Abstract Book - 3rd International Symposium on Medicinal Plants ...

8.3 Development of Medicinal Plants Extracts Producing Modes
Grubnik Igor, Bondarenko Alena, Gladuch Ievgeniy, and Stepanenko Sergiy
National University of Pharmacy, Kharkiv, Ukraine.
<strong>Abstract</strong>: The relevance of herbal medicine has grown immeasurably the last decade. The
therapeutic effects of many types of herbs used in the present time in medical practice, due to the
presence of various biologically active substances, which at introduction into human body
determine one or another physiological effect. These acting physiologically active substances have
diverse composition and belong to different classes of chemical compounds. The aim of our study
was to determine optimal conditions for extraction of biologically active compounds from herb and
roots of comfrey, fruits of chestnut, sage grass, plantain leaves, violet grass leaves of burdock and
ivy leaves. As a method of extraction remaceration method has been chosen that can effectively
extract the main groups of compounds. We have studied the influence of such factors as the
degree of raw materials grinding, the type of extractant, the ratio of raw material – extractant,
extraction time and temperature. Have investigated raw materials with different particle size. As
extractant have studied solvents of different polarity: hexane, chloroform, ethyl alcohol, wateralcohol
mixtures (containing different amounts of ethanol), purified water. We have investigated
the following raw material – extractant ratio from 1:5 to 1:20. Extraction was carried out at two
temperatures: 25 °C and 95 °C. The evaluation criteria were yield of extractives and the yield of
biologically active substances of different chemical nature. The experiment revealed that at the
extraction of raw materials by 40 % ethyl alcohol yield of extractives and the amount of oxidized
phenols was the highest. By increasing the ratio of raw material to extractant from 1:10 to 1:20
yield of extractives and the amount of oxidized phenols increased slightly. For most types of
medicinal plants has been established optimal ratio of raw material-extractant 1:12. To develop
production technology for dense extracts of plant materials and the selection of the optimum
extraction temperature were obtained extracts in two temperature modes: at room temperature
(each extraction lasted for 12 hours), and at a temperature of 90 °C (each extraction – within 2
hours), the multiplicity of drains 5. The results showed that temperature significantly affects only
the extraction of polysaccharides from plant materials. Basing on the conducted work we have
developed a technology for producing substances from various kinds of medicinal plants and
gained a few series in the laboratory for further study.
Key words: Development, medicinal plants extracts, modes.
8.4 Design and Synthesis of Some Benzoxazolinone Derivatives
F. Guenadil and H. Aichaoui
Laboratoire de Chimie Pharmaceutique, Departement de Biologie Universite´ d'el Tarf 36000, BP
73, El Tarf, Algeria
<strong>Abstract</strong>: Benzoxazolinone (BOA) was first discovered in nature by Virtanen and Hietala as an
anti-Fmariulll factor in rye seedlings. This heterocyclic template has long been known as a
bioisostere of catechol and can be considered a „„privileged scaffold‟‟ in the design of new
pharmacophores. Therapeutic applications of this platform are very broad and range from
analgesic anti-inflammatory compounds to anticocaine and neuroprotective anticonvulsant agents.
In particular, their derivatives 6-benzoyl- Benzoxazolinone (CERM-10194) and its sulfur surrogate
(S-14080) underwent clinical trials as anti-inflammatory analgesics. They were found to inhibit not
only the arachidonic inflammatory cascade, but also to induce the release of an opioid peptide
(possibly endomorphin) in the periphery. On the other hand, Valproic acid (VPA) is a well-known
therapeutic agent that has been for a long time in clinical use for treatment of epilepsy and bipolar
disturbs without significant toxicity. Valproic acid has been recently reported to reduce estradiolinduced
MCF-7 cell proliferation. Thus, in an effort aimed at developing mild and flexible strategies
to design new Benzoxazolinones and synthesize heterocyclic scaffolds to prepare new valuable
building blocks in medicinal chemistry, we devised an efficient method to get access to 6-benzoyl-
3-valproyl-Benzoxazolinone and their corresponding sulfur bioisoster, which are analogs of the
prototypic CERM 10194 and S-14080.
Key words: CERM 10194, derivatives, epilepsy, benzoxazolinone, valproic acid.
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