Natural compounds are extensively used in the treatment of various diseases. Regular consumption of polyphenols plays an important role in the protection of health by reducing the risk of ...degenerative diseases, including cancer. The evaluation of the cytotoxic effect of the newly obtained multifruit polyphenolic preparation (composed of seven fruit) on T47D and MCF-7 breast cancer cells and MCF-12A normal cells. The PP was produced on the basis of combined ultrafiltrates obtained from chokeberry, raspberry, wild strawberry, apricot, peach, bilberry, and cranberry. The experiments were performed using human mammary gland cancer cell lines T47D (ductal cancer) and MCF-7 (adenocarcinoma) and normal breast cell line MCF-12A. Chromatographic techniques confirmed the highest contribution of cyanidin 3-O-glucoside, p-coumaroyl glucoside and chlorogenic acid in the PP. The PP exhibited dose-dependent cytotoxic effects towards MCF-7 and T47D cancer cell lines (IC50 = 1.2 μg . cm-3) and MCF-12A cells (IC50 = 0.6 μg . cm-3). The MTT cytotoxicity assay and microscopic observations confirmed the cytopathic effect of the PP on cell lines. It is supposed that berry polyphenols interfered with estrogen receptors leading to changes in the production of paracrine growth factors and therefore, PP was less cytotoxic towards the MCF-7 and T47D cell lines than against the MCF-12A cell line.
Gastric cancer (GC) has high incidence rates and constitutes a common cause of cancer mortality. Despite advances in treatment, GC remains a challenge in cancer therapy which is why novel treatment ...strategies are needed. The interest in natural compounds has increased significantly in recent years because of their numerous biological activities, including anti-cancer action. The isolation of the bioactive compounds from Coptis chinensis Franch was carried out with the Centrifugal Partition Chromatography (CPC) technique, using a biphasic solvent system composed of chloroform (CHCl3)—methanol (MeOH)—water (H2O) (4:3:3, v/v) with an addition of hydrochloric acid and trietylamine. The identity of the isolated alkaloids was confirmed using a high resolution HPLC-MS chromatograph. The phytochemical constituents of Coptis chinensis such as berberine, jatrorrhizine, palmatine and coptisine significantly inhibited the viability and growth of gastric cancer cell lines ACC-201 and NCI-N87 in a dose-dependent manner, with coptisine showing the highest efficacy as revealed using MTT and BrdU assays, respectively. Flow cytometry analysis confirmed the coptisine-induced population of gastric cancer cells in sub-G1 phase and apoptosis. The combination of coptisine with cisplatin at the fixed-ratio of 1:1 exerted synergistic and additive interactions in ACC-201 and NCI-N87, respectively, as determined by means of isobolographic analysis. In in vivo assay, coptisine was safe for developing zebrafish at the dose equivalent to the highest dose active in vitro, but higher doses (greater than 10 times) caused morphological abnormalities in larvae. Our findings provide a theoretical foundation to further studies on more detailed mechanisms of the bioactive compounds from Coptis chinensis Franch anti-cancer action that inhibit GC cell survival in in vitro settings.
Plant sources, chemical properties, bioactivities, as well as the synthesis of indigo dye and its derivatives, are reviewed in this paper. These compounds were chosen because of their significant ...benefits and scope of application as both coloring agents in the textile industry and as pharmacologically active natural products. Their use in traditional chinese medicine (TCM) has directed the attention of European researchers and medical doctors alike. The preparation of indigoferous plants--Indigo naturalis is currently about to be introduced into the European Pharmacopoeia.
Although numerous studies have been conducted on ginger extracts and fractions, the data on the pharmacological activity of single constituents of
are still insufficient. To assess the antidementia ...properties of the plant, a thin layer chromatography (TLC)-based bioautography acetylcholinesterase inhibitory assay was performed on the
diethyl ether extract. It led to the recognition of three active inhibitors among volatile constituents of the plant:
-curcumene (A),
-sesquiphellandrene (B) and
zingiberene (C). The identification of the components was possible thanks to the application of a TLC-HPLC-MS interface analysis of active zones and the GC-MS qualitative analysis of the tested samples. Based on the obtained results, the influence of several extraction techniques (hydrodistillation-HD, pressurized liquid extraction or accelerated solvent extraction-ASE, shaking maceration-SM, supercritical fluid extraction-SFE, and ultrasound-assisted extraction-UAE) on the recovery of the active metabolites from plant material was assessed to deliver enriched extracts. As a result, HD and SFE, were found to be the most efficient methods to recover the volatile components and the concentrations of A, B, and C reached 0.51 ± 0.025, 0.77 ± 0.045, and 1.67 ± 0.11 percent, respectively. Only HD and SFE were found to recover monoterpene hydrocarbons from the plant matrix. The remaining techniques provided extracts rich in more complex constituents, like sesquiterpenes.
