Eriocaulon buergerianum Koern. (Eriocaulaceae) is a herbaceous perennial plants, distributed in China, Korea, the Ryukyus and Japan. Its capitula have been used as a traditional Chinese medicine named ‘Gujingcao’ to disperse brighten eyes, wind-heat, and eliminate nebula. Flavonoids, isoflavones, naphthopyranones, and xanthones are the major constituents of this plant. In our studies on the anti-inflammatory constituents of Formosan plants, many species have been screened for in vitro inhibitory activity on neutrophil pro-inflammatory responses, and E. buergerianum has been found to be an active species. Investigation on CH2Cl2-soluble fraction of the capitula of E.
buergerianum has led to the isolation of a new isoferulylglyceryl ester, (E)-2-hydroxy-3-(3-(4-hydroxy-3-methoxyphenyl)acryloyloxy)propyl nonacosanoate (1), along with 8 known compounds (2–9). The structure of new compound 1 was determined through spectral analyses including extensive 2D NMR data.
Synthesis of TheDerivatives of SinapicAcidWhich Is Separated from
Gynura Bicolor.: The Improvements of The Antioxidant Activity
Shin-Chang-Huang(黃信璋)a，Mei-Ing-Chung(鍾美英)*, a
aFaculty of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan
Gynura bicolor (Roxb.&Willd.) DC is widely distributed in certain areas of Asia and is very popular in vegetarian cuisine in Taiwan. Gynura Bicolor, a perennial plant in Pingtung, Keelung of Taiwan, is a folk medicine in China. The antioxidant activity and treatment of liver diseases have been reported. Furthermore, G. bicolor DC are used as a recipe to treat diabetes mellitus in some parts of China. (anti-hyperglycemic) In our studies, we have isolated some components, such as thymol, sinapic acid etc. from this plant. And then we modify the side chain of these structures with halogen, amide or amine. We have found that some modifications have better antioxidant activity. Whether the antioxidant activity will increase or decrease depends on what we add to the side chain. We hope that we can make better antioxidant activity on sinapic acid by replacing the carboxylic group. As a result, our components and semi-synthesis products demonstrate different outcome about their activity.
Deoxyelephantopin and Its Derivative D35 Inhibit Lung Metastasis of Human Triple-Negative Breast Cancer in Xenograft Mice
Jo-Yu Chen1,2, Yo-Ting Cheng1, Kyoko Nakagawa-Goto3, Kuo-Hsiung Lee4, Lie-Fen Shyur1,*
1 Agricultural Biotechnology Research Center, Academia Sinica, Taipei 115, Taiwan
2 Graduate Institute of Pharmacognosy, College of Medicine, Taipei Medical University, Taipei 110, Taiwan,
3 College of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, JAPAN
4 Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA
Triple-negative breast cancer (TNBC) is a highly metastatic breast cancer, and chemotherapy is the only systemic therapy available for TNBC; however, drug resistance to standard chemotherapeutics is commonly observed. The use of bioactive phytoagent or its derivative, alone or in combination with anti-cancer drug, may provide alternative and promising treatment options. In the current study, we semi-organically synthesized a derivative (designated D35) from a bioactive compound deoxyelephantopin (DET) isolated from medicinal plant Elephantopus scaber (Asteraceae) and investigated their anti-TNBC effects in vitro and in xenograft lung metastasis mouse model using MDA-MB-231 cell line. By employing various assays, including cell viability assay, Boyden chamber, time-lapse microscopy, and immunohistochemistry assay, we observed that D35 exhibited a better effect (2~3.6-fold decreased in effective doses) than DET on inhibiting cell migration, invasion, and respectively. Although the low dose post-treatment with D35-2 did not show substantial activity on inhibiting lung metastasis (9%), PTX-5+D35-2 co-treatment group (alternate administration of PTX-5 and D35-2) greatly reduced lung metastasis to 71%. Our data suggest that DET derivative D35 may have a potential to further development into a complementary or sensitizing agent to chemotherapeutic drug.
Inhibitory effects of pimpinellin from Toddalia asiatica on LPS-induced inflammatory response in RAW264.7 macrophages.
