Cinnamomi Cortex Research Articles

Structures of potent antiulcerogenic compounds from [formula omitted

Three potent antiulcerogenic compounds, cassioside : (4S)-2,4-dimethyl-3-(4'-hydroxy-3'-hydroxymethyl-1'-butenyl)-4-( β-D-glucopyranosyl)methyl-2-cyc cinnamoside : (3R)-4- [(2'R, 4'S)-2'-hydroxy-4'-(β-D-apiofuranosyl-(1 →6)-β-D-glucopyranosyl)-2',6',6'-trimethylcyclo-hexylidene ] -3-buten-2-one and 3,4,5-trimethoxyphenol-β-D-apiofuranosyl-(1 →6)- β-D-glucopyranoside were isolated from a hot water extract of Cinnamomi Cortex ( the dried stem bark of Cinnamomun cassia Blume ) and their structures were determined.

Inhibition of Aldose Reductase Activities by Kampo Medicines

Four kampo medicines, Shu-Jing-Huo-Xie-Tang (SJHXT), Gui-Zhi-Jia-Shu-Fu-Tang (GZJSFT), Niu-Che-Shen-Qi-Wan (NCSQW), and Ba-Wei-Di-Huang-Wan (BWDHW), traditional oriental herb prescriptions, exhibited potent inhibitory activities on rat lens aldose reductase in vitro at the concentration of 0.1 mg/ml using either glucose or DL-glyceraldehyde as a substrate. Four crude drugs, constituents of GZJSFT, Shakuyaku (Paeoniae radix), Kanzo (Glycyrrhizae radix), Sojutsu (Atractyloidis Lanceae rhizoma) and Keihi (Cinnamomi cortex) also inhibited rat lens aldose reductase activities at the concentration of 0.1 mg/ml in vitro. When these kampo medicines and crude drugs were incubated with human red blood cells, two kampo medicines (SJHXT, GZJSFT) and two crude drugs (Shakuyaku, Kanzo), significantly inhibited the accumulation of sorbitol within human red blood cells. These results suggest that the effectiveness of these kampo medicines to some of the chronic diabetic complications may be due to the inhibition of aldose reductase activities.

Anti-thrombic actions of 70% methanolic extract and cinnamic aldehyde from cinnamomi cortex.

The anti-thrombic activities of a 70% methanolic extract (CMe) from Cinnamomi Cortex on blood coagulation and fibrinolysis were investigated. CMe prevented the hepatic venous thrombosis in high butter diet-treated rats, and the decreases of blood platelets and fibrinogen in normal rats induced by endotoxin. CMe also inhibited the blood platelet aggregation induced by collagen, arachidonic acid and adenosine diphosphate (ADP) and the conversion of fibrinogen to fibrin induced by thrombin in in vitro experiments. Cinnamic aldehyde, a major. essential oily component of CMe were showed stronger inhibitory activity than that of CMe on the blood coagulation. These results suggest that Cinnamomi Cortex has anti-thrombic activities.

In vitro effect of cinnamic aldehyde, a main component of Cinnamomi Cortex, on human platelet aggregation and arachidonic acid metabolism.

The in vitro effect of cinnamic aldehyde, a main component of Cinnamomi Cortex, on platelet aggregation and arachidonic acid (AA) metabolism in human platelets was studied. Cinnamic aldehyde reduced platelet aggregation of both platelet rich plasma and washed platelets, dose-dependently. This compound also decreased the formation of the metabolites of AA such as thromboxane B2 (TXB2), 12-hydroxy heptadecatrienoic acid and 12-hydroxyeicosatetraenoic acid in collagen-stimulated washed platelets. The conversion of exogenous [14C]AA to cyclooxygenase metabolites or 12-lipoxygenase metabolite was not altered significantly by the addition of cinnamic aldehyde. On the other hand, collagen-induced release of [14C]AA and its metabolites from washed platelets prelabeled with [14C]AA was markedly reduced by the addition of cinnamic aldehyde. These results suggested that cinnamic aldehyde suppressed the release of AA from platelet membrane phospholipids and then reduced the formation of thromboxane A2. This inhibitory effect of cinnamic aldehyde on AA release and TXB2 formation may contribute to reduced platelet aggregation.

Determination of Cinnamomi Cortex by high-performance liquid chromatography

Determination of Cinnamomi Cortex by high-performance liquid chromatography

Inhibitors of angiotensin-converting enzyme in crude drugs. II.

