Propolis (bee glue) is a resinous substance produced by different species of bees i.a. from available plant resins, balsams, and exudates. It is characterized by significant biological activity (e.g., antimicrobial and antioxidant) and phytochemical diversity related to the available plant sources in specific geographical regions. The available scientific literature on propolis is quite extensive; however, there are only a few reports about propolis originating from Georgia. Therefore, our research was focused on the characterization of Georgian propolis in terms of phytochemical composition and antimicrobial/antioxidant activity. Performed research included UHPLC-DAD-MS/MS phytochemical profiling, determination of total phenolic and flavonoid content, antiradical and antioxidant activity (DPPH and FRAP assays) as well as antibacterial activity of propolis extracts obtained using 70% ethanol (70EE). Georgian propolis extracts exhibited strong activity against Gram-positive bacteria (22 mm—disc assay/64 µg/mL—MIC for S. aureus, sample from Imereti) and weaker against Gram-negative strains as well as strong antioxidant properties (up to 117.71 ± 1.04 mgGAE/g in DPPH assay, up to 16.83 ± 1.02 mmol Fe2+/g in FRAP assay for samples from Orgora and Qvakhreli, respectively). The phytochemical profile of Georgian propolis was characterized by the presence of flavonoids, free phenolic acids, and their esters. In most of the samples, flavonoids were the main chemical group (52 compounds), represented mainly by 3-O-pinobanksin acetate, pinocembrin, chrysin, galangin, and pinobanksin. The primary plant precursor of the Georgian bee glue is black poplar (Populus nigra L.) while the secondary is aspen poplar (P. tremula L.).
Using an ethnomedical data approach, some Georgian plants, which are used in Georgian traditional medicine for cancer or non-cancer diseases, were collected and evaluated for cytotoxic activity. The cytotoxic effect of the methanol extracts of species from the genera Galanthus and Leucojum was evaluated in vitro on three human cell lines (Hela, ephitheloid cervix carcinoma; HCT-116, colon carcinoma; HL-60, acute myeloid leukaemia). Cell type cytotoxic specificity was observed for some extracts. Overall, the HCT-116 cells were much more sensitive to most of the extracts than were the other cell lines. Plants that showed pronounced cytotoxic activity will be further evaluated for the possible isolation of active antitumour compounds.
Helicobacter pylori (H. pylori) is considered the most common bacterial pathogen colonizing stomach mucosa of almost half the world’s population and is associated with various gastrointestinal diseases (from digestive problems and ulcers to gastric cancer). A lack of new drugs and a growing number of H. pylori antibiotic-resistant strains is a serious therapeutic problem.As a mixture of natural compounds, propolis has antimicrobial activity based on high concentrations of bioactive polyphenols (mainly flavonoids and phenolic acid derivates). The chemical composition of tested Georgian propolis is characterized by the presence of flavonoids aglycones, and phenolic acid monoesters, e.g., pinobanksin-5-methyl ether, pinobanksin, chrysin, pinocembrin, galangin, pinobanksin-3-O-acetate, pinostrobin and pinobanksin-3-O-butanoate, or isobutanoate and methoxycinnamic acid cinnamyl ester. The anti-H. pylori activity of 70% ethanol water extracts of 10 Georgian propolis samples was evaluated in vitro by MIC (minimal inhibitory concentration) against the reference strain (H. pylori ATCC 43504) and 10 clinical strains with different antibiotic-resistance patterns. The strongest anti-Helicobacter activity (MIC and MBC = 31.3 µg/mL) was observed for propolis from Orgora, Ota, and Vardzia and two from Khaheti. Lower levels of activity (MIC = 62.5 µg/mL) were found in propolis obtained from Qvakhreli and Pasanauri, while the lowest effect was observed for Norio and Mestia (MIC = 125.0 µg/mL). However, despite differences in MIC, all evaluated samples exhibited bactericidal activity. We selected the most active propolis samples for assessment of urease inhibition property. Enzyme activity was inhibited by propolis extracts, with IC50 ranging from 4.01 to 1484.8 µg/mL. Principal component analysis (PCA) and hierarchical fuzzy clustering (dendrograms) coupled with matrix correlation analysis exhibited that the strongest anti-Helicobacter activity was connected with black poplar origin and high flavonoid content of propolis. Samples with lower activity contained higher presence of aspen markers and/or dominance of non-flavonoid polyphenols over flavonoids. In summary, Georgian propolis can be regarded as a source bioactive compounds that can be used as adjuvant in therapy of H. pylori infection.
By using ultrafiltration membrane with a certain porosity, it is possible to achieve selective fractionation of dimeric and monomeric alkaloids at the molecular weight level. With porosity of the membrane 100-150A° and filtration of alcohol extracts of Vinca rosea L. obtained from the aerial part of the plant, selective fractionation was achieved within the molecular masses from M+ 168 to M+ 426. In the fraction of minor alkaloids, a norharman (M+ 168), dihydrositsirikin (M+ 356) and vindorosine (M+ 426) were identified by the method of LC-MS/MS and GC/MS. The fraction of the minor alkaloids showed strong cytotoxic activity against the DLD-1 and WS-1 cell lines (Resazurin test), and according to the Hoechst test, to the cells of all A-549, DLD-1 and WS-1 lines.
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