Ching-Ting Huang*1、Shyh-Shyun Huang1、Guan-Jhong Huang2
1 Department of pharmacy, College of pharmacy, China Medical University, Taichung 40402, Taiwan
2 Department of Chinese pharmaceutical Sciences and Chinese Medicine Resources, China Medical University, Taichung 40402, Taiwan
This study was aimed to confirm the anti-inflammatory effects of pimpinellin isolated from Toddalia asiatica (Rutaceae) on lipopolysaccharide (LPS)-induced inflammatory response in RAW264.7 macrophages, which may associated with transcription factor NF-κB. The methods were examined using ELISA assay and western blot analysis. The result shows that pimpinellin could significantly suppress the production of nitrite thought inhibited iNOS protein expression compared with LPS group. And significantly inhibited translocation of NF-κB from cytoplasm to nucleus by decreased IκB degradation in the cytoplasm, which in a dose-dependent manner. In conclusion, the anti-inflammatory effects by pimpinellin in LPS-treated RAW264.7 macrophages were through regulating the NF-κB signaling pathways.
運用 UHPLC/QTOFMS 建立藿香類藥材之指紋圖譜 及其在製劑上的應用
陳佩儀 溫彩玉 盧芬鈴 林美智 施養志* 衛生福利部食品藥物管理署
藿香藥材(AgastachisHerba)基原為植物藿香 Agastacherugosa(Fisch. etMey.) O.
Kuntze 之 乾 燥 地 上 部 ， 廣 藿 香 藥 材 (PogostemonisHerba) 基 原 為 植 物 廣 藿 香 Pogostemoncablin(Blanco) Benth.之乾燥地上部，兩者皆為唇形科(Labiatae)植物，
於外觀型態上相似，但成分具差異，目前臺灣中藥典第二版已將兩者品項分列收 載為藿香及廣藿香藥材。本研究蒐集市售藿香藥材 32 件，廣藿香藥材 11 件，與 本署標本室收藏之對照藥材共同比對以確認基原。樣品經甲醇萃取後，以超高效 液相層析串聯四極桿/飛行式質譜儀（UHPLC/QTOFMS）建立藿香類藥材之指紋圖 譜。分析條件為層析管柱 HALO C18 column (3.0 ×150 mm, 2.7µm)，水和乙腈(均含 0.1 %的甲酸)作移動相，以 0.5 mL /min 流速作梯度沖提，質譜條件設定為正離子 模式。透過一級質譜測定精確分子量與二級質譜斷裂片之資訊，比對文獻資料與 標 準 品 acacetin 、 apigenin 、 apigenin-glucopyranoside 、 pachypodol 、 retusin 、 kaempferol-3,7,4’-trimethylether、patchouli alcohol，成功建立藿香類藥材成分，於 市售藿香製劑中亦可檢驗出相同成分。本方法除作為藥材之基原確認及品質評價，
並可應用於藿香類製劑之基原鑑別，提升檢驗效率及準確度。
利用 Nested PCR-DNA 定序方法鑑定天麻藥材基原及其製劑 呂康祖*, 謝詠筌, 李蕙君, 林美智, 施養志
食品藥物管理署 研究檢驗組
天麻為蘭科多年生寄生草本植物天麻 (Gastrodiaelata Bl.)的塊莖，本研究即利 用 Nested PCR-DNA 定序方法，建立藥材及製劑天麻基原鑑別方法，並藉以了解天 麻基原植物的使用情形。本研究收集來自本署標本室收藏、藥廠價購及赴大陸採 集計 35 件藥材檢體，製劑檢體則購自國內藥廠包括 1 種單方、2 種複方共 7 件天 麻製劑。先以天麻藥材測試多種 DNA 標記，取多種 DNA 標記之共用引子分別進 行 PCR 及定序分析，選出 ITS 片段序列做為鑑別依據，並在 ITS1-5.8S-ITS2 片段 中，再設計專一性引子做 Nested PCR，同時修正不同位置之 primer 設計，使能應 用於不同來源之天麻檢體及中藥製劑，並避免其他藥材成分的干擾。經 Nested PCR 擴增的 ITS 片段大小為 305 bps，經 DNA 定序分析，35 件藥材檢體序列均一致，
確認可以做為天麻鑑定依據。再以此確認之 DNA 序列及 Nested PCR-DNA 定序方 法鑑定製劑檢體，確認可於這些有著多種藥材成分組成的方劑中，專一地鑑定出 製劑中所使用的天麻基原。
Hung-Chi Chang1, Jaw-Chyun Chen2, Jiun-Long Yang3, Hsin-Sheng Tsay4, Jing-Yu Wang2, Chien-Yun Hsiang5, Tin-Yun Ho6*
1. Department of Golden-Ager Industry Management, Chaoyang University of Technology, Taichung, Taiwan;
2. Department of Medicinal Botany and Health Applications, Da-Yeh University, Changhua, Taiwan;
3. Department of Biological Science and Technology, , China Medical University, Taichung, Taiwan;
4. Graduate Institute of Biochemical Sciences and Technology, Chaoyang University of Technology, Taichung, Taiwan;
5. Department of Microbiology, China Medical University, Taichung, Taiwan;
6. Graduate Institute of Chinese Medical Science, China Medical University, Taichung, Taiwan.
Diarrhea diseases constitute one of the most important health problems worldwide.