The effects of rhatannin, Chinese gallotannin and tannin fractions isolated from Arecae Semen, Cinnamomi Cortex, Ephedrae Herba, Epimedii Herba. Moutan Cortex, Polygoni avicularis Herba, Potentillae Herba and Rhei Rhizoma on the activities of angiotensin-converting enzyme (ACE) and other six proteases were investigated. These tannin samples had no significant effect on the activity of kallikrein, but all of them inhibited the activities of carboxypeptidase B, leucine aminopeptidase, trypsin and chymotrypsin although to lesser extents as compared to the effects on ACE. On the other hand, all the samples except for Chinese gallotannin and the fraction from Moutan Cortex, enhanced the activity of carboxypeptidase A. All the samples showed non-competitive inhibition patterns with ACE. Rhatannin and the tannin samples obtained from Arecae Semen, Ephedrae Herba, Epimedii Herba, Polygoni avicularis Herba, and Rhei Rhizoma showed more potent inhibitory effects on ACE than the other samples, and their I50 values were 3.7, 1.0, 1.9, 2.9, 1.1, and 1.2 μg/ml, respectively. The apparent Ki value of rhatannin for ACE was 5×10-7M with Bz-Gly-His-Leu as the substrate, and this value is 5 times and 300 times higher than those of SQ 20881 (Ki=1×10-7M) and SQ 14225 (Ki=1.7×10-9M). respectively. Thus, it is suggested that rhatannin and some of the tannin samples obtained from the above crude drugs (which are believed to have hypotensive effects) show high specificity as ACE inhibitors.

Cinncassiol E, A diterpene from the bark of Cinnamomum cassia

Cinncasiol E, a hexacyclic diterpene of a new skeletal type, was isolated from a fraction with antiallergic activity obtained from a water extract of Cinnamomi cortex. Its structure was deduced by spectroscopic methods.

Pharmacological analysis of the traditional Chinese prescription "goreisan-ryo"

Pharmacological activities of "Goreisan", a traditional Chinese prescription, which has been used for nephrosis, nephritis, heart disease and acute disorder of the stomach, were compared with those of the component crude drugs, i.e. Alismatis Rhizoma (I), Polyporus (II), Hoelen (III), Atractylodis Rhizoma (IV) and Cinnamomi Cortex (V). The decoction of each crude drug was administered orally to mice either singly or in combination with other components. As regards diuretic activity, a significant increase in the urine volume was observed only when the decoction was prepared from a mixture of 5 component drugs or that of I and IV. As for an improvement of experimental uremia, only I which was administered singly showed a positive effect, suggesting that the effect of I is diminished in the presence of another drug. Formation of stress gastric ulcer was prevented by the decoction of V, whereas it was promoted by either of I, II, and IV. In view of these results, the significance of the original prescription Goreisan was discussed.

Inhibitors of angiotensin converting enzyme in crude drugs. I.

The effects of rhatannin, Chinese gallotannin and tannin fractions isolated from Arecae Semen, Cinnamomi Cortex, Ephedrae Herba, Epimedii Herba. Moutan Cortex, Polygoni avicularis Herba, Potentillae Herba and Rhei Rhizoma on the activities of angiotensin-converting enzyme (ACE) and other six proteases were investigated. These tannin samples had no significant effect on the activity of kallikrein, but all of them inhibited the activities of carboxypeptidase B, leucine aminopeptidase, trypsin and chymotrypsin although to lesser extents as compared to the effects on ACE. On the other hand, all the samples except for Chinese gallotannin and the fraction from Moutan Cortex, enhanced the activity of carboxypeptidase A. All the samples showed non-competitive inhibition patterns with ACE. Rhatannin and the tannin samples obtained from Arecae Semen, Ephedrae Herba, Epimedii Herba, Polygoni avicularis Herba, and Rhei Rhizoma showed more potent inhibitory effects on ACE than the other samples, and their I50 values were 3.7, 1.0, 1.9, 2.9, 1.1, and 1.2 μg/ml, respectively. The apparent Ki value of rhatannin for ACE was 5×10-7M with Bz-Gly-His-Leu as the substrate, and this value is 5 times and 300 times higher than those of SQ 20881 (Ki=1×10-7M) and SQ 14225 (Ki=1.7×10-9M). respectively. Thus, it is suggested that rhatannin and some of the tannin samples obtained from the above crude drugs (which are believed to have hypotensive effects) show high specificity as ACE inhibitors.

