe at the same level as common buckwheat flour.

AcknowledgmentsWe thank Dr. Y. Mukasa, for his useful advice. We

thank Mr. S. Nakamura, Mr. K. Abe, and Mr. T. Fukaya for preparation of common and Tartary buckwheat. We also thank Ms. K. Fujii, Ms. M. Hayashida, and Ms. T. Ando for technical assistance.

Page 7: Acute and Subacute Toxicity Studies on Rutin-Rich Tartary ... · Rutin, a type of flavonol, is widely distributed in the ... with a positive urine protein test was significantly higher

Toxicity in Rutin-Rich Tartary Buckwheat Dough 181

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