| 摘要: | 寬筋藤（Lour.）Merr（防己科）是一種廣泛應用於民間醫藥在泰國，馬來西亞，印尼和中國來治療黃疸，風濕，泌尿疾病，而且，尤其是糖尿病，它被視為珍貴的中藥藥材。我們初步生物活性測試表明，甲醇提取物的莖和葉都對這種植物呈劑量依賴效應，刺激胰島素分泌的β細胞。在以前的研究中，五種類型的化合物，其中包括類固醇，類黃酮，benzoquinoid，和酪胺類似物。其中在我們實驗室分離出來的N -formylnornucidferine和cycloeucalenol表明能刺激胰島素分泌的β細胞。所以繼續研究這種植物的化學成分。
寬筋藤之老莖的甲醇抽取物，該抽取物進一步的利用色層層析法與高效液相層析法去進行分離。從該植物分離與純化，共得到四十個化合物，包括 : borapetoside C (DS-01)、borapetoside B (DS-02)、(2R,5R,6R,8R,9S,10S,12S)-15,16-Epoxy-2-hydroxy-6-O-(β-D-glucopyranosyl)-cleroda-3,13(16),14-trien-17,12-olid-18-oic acid methylester (DS-03)、borapetoside F (DS-04)、(2R,5R,6S,9S,10S,12S)-15,16-epoxy-2-hydroxy-6-O-(β-D-glucopyranosyl)-cleroda-3,7,13(16),14-tetraen-17,12-olid-18-oic acid methylester(DS-05)、rumphioside B (DS-06)、(1R,4S,5R,8S,9R,10S,12S)-15,16-epoxy-4-O-(β-D-glucopyranosyl)-cleroda-2,13(16),14-triene-17(12),18(1)-diolide (DS-07)、tinocrisposide A (DS-09)、tinocrisposide B (DS-10)、borapetoside E (DS-11)、borapetoside D (DS-12)、rumphioside I (DS-13)、rumphioside A (DS-08)、rumphioside F (DS-14)、rumphioside C (DS-15)、tinocrisposide C (DS-16)、tinocrisposide D (DS-17)、borapetoside A (DS-18)、borapetol B (D-01)、borapetol A (D-02)、borapetic acid A (D-03)、borapetic acid B (D-04)、borapetic acid C (D-05)、N-formylanonaine (N-01)、N-formylnornuciferine(N-02)、N-acetylanonaine(N-03)、N-acetylnornuciferine(N-04)、N-Demethyl-N-formyldehydronuciferine(N-05)、N-2,3,9-methyltetrahydrocolumbamine (N-06)、N-trans-feruloyltyramine (Am-01)、N-cis-feruloyltyramine (Am-02)、N-trans-caffeoyltyramine (Am-03)、paprazine (Am-04)、trans-isoferulic acid (Am-05)、acantrifoside E (B-01)、3-hydroy-3-methylglutaryl-acantrifoside E(B-02)、apigenin(F-01)、secoisolariciresinol(L-01)、syringaresinol (L-02)、cycloeucalenol(S-01)。
其中DS-09、DS-10、DS-16、DS-17、D-03、D-04、D-05、N-06、B-02為新化合物; N-05、Am-04、N-05、B-01、L-02為首次自寬筋藤屬植物分離而得。利用一維和二維核磁共振光譜和文獻比對去確定這些化合物的結構，並去調查和測試這些化合物的生物活性。上述部分化合物具有回復與增加存活β細胞功能的生物活性。
Tinospora crispa (Lour.) Merr (Menispermaceae) is a folk medicine wildly used in Thailand, Malaysia, Indonesia and China to treat jaundice, rheumatism, urinary disorders, and, especially, diabetes mellitus, which is regarded as valuable herbs in traditional Chinese medicine. Our preliminary bioassay test indicated that the methanol extract of both the stems and leaves of this plant showed a dose-dependent effect to stimulate insulin excretion of beta-cells. In the previous study, five types of compounds, including steroid, flavonoid, benzoquinoid, and tyramine analogues, have been isolated in our laboratory. Among them, N-formylnornucidferine and cycloeucalenol showed the stimulation of insulin secretion of beta-cells. So we continue in the study on chemical constituents of this plant.
The dried stems of Tinospora crispa were extracted with methanol. The extracts were further separated by column chromatography and HPLC. Including forty compounds: borapetoside C (DS-01)、borapetoside B (DS-02)、(2R,5R,6R,8R,9S,10S,12S)-15,16-epoxy-2-hydroxy-6-O-(β-D-glucopyranosyl)-cleroda-3,13(16),14-trien-17,12-olid-18-oic acid methylester (DS-03)、borapetoside F (DS-04)、(2R,5R,6S,9S,10S,12S)-15,16-epoxy-2-hydroxy-6-O-(β-D-glucopyranosyl)-cleroda-3,7,13(16),14-tetraen-17,12-olid-18-oic acid methylester(DS-05)、rumphioside B (DS-06)、(1R,4S,5R,8S,9R,10S,12S)-15,16-epoxy-4-O-(β-D-glucopyranosyl)-cleroda-2,13(16),14-triene-17(12),18(1)-diolide (DS-07)、tinocrisposide A (DS-09)、tinocrisposide B (DS-10)、borapetoside E (DS-11)、borapetoside D (DS-12)、rumphioside I (DS-13)、rumphioside A (DS-08)、rumphioside F (DS-14)、rumphioside C (DS-15)、tinocrisposide C (DS-16)、tinocrisposide D (DS-17)、borapetoside A (DS-18)、borapetol B (D-01)、borapetol A (D-02)、borapetic acid A (D-03)、borapetic acid B (D-04)、borapetic acid C (D-05)、N-formylanonaine (N-01)、N-formylnornuciferine(N-02)、N-acetylanonaine(N-03)、N-acetylnornuciferine(N-04)、N-demethyl-N-formyldehydronuciferine(N-05)、N-2,3,9-methyltetrahydrocolumbamine (N-06)、N-trans-feruloyltyramine (Am-01)、N-cis-feruloyltyramine (Am-02)、N-trans-caffeoyltyramine (Am-03)、paprazine (Am-04)、trans-isoferulic acid (Am-05)、acantrifoside E (B-01)、3-hydroy-3-methylglutaryl-acantrifoside E (B-02)、apigenin(F-01)、secoisolariciresinol(L-01)、syringaresinol (L-02)、cycloeucalenol(S-01)。
Among them, DS-09、DS-10、DS-16、DS-17、D-03、D-04、D-05、N-06 and B-02 are new compounds. Compounds N-05、Am-04、N-05、B-01 and L-02, were found for the first time from the genus of Tinospora. We, herein, reported from the dry stem part. Their structures have been identified by 1D-NMR and 2D-NMR spectra. Some of these compounds with biological activity for increased survival and response of β-cell function. |
