chat (la - 4a) cho they Ca 4 chat deu CO hoat tinh tren cac chung vi khuan khac nhau vai mup do khac nhaụ Chat 2a, 3a, 4a co hoat tinh khang vi khuan B. subtilis. ChAt la, 2a, 4a bieu hien hopt tinh khang vi khuan Ẹ coll. Ngoai ra, chat la con co hopt tinh khang vi khuan S. aureus.
- Ket qua thu, hoat tinh khang nem dm cac chat la - 4a cho they ca 4 chat deu CO tac dung tren chung nem moc Fusarium oxysporum va
chung nem men Candida albicans. TCF ket qua CO the nhan they tac dung cua chat 2a va 4a tren chung nem mOc Fusarium oxysporum manh hop so vai chat la va 3ạ Nhú vay, 2 nhom the do trong nhan benzen lam tang hoat tinh khang nem cua cac chat.
IM hog tinh khang to bao ung thu,
- Ket qua thí hoat tinh khang to bao ung thu, cua 4 chat (la - 4a) cho they chi 2 chat 2a va
4a co hoat tinh khang to bao ung thu, Hep-G2 vai mik de khac nhaụ Nhú vay, 2 nh6m the clo trong nhan benzen co anh Wang den hoat tinh khang to bao ung thú Hep-G2 dm chat 2a va 4ạ - Kat qua thii, hoat tinh khang to bao ung thu, cua 4 chat (lb - 4b) tren 4 d6ng to bao ung thú ngúai cho they chat lb co hoat tinh khang to bao ung thu, tren 3 d6ng: to bao ung thú ph& A549, to bao ung thú t6, cung Hela va to bao ung thu, buOng trúng OVCAR-8. Chat 2b chi co hoat tinh khang to bao ung thú bueng tru,ng OVCAR-8. Hai chat 3b va 4b kh6ng the hien hopt tinh khang to bao ung thú tren 4 d6ng to bao kiem dinh. vay, khi tren nhan therm dm hap phan aldehyd tham chtira nguyen tu, fluor (6' chat lb) thi hoat tinh khang to bao ung thú tot hen so vai khi thay the nguyen tu, fluoro bai 2 nguyen by clo vi tri ortho va para (6, chat 2b). Cu the la chat lb tac dung tren 3 d6ng to bao ung thú, con chat 2b chi tac dung tren 1 d6ng to bao ung thú. Han ne,a, del vai dong to bao OVCAR-8, chat lb cOng the hien tac dung khang manh hen so vai chat 2b.
Ket IWO
- Da tong hap duvc 8 chat (la - 4a, lb - 4b), trong dO co 4 chat (lb, 2b, 3b, 4b) chúa they cOng b6 trong cac tai lieu tham khao &roc.
- De thu, tac dung khang khuan va xac dinh nOng de 6,c the toi thieu (MIC) cua 4 chat tong hop duvc (la - 4a) vai 4 chung vi khuan kiem dinh gem: Escherichia coli, Pseudomonas aeruginosa, Bacillus subtillis, Staphylococcus aureus. Ket qua cho they 3 chat (2a - 4a) ca hoat tinh manh doi vai chung Bacillus subtillis (vai MIC = 25 ug/m1), 3 chat (la, 3a, 4a) co tac dung tren chung vi khuan kiem dinh Escherichia coli (veil MIC Ian krat là 25, 50, 12,5 Kim!), ngoai ra chat la co hopt tinh khang
Staphylococcus aureus (vai MIC = 50 ug/m1). Da thin tac dung khang nem va xac dinh nOng do Crc the toi thieu (MIC) dm 4 chat (la - 4a) vai 4 chung vi nem kiem dinh gem: Aspergillus niger, Fusarium oxysporum, Saccharomyces cerevisiae, Candida albicans. Ket qua cho they ca 4 chat deu CO hoat tinh khang 2 chung vi nem Fusarium oxysporum (MIC = 25 - 50 ug/m1)va Candida albicans (vai MIC
= 50 ug/m1). De thin tac dung khang met d6ng to bao ung thu, gan ngoai (Hep-G2) cua 4 chat (la - 4a). Ket qua cho they 2 chat 2a va 4a co hoat tinh khang to bao ung thú Hep-G2 vai IC50 In luvt la
• Nghien ciru - Ky. thuOt
4,93 va 3,94 pg/ml. Bon ch6t (lb - 4b) da" du,ac thP, ho@t tinh khang to bao ung thu, trOn 4 dOng to baọ Ket qua cho thy 1 b co ho@t tinh ten 3 clang to bao: ung thu, bung trimg OVCAR-8 (IC50 = 53,7 pg/ml), ung thu, t0, cung Hela (IC50 = 60,6 pg/ml) va ung thú phi A459 (IC50 = 80,4 pg/ml). Ch6t 2b co hopt tinh ten d6ng to bao ung thu, buOng trOng OVCAR-8 vai IC50 = 85,4 pg/ml.