Studies on anti-inflammatory agents. VI. Anti-inflammatory constituents of Cinnamomum sieboldii Meissn (author's transl)

The crude drug"Cinnamomi Cortex"the bark of Cinnamomum cassia BLUME and other plants of the same genus (Lauraceae) is well described in herbals or medicinal books of Chinese medicine, and has been used medicinally from old times. This important crude drug is clinically prescribed for sweating, anti-pyretic, and analgesic effects in many Chinese medicine and widely used for aromatic stomachics as folk remedy or spice in the world. In the course of search for active anti-inflammatory constituents in the crude drugs and plants, an aqueous methanolic (1 : 1, v/v) extract from the bark of Cinnamomum sieboldii MEISSN. was found to have the potent inhibitory activity of the formation of granulation tissue through the screening by the fertile egg method. Exploration on the bark of this plant resulted in the isolation of the known (-)-epicatechin (1), (+)-catechin (2), procyanidin B2 (5), and procyanidin B4 (6), and new compounds named cinnamonol D1 (9), and cinnamonol D2 (10) as their acetates, respectively. The activity increased in the order of monomers, dimers, and trimers.

Constituents of cinnamomi cortex. IV. Structures of cinncassiols C1 glucoside, C2 and C3.

The structures of three novel diterpenes, cinncassiol C1 glucoside (1), cinncassiol C2 (2) and cinncassiol C3 (3), which had been isolated from the fraction exhibiting anticomplement activity of the water extractive of Cinnamomi Cortex, were characterized.

Constituents of cinnamomi cortex. V. Structures of five novel diterpenes, cinncassiols D1,D1 glucoside, D2,D2 glucoside and D3.

The structures of cinncassiol D1 (1), cinncassiol D1 glucoside (2), cinncassiol D2 (3), cinncassiol D2 glucoside (4) and cinncassiol D3 (5), isolated from the fraction exhibiting anti-complement activity of the water extractive of Cinnamomi Cortex (Toko Keihi), have been characterized by means of chemical, spectral and X-ray analyses. They are novel pentacyclic diterpenes with a new skeleton.

Cinncassiol D 1 and its glucoside, novel pentacyclic diterpenes from cinnamomi cortex

A new pentacyclic diterpene with a new skeleton and its glucoside were obtained from the fraction exhibiting anti-complement activity of the water extractive of Cinnamomi Cortex. Their structures were elucidated as 1 and 3 by chemical, spectral and X-ray crystallographic studies.

Cinncassiol C1, a novel type of diterpene from Cinnamomi Cortex.

A new and highly functionalized diterpene, which had been isolated from the water extractive exhibiting anti-allergic activity of Cinnamomi Cortex and named cinncassiol C1, was assigned the full structure VII by chemical, spectral and X-ray crystallographic study.

The constituents of Cinnamomi Cortex. III. Structures of cinncassiol B and its glucoside.

Compounds 7-13 were isolated from the water extractive of Cinnamomi Cortex (the dried bark of Cinnamomum cassia BLUME, "Toko Keihi"in Japanese, Lauraceae), which shows anti-complement activity. Among them, the compounds 7 and 8 were characterized by chemical and spectral means and named cinncassiol B and cinncassiol B 19-O-β-D-glucopyranoside, respectively.

The constituents of cinnamomi cortex. I. Structures of cinncassiol A and its glucoside.

Compounds I-X were isolated from the water extractive of Cinnamomi Cortex, which shows anti-complement activity. Among them, the structures of I-VI were clarified on the basis of chemical and spectral studies. Compounds I and II were identified as cinnzeylanine and cinnzeylanol, respectively. Compounds III and IV were proved to be dehydrated products of I and II, respectively. Compound V was shown to be 19-hydroxylated IV and was named cinncassiol A. VI was identified as cinncassiol A 19-O-β-D-glucopyranoside.

Local anaesthetic action of the Chinese medicine "Saiko-Keiski-To".

The local anaesthetic action of the Chinese herbal medicine „Saiko–Keishi–To” (SK) and its component crude drugs was examined using the sciatic nerve of the frog. The local anaesthetic action of the 2 % solution of SK extract was 0.29 ± 0.08 times that of 0.5 % procaine solution, and 2 % solutions of extracts of Bupleuri Radix, Cinnamomi Cortex and Zingiberis Rhizoma showed 1.65 + 0.22, 1.66 + 0.13 and 0.73 + 0.20 times the 0.5 % procaine effect respectively.

Effect of antacids on the dissolution behavior of tetracycline and methacycline.

The effect of antacids on the dissolution behavior of tetracycline hydrochloride and methacycline hydrochloride from commercial capsules was studied. The dissolution of the tetracyclines was found to be markedly retarded by antacids such as aluminium silicate and magnesium trisilicate. An attempt was made to elucidate the mechanism of this effect. The results suggest that the effects of antacids on the dissolution may be due to the adsorption of the drugs on antacid particles as well as to the increased pH of the medium. A study was also carried out to determine the influence of stomachics using Cinnamomi Cortex as a test material. In dissolution experiments on commercial capsules, a significant dissolution inhibition by the stomachic was found.