Nghiên cứu hóa học và thăm dò hoạt tính sinh học của loài thông lá dẹt (pinus krempfii lecomte) và ngũ gia bì hương (acanthopanax trifoliatus L. Merr) - 21

THE NEW CONTRIBUTIONS OF THE THESIS

Thesis title: Study of chemistry and biological activities of Pinus krempfii Lecomte and

Acanthopanax trifoliatus L.Merr. Major: Organic Chemistry Code: 62.44.27.01.

PhD : LeThi Hong Nhung

Supervisor: 1. Assoc. Prof. Trinh Thi Thuy

2. Dr. Nguyen Thanh Tam

Education Insitutions: Institute of Chemistry – Vietnam Academy of Science and Technology.

The new contributions of the thesis:

- This the first time species Pinus krempfii Lecomte has been studied on the chemical constituents and biological in Vietnam.

- Seven compounds named Tectochrysin (PK1), Pinostrobin (PK2), Pinobanksin (PK3), Galangin (PK4), Strobopinin (PK5), Cryptostrobin (PK6), Isolariciresinol (PK7) were isolated and elucidated from the root of Pinus krempfii Lecomte. Among these, two compounds PK4 and PK7 were isolated from this species for the first time.

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- The isolated compounds has been studied on biological activities. The results showed that two compounds PK4 and PK7 have fairly good antioxidant activity (PK7: EC50 = 27,12 g/ml); four compounds: PK3, PK4, PK6 and PK7 exhibited cytotoxic activity on 4 human cancer cell lines including KB, HepG2, Lu MCF7.

- A new lupane-triterpene carboxylic acid named 11α,23-dihydroxy-3-oxo-lup-20(29)- ene-28-oic acid (AT3), together with two known 24-nor-11α-hydroxy-3-oxo-lup-20(29)- ene-28-oic acid (AT1), 24-nor-3α,11α-dihydroxy-lup-20(29)-ene-28-oic acid (AT2) with high content (0.26 and 0.25% of dried plant material, respectively) were isolated from the aerial part of Acanthopanax trifoliatus L.Merr.

Nghiên cứu hóa học và thăm dò hoạt tính sinh học của loài thông lá dẹt (pinus krempfii lecomte) và ngũ gia bì hương (acanthopanax trifoliatus L. Merr) - 21

- Starting from AT1 and AT2, 23 new derivatives, including: 4 ester (AT4-AT7), 1 oxo (AT8), 8 amide (AT9-AT17) derivatives of AT1 and 1 ester (AT18), 8 amide (AT19- AT26), 1 nitrile (AT27) derivatives of AT2 have been synthesized.

- Some of the synthesized compounds have been selected for the cytotoxicity test on 4 human cancer cell lines including KB, HepG2, MCF7 and Lu and antimicrobial assay to Bacillus subtilis for the first time. Among these, compounds AT11, AT12, AT13, AT22

showed stronger cytotoxicity than the parent compounds, especially compound AT22 are six to fifteen times more active than its lead compound on all four tested cell lines with IC50 values are 3,65 ÷ 4,42µg/ml. Three compounds AT11, AT16 and AT18 exhibited inhibitory activity against Bacillus subtilis with average level.



SUPERVISOR


Assoc.Prof. Trinh Thi Thuy Dr. Nguyen Thanh Tam

Hanoi, 30th September 2014

PhD STUDENT


Le Thi Hong Nhung


EDUCCATION INSTITUTION

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