Tai lieu tham khao
1. Nguy8n Quang Oat, NO Mai Anh, Dinh Thi Thanh Hai, Imphea Rith (2001), "TOng hgp va tac Thanh Hai, Imphea Rith (2001), "TOng hgp va tac dung khang khunn, khang nArn cua 5-(5'-nitro-2'- furfuryliden)2-thioxo-4-thiazolidinon va dan ch6t", Tap chi Ducrc hoc, so thang 11, tr. 13-16.
2. Al-Shamama Hussien, Pafahl Magnus (2004), "Preparation of 5-benzylidene rhodanines and analogs "Preparation of 5-benzylidene rhodanines and analogs
as antidiabetes and antitumor agents", J. Virol, Vol. 17
(2), PP. 759-762.
3. Goodman and Gilman's (2001), The
Pharmacological basic of therapeutics, pp. 1389 —
1392, Mc Graw - Hill Medical Publishing Division, 10th
edition, Vol. IỊ
4. HanChen, Yun-HuaFan,Ạ N...(2004), "Synthesis and biological evaluation of thiazolidine-2,4-dion and 2,4-thiazolidine derivatives as inhibitors of translation
invitation", Bioorganic & Medicinal Chemistry Letters,
V0. 14, issue 21, pp. 5401 — 5405.
5. Habib N. S., Rida S. M., Badaway Ẹ Ạ M. (1997), "Synthesis and antimicrobial activity of rhodanin "Synthesis and antimicrobial activity of rhodanin
derivatives", Eur. J. Med. Chem., Vol. 32, pp.759-762.
6. Likhiwitayawuid K., Angerhofer C. K. et al.
(1993), "Methods in cytotoxicity assay", J. Nat. Prod.,
56 (1), 30 — 38.
7. Maria Sol Shmidt et al. (2008) " Simple and efficient microwave assited N-alkylation of !satin", efficient microwave assited N-alkylation of !satin",
Molecules, 13 (4), 831-840.
8. Vlietlinck Ạ J., Vanden Berger D. Ạ (1991), "Screening method for antibacterial and antivirial "Screening method for antibacterial and antivirial
agents from higher plants", Methods in Plants
Biochemistry, 6, 47- 68.
(Ngay nhan bak 30/07/2015 - Ngay duyat clang: 04/09/2015)
Nghien cum tic dung dieu chinh roi loan lipid mau cua the pham roi loan lipid mau cua the pham Sagydi (SAD) tren mo hinh ngoai sinh
chwit cong trang
Nguyen Thi Thtly1, Pham Thi Van Anh2*, Nguyen Duy Nhu3
Tritong Dui hoc. Dtroc. Ha Ntii
2 Thrang Dai hoc Y Ha Nqi " Ging ty TNHH TW. Linh
E-mail: phamthivananhhaikkvahoọcom
Summary
Anti-dyslipidaemic effect of the Sagydi products (SAD) produced from Gynostemma pentaphyllum (Thunb.) Makino (Cucurbitaceae) and Salacia cochichinensis Lour. (Celastraceae) was studied on the dyslipidaemic model in rats with exogenous dyslipidaemiạ SAD was given orally to rats at the daily dose of 0.36 gr/kg and 1.08 gr/kg. At the latter dose (1.08 gr/kg daily) for a course of 4 consecutive weeks, TG decreased (p < 0.05), and TC, LDL-C tended to decrease (p > 0.05). SAD exhibited the anti- dyslipidaemic effect at the daily dose of 0.36 g/kg in dyslipidaemic rats (p <0.05).
