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Abstracts. PHYTOPHARM 2017
3. The study of the chemical composition (phytochemical screening) of the research objects to select the main group of biologically active substances;
4. Standardization of plant raw materials and the development of regulatory documents;
5. Development of technologies for the production of total extracts for each object being studied and isolation of individual compounds;
6. The establishment and confirmation of the structure of molecules by spectral methods of analysis, interpretation, and analysis of data, taking into account the possible isomers;
7. Evaluation of the pharmacological activity of the total extract and individual agents in experimental models of pathological conditions, as well as the study of their general and specific toxicity;
8. Evaluation of the possibility of chemical modification and synthesis of active molecules on the basis of pharmacological studies and computer predictions;
9. Justified choice of a rational formulation and development of technology of drugs based on the target of the pharmaceutical substance;
10. The development of technological schemes for the production of the active pharmaceutical substance, including the full (closed) production cycle (from plant raw materials to the finished product);
11. Development and justification of the composition of phytochemicals for food or pharmaceutical goods.
Solving these problems will allow for a continuous search for new promising natural substances and the development of active pharmaceutical and food substances of plant origin for the treatment and prevention of socially significant diseases. SPCPA is interested in partnership with educational and research institutions for joint solutions of tasks in the field of herbal remedy development and active involvement in the activities of the phytopharmaceutical platform.
ACTIVITY-GUIDED ISOLATION OF ANTI-INFLAMMATORY CONSTITUENTS FROM THE AERIAL PARTS OF THE VIETNAMESE MEDICINAL PLANT HELICTERES HIRSUTA LOUR
© Nguyen T.T.1, Gao X.1, Nikles S.1, Pferschy-Wenzig E.M.1, Kunert O.2, Bauer R.1
11nstitute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz, Graz, Austria; 2 Institute of Pharmaceutical Sciences, Department of Pharmaceutical Chemistry, University of Graz, Graz, Austria
The genus Helicteres (Sterculiaceae family) composes mainly of plants distributed in the tropical parts of Asia and America. It is supposed to have around sixty species, of which seven, including two subspecies, are endemic in Vietnam [1]. Helicteres species described as traditional medicinal plants in Vietnam are used in folk medicine as anti-inflammatory agent, vermifuge, and tonic agents [2]. Previous studies have shown that triterpenoids, flavonoids, and lignans are the major components of Helicteres species. Cucurbitacin B and isocucurbitacin B isolated from Helicteres angustifolia [3] as well as six lignans derived from the stems of Helicteres hirsuta [4] possessed cytotoxicity on cancer cell lines.
The purpose of this study was to further investigate the chemical composition, as well as the antiinflammatory activity of Helicteres hirsuta. The aerial parts were successily extracted with solvents of increasing polarities: n-hexane, dichloromethane, ethylacetate and methanol. The extracts were tested in COX-1/COX-2 enzyme inhibition assays in vitro for inhibition of prostaglandin biosynthesis.
The results showed that all extracts exhibited inhibition of COX-1/COX-2 enzymes at 50 ^g/ml with DCM extract being the most potent. Using silica gel column chromatography and semi-preparative HPLC (RP-8, RP-18), three new compounds were isolated. Their structures were elucidated by UV (PDA-HPLC), MS, NMR as 4,4'-sulfinylbis(2-(tert-butyl)-5-methylphenol) (1), 7,4'-di-O-methylisoscutellarein (2) and 7-O-methylisoscutellarein (3), respectively. To our knowledge, this is the first time these compounds have been isolated from this plant. Compound 1 is novel in nature. Investigation to confirm the anti-inflammatory activities of the compounds are in progress.
References:
1. Pham Hoang Ho.1999. Cay co Viet Nam, 1:491-498.
2. Vo Van Chi. 1997:1230-1232.
3. Pana MH, Chen CM, Lee SW. Chen ZT. 2008. Chemistry & Biodiversity. 5:565-574.
4. Chin YW, William P, 2006. Phytotherapy research. 20: 62-65.
Obzory po kliniceskoj farmacologii i lekarstvennoj terapii [Reviews of clinical pharmacology and drug therapy]
vol. 15/2017/suppLement 1