Particularly in developing countries, a very large number of people, especially young children suffer from the menace. To tackle this problem, the World Health Organization (WHO) has to constitute the Diarrhea Diseases Control Program (DDCP) which guides studies on traditional medicinal practices and preventive measures. Gusuibu, a traditional folk medicine has been claimed to heal certain types of diarrhea. However, so far no scientific study has been carried out on anti-diarrhea mechanism of “Gusiubu”.
The present study was carried out to examine the traditional claim of anti-diarrhea activity of the ethanol extracts of six sources of folk medicinal ferns used as “Gusuibu”.
Inhibitory effects of six sources were evaluated on the LTB and GMI interaction by GM1-enzyme linked immunosorbent assay. Our results indicated that Drynaria fortunei (DF) had no anti-diarrhea effect, while, among the remaining five species, four belonging to family Davalliaceae had significant ability to inhibit LT-induced diarrhea indicating their potential application in the anti-diarrhea remedies.
某教學醫院藥事人員參與中藥材辨識課程之成效 王明傑 李銘嘉 吳安然 吳大圩
佛教慈濟醫療財團法人台北慈濟醫院 藥學部
中藥材的真偽和品質優劣對於中醫治療的成效，有著相當重要的影響。在中 國大陸，由於各種藥材的產地分佈不同，各地民眾用藥習慣相異，地理上的區隔 與資訊的缺乏使得部份中藥材存在著混淆的情況。對於醫院中藥藥劑部門而言，
如何正確辨識中藥材也是藥師訓練的重要課題，但相關的資源卻相對缺乏。近年 來，衛生福利部中醫藥司開始推動台灣市售易混淆中藥材辨識課程，期待可藉由 這類訓練課程，矯正醫療機構中藥執業人員對於中藥材的錯誤認識，某醫院中藥 局主管，在得知有此訓練課程後，即申請院方同意派訓藥師，並評估受訓後之成 效。
該院藥學部中藥局自 98 年至 102 年間選派藥師參與每次為期三天(12 堂課，
24 小時)的辨識訓練課程，以期待能藉由此訓練提升藥師對中藥材正確辨識的能力。
在課程所介紹的約 90 種易混淆誤用品項中，獲知正確的藥材資訊後，即積極向藥 商反映並要求尋找正確取代品。取得正品後，除了盡速更正藥材外，也告知院內 中醫師及藥師品項更新的相關訊息，至於原本的混淆品項，則留作教學用途。在 一系列藥材辨正的過程中，總共更正了基原接近的代用品白花蛇舌草、白茅根、
石斛等 3 項；基原錯誤的誤用品白英、澤蘭等 2 項；功效類似但基原相異的金錢 草、旱蓮草、桑寄生、敗醬草、蒲公英等 5 項以及藥用部位錯誤的夏枯草 1 項，
共計 11 項。
經由以上藥材辨正的成果，可證實此類課程確實可提升醫療機構之中藥執業 藥師正確辨識中藥材的能力，該院中藥局後續並重新調整進貨的標準流程，加強 基原的查核，驗收區備有正品及混淆品的樣品供實物比對，確保進藥正確性。成 效上，實物比對驗收執行後，這些易混淆飲片品項即未再出現錯誤情況，對於病 人用藥之療效與安全可得到更佳的保障。由以上結果，中藥局擬每年派員參加相 關課程，以期待提升所有中藥局藥師中藥材正確辨識之能力，希望分享這樣的經 驗，作為其它醫療機構對中藥執業人員易混淆中藥飲片辨識訓練的參考。
李蕙君 謝詠筌 呂康祖 劉宜祝 林美智 施養志 衛生福利部食品藥物管理署 研究檢驗組
防己藥材之正品基原為防己科植物粉防己(Stephania tetrandra S. Moore)之乾 燥塊根，惟”木防己湯”需使用防己科植物木防己(Cocculus orbiculatus (L.) DC.)，另名 稱相似易混淆藥材尚有日本藥局方所載之防己，實為防己科的漢防己(Sinomenium acutum Rehder et Wilson)之莖及根莖。本研究利用比對 ITS 序列，設計防己科易混 淆之防己及其誤用品藥材通用引子對，可得約 500 鹼基對之產物，將其產物定序 並比較其序列，發現共 18 件標示防己或粉防己之藥材中，有 15 件均能檢出粉防 己藥材序列，僅 3 件藥材檢體未檢出，另以粉防己專一性引子對鑑定結果亦同。
將利用此 2 組引子對開發 Nested PCR 方法以應用於防己製劑之鑑別。
New labdane type diterpene glycosides from Alpinia densespicata Hayata
Li-Jie Zhang1, Huang-Tse Huang1, and Yao-Hau Kuo1, 2, 3, *
1Division of Chinese Materia Medica Development, National Research Institute of Chinese Medicine, Ministry of Health and Welfare, Taipei, 112,
Taiwan.