Keywords: SAD, Gynostemma pentaphyllum and Salacia cochichinensis, Anti- dyslipidaemic
• Nghien an' - K9 thuOt
DOt yen de
Hien nay ten the giai cOng nhú a Viet Nam, nhieu than dugc da duvc chirng minh c6 tac dung ha lipid mau nhu, ngau tat, nghe, deu carn...I1-5Ị Trong d6, giao c6 lam (Gynostemma pentaphyllum (Thunb.) Makino, Cucurbitaceae) va ch6c mau (Salacia cochichinensis Lour., Celastraceae) da &roc nghien dru chOng minh c6 tac dung dieu chinh rei loan lipid mau khi sir dung dan dOc Tuy nhien khi ph6i hap vai nhau, lieu tac dung dieu chinh rei loan lipid mau c6 tang len? De sang to van de, nghien 03,u &roc ben hanh vai the phem SAD la sky ph& hop giCra cao kho giao c6 lam va cao khO re ch6c mau ten m6 hinh gay rei loan lipid mau (RLLPM). De gOp phen khang dinh tac dyng dieu tri rei loan lipid dm SAD, nghien cO,u thvc hien vai muc
Danh gift tac dung di& chinh roi lopn lipid mau cua the pham SAD tren m6 hinh ngopi sinh 6,
chu6t cong tr6ng.
961 tunyng, nguyen lieu va phunyng phap nghien cOu
Che phem nghien cCru
SAD do C6ng ty TNHH Tue Linh cung cep
dat TCCS, la sly ket hop giCra: Cao khO giao
co lam (Gynostemma pentaphyllum (Thunb.) Makino, Cucurbitaceae) va cao khO re choc mau
(Salacia cochichinensis Lour., Celastraceae) theo ty le 1:1.
°Ong vet nghien cCru
ChuOt cOng tang chung Wistar, khoe manh, trong lacyng tO, 200-300 g, do Vien ye sinh Dich
to Trung úang cung ch. Chudt &roc nuoi On
dinh 5-7 ngay tru,ac khi nghien ci:ru tai phong thi nghiem cua Bd mon Dtroc ly — Truteng Dai hoc Y Ha Ndị
I-16a ch'it va thiet bi nghien cCru
Hod chAt phyc vu nghidn c6v: Cholesterol tinh khiet (Merck — arc), deu lac (tong ty Tru,ang An — Viet Nam), propylthiouracil vien nen 50 mg (Net &roc Rieserstat - Lomapharm Rudolf Lohmann GmbH KG - arc), acid cholic (Sigma — Singapore), Atorvastatin vien nen 20 mg (STADA - Viet Nam), kit dinh lacing cac enzym va chat chuyen hoa trong mau: TC, TG, LDL-C, HDL-C cua Hang Hospitex Diagnostics (Y) va Hang DIALAB GmbH (Ao).
May m6c phyc vy nghien c&u: May Screen master cua Hang Hospitex Diagnostics (Y).
Phwang phh nghien COW
Mo hinh rOi loan lipid mau ngoai sinh dircyc thvc hien: cho chudt cong tang uOng h6n hop au che,a cholesterol (1 ml h6n hop deli cholesterol chira: 0,1 g cholesterol, 0,01 g acid cholic va 0,005 g propylthiouracil) vai lieu 1 m1/100 g can nang m8i ngay vac, buoi sang, trong suOt 4 tuen lien tuc a gay RLLPM. ChuOt cOng dagc chia thanh 5 10, m6i 16 9 con, cac 16 &roc uOng thuOc trong 4 tuen, lieu m6i ngay nhú sau:
Ten Nham Ueng hang ngay
La 1 (n = 9) Chimg sinh hoc UOng nu& cat v6i ding the tich nh6m Wong thu6c
Le 2 (n = 9) LC) m6 hinh UOng him hop dhu cholesterol 1 m1/100 g chuOt, sau 2 gib' uong mirk cat 1 m1/100 g chu6t Chimg &rang