Научная статья на тему 'Phytopharmaceuticals platform as a basis for finding and developing new pharmaceutical substances'

Phytopharmaceuticals platform as a basis for finding and developing new pharmaceutical substances Текст научной статьи по специальности «Фундаментальная медицина»

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Текст научной работы на тему «Phytopharmaceuticals platform as a basis for finding and developing new pharmaceutical substances»

EFFECT OF THE METABOLITES OF MEDICAL PLANTS ON MICROORGANISMS OF HUMAN NORMOFLORA

© Molokhova E.I., Sorokina U.V., ZaporovI.A.

Perm pharmaceutical academy, Russia

The Implementation of metabolites compositions of herbal substances in ingredients of medicine is a current trend in improvement of combined probiotics [1]. The positive influence of polyphenolic fractions of plants on biofilm-formation Escherichia coli is established [2]. However, the influence of bio-substrates on microbial growth and activity of Lacto- and Bifidobacteriuma has been poorly studied so far.

The Influence of the Extractions from Briar (Rosa majalis) and the Roots of Barberry (Berberis vulgaris) received according to O0C.1.4.1.0018.15 [3] on the activity of acid production and the growth of Lactobacillus plantarum 8P-A3, Bifidobacterium bifidum has been experimentally studied [4]. At the same time, it was shown that acidity of extracts have not major impact on the obtained data. The activity of extraction on the level of luminescence was studied on cell population of Escherihia coli lux + [5].

The pronounced stimulating effects on the acid production of Bifidobacterium of the extract of Briar (more than 5,4 times), and of Barberry (more than 2.5 times) were established. Metabolical fractions of

Briar have shown the stimulating effect on growth of lactobacilli (more than 2,67 times) and Bifidobacterium (more than 1,72 times), at the same time the extract of Barberry hasn't impact on growth of bifidobacteria and has inhibited lactobacilli. The stimulating dose-dependent effect of the extract of Barberry on cell population of Escherihia coli lux + was established. The received results demonstrate the modulating influence of the studied extraction on biofilm-forming ability of intestinal bacteria.

References:

1. Kurkin V. A. 2016. Questions of biological, medical and pharmaceutical chemistry. 2:15-21.

2. Samoylova ZYu, Musika NG, Smirnova GV, et al. 2013. News of the Samara scientific center of the Russian Academy of Sciences. 15(3):1424-1425.

3. OFS.1.4.1.0018.15 Infusions and broths.

4. Chistokhina LP. 2004. Perm: Thesis. 171.

5. Pshenichnov RA, Maslennikova IL, Nikitina NM. 2005. Mikrobiolyuminestsention (optimization of sensors and expansion of the sphere of use of reaction). Perm: 76.

PHYTOPHARMACEUTICALS PLATFORM AS A BASIS FOR FINDING AND DEVELOPING NEW PHARMACEUTICAL SUBSTANCES

© Narkevich I.A., Luzhanin V. G., Kartasheva N.S., Povydysh M.N.

St. Petersburg State Chemical-Pharmaceutical Academy, St. Petersburg, Russia

Natural compounds have been used in folk medicine for thousands of years, occupying at present more than 30% of the worlds pharmaceutical market. They possess higher chemical diversity compared to substances obtained by synthetic means, but only a small portion of their pharmacological potential is used by modern medicine. The effect of biologically active substances on plant physiological processes is widely known, and the availability of natural resources and their renewability allow to consider plants as a sources of active molecules that are safe for the pharmaceutical industry.

Phytopharmaceuticals platform created on the basis of the St. Petersburg State Chemical-Pharmaceutical Academy (SPCPA) is regarded as the intellectual, scientific, industrial and logistical platform for research and development of active pharmaceutical and food substances of plant origin, including elements of phytoengineering and providing the full ( closed)

production cycle. This platform consists of 9 structural divisions of the SPCPA: Department of Pharmacognosy, the nursery of medicinal plants, the Department of Organic Chemistry, Center for Quality Control of drugs, Centre of Experimental Pharmacology, Center of Pharmaceutical Technology, as well as dosage forms technology departments, industrial technology of drugs and pharmacology and clinical pharmacology.

The scientific reserve has been formed, the instrumental base and human resources make it possible on the basis of this platform with the help of specialized partners to address the following methodological, technical and technological objectives:

1. Creation of an information and analytical base consisting of plant data, their chemical composition and biological activity.

2. Harvesting of wild or cultivated plant raw material using rules of GACP;

Obzory po kliniceskoj farmacologii i lekarstvennoj terapii [Reviews of clinical pharmacology and drug therapy] vol. 15/2017/suppLement 1

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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

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