2Gradaute Institute of Integrated Medicine, China Medical University, Taichuang 400, Taiwan
3Department of Horticulture and Biotechnology, College of Agriculture, Chinese Culture University, Taipei 111, Taiwan.
From the 95% EtOH extract of dried aerial parts of Alpinia densespicata Hayata, fifteen new labdane type diterpene glycosides were isolated. The structures of new isolates were elucidated by 1D, 2D-NMR and HRESIMS data. These isolated new compounds were identified as 3,17-dihydroxy-labda-8(9),13(14)-dien-15,16-olide-3-β- O-(2-rhamonopyranose)-glucopyranoside (1), 3,17-dihydroxy-labda-7(8),13(14)-dien- 15,16-olide-3-β-O-(2-rhamonopyranose)-glucopyranoside (2), 3β,17-dihydroxy-labda- 8(9),12(13)-dien-15-oic acid-3-O-(2-rhamonopyranose)-glucopyranoside (3), 3,17-dihydroxy-labda-7(8),12(13)-dien-15-oic acid-3-β-O-(2-rhamonopyranose)- glucopyranoside (4), 12,17-epoxy-3-hydroxy-17-β-methoxy-labda-13-en-16,15-olide-3- β-O-(2-rhamonopyranose)-glucopyranoside (5), 12,17-epoxy-3-hydroxy-17-α-methoxy- labda-13-en-16,15-olide-3-β-O-(2-rhamonopyranose)-glucopyranoside (6), 12,17- epoxy-3-hydroxy-17-oxo-labda-8(9),13-dien-16,15-olide-3-β-O-(2-rhamonopyranose)-g lucopyranoside (7), 12,17-epoxy-3-hydroxy-7-oxo-labda-8(9),13-dien-16,15-olide-3- β-O-(2-rhamonopyranose)-glucopyranoside (8), 12,17-epoxy-3,9α-dihydroxy-labda- 8(9),13-dien-16,15-olide-3-β-O-(2-rhamonopyranose)-glucopyranoside (9), 12,17- epoxy-3,17α-dihydroxy-labda-8(9),13-dien-16,15-olide-3-β-O-(2-rhamonopyranose)-gl ucopyranoside (10), 3,7β-dihydroxy-labda-8(17),13(14)-dien-15,16-olide-3-β-O- (2-rhamonopyranose)-glucopyranoside (11), 7α-hydroxy-labda-8(αCH3),12(13)-en- 16,15-olide-19 oic acid-19-O-glucopyranoside (12), 7-oxo-polyrhaphin D 3-β-O-glucopyranoside (13), 7-oxo-polyrhaphin D 3-α-O-glucopyranoside (14), 3-hydroxy-7-oxo-labda-8(βCH3),12(13)-en-16,15-olide-3-β-O-glucopyranoside (15), and named alpindenoside E to S, respectively. All the isolates cannot show the anti-inflammatory activity by LPS-induced NO in RAW 264.7 cell and are invalid for
冬蟲夏草二次代謝物之生物活性研究
Studies on the biological activities of secondary metabolites from
Cordyceps sinensis
楊宗憲 1，張伊伶 1，呂尚謙 2,3，劉坤湘2,3，李冠漢1,3*
1嘉南藥理科技大學，藥學系
2嘉南藥理科技大學，化粧品應用與管理系
3嘉南藥理科技大學，新藥創建研究中心
冬蟲夏草具有「中藥之王」之美稱，其菌絲體及子實體具有抗腫瘤、抗氧化、
抗菌、免疫調節等功效，除做為傳統中藥由來已久，近年來經科學實驗分析，證
抗菌、免疫調節等功效，除做為傳統中藥由來已久，近年來經科學實驗分析，證