Breast cancer (BC) is the most common malignancy among women worldwide. In recent years, significant progress has been made in BC therapy. However, serious side effects resulting from the use of ...standard chemotherapeutic drugs, as well as the phenomenon of multidrug resistance (MDR), limit the effectiveness of approved therapies. Advanced research in the BC area is necessary to create more effective and safer forms of therapy to improve the outlook for individuals diagnosed with this aggressive neoplasm. For decades, plants and natural products with anticancer properties have been successfully utilized in treating various medical conditions. Anthraquinone derivatives are tricyclic secondary metabolites of natural origin that have been identified in plants, lichens, and fungi. They represent a few botanical families, e.g., Rhamnaceae, Rubiaceae, Fabaceae, Polygonaceae, and others. The review comprehensively covers and analyzes the most recent advances in the anticancer activity of 1,8-dihydroanthraquinone derivatives (emodin, aloe-emodin, hypericin, chrysophanol, rhein, and physcion) applied both individually, or in combination with other chemotherapeutic agents, in in vitro and in vivo BC models. The application of nanoparticles for in vitro and in vivo evidence in the context of 1,8-dihydroanthraquinone derivatives was also described.
Studies on hydroglycolic (HG) extracts of
(AB)-a less investigated representative of the genus-were performed to determine their potential for cosmetic applications compared to the well-known
(AM). ...Three types of water:polyethylene glycol extracts (1:1, 4:1, 6:1
/
) were obtained from both species and analyzed for their composition by high performance liquid chromatography coupled with mass spectrometry (HPLC-ESI-Q-TOF-MS) and assayed for their biological activities. The study led to the identification of 11 metabolites from different natural product classes with the highest share corresponding to 5-caffeoylquinic acid, axillarin, coumaroylquinic acid isomers and 3-caffeoylquinic acid. The highest antiradical capacity in DPPH and ABTS scavenging assays was shown for HG 4:1 of AB and AM extracts. HG 1:1 extracts from both species inhibited monophenolase and diphenolase activity of tyrosinase, whereas AB HG 4:1 extract showed significant monophenolase inhibition. The highest sun protection factor (SPF) was determined for AM HG 4:1 extract, equal to 14.04 ± 0.17. The AB extracts were cytotoxic for both human keratinocytes HaCaT and A375 melanoma, however HG 1:1 and 4:1 extracts were more cytotoxic for cancer than for noncancerous cells. In conclusion, AB HG 1:1 and 4:1 extracts display significant potential as active cosmetic ingredients.
The main aim of the study was to assess the acetylcholinesterase-inhibitory potential of triterpenoid saponins (astragalosides) found in the roots of
. For this purpose, the TLC bioautography method ...was applied and then the IC
values were calculated for astragalosides II, III and IV (5.9 μM; 4.2 μM, and 4.0 μM, respectively). Moreover, molecular dynamics simulations were carried outto assess the affinity of the tested compounds for POPC and POPG-containing lipid bilayers, which in this case are the models of the blood-brain barrier (BBB). All determined free energy profiles confirmed that astragalosides exhibit great affinity for the lipid bilayer. A good correlation was obtained when comparing the logarithm of n-octanol/water partition coefficient (logPow) lipophilicity descriptor values with the smallest values of free energy of the determined 1D profiles. The affinity for the lipid bilayers changes in the same order as the corresponding logPow values, i.e.,: I > II > III~IV. All compounds exhibit a high and also relatively similar magnitude of binding energies, varying from ca. -55 to -51 kJ/mol. Apositive correlation between the experimentally-determined IC
values and the theoretically-predicted binding energies expressed by the correlation coefficient value equal 0.956 was observed.
The
L. genus has been widely used in traditional medicine in many countries throughout the world. The study aimed to investigate the chemical composition and bioactivity of the hydroethanolic extract ...(50% v/v) obtained by ultrasonication from the aerial flowering parts of
L. (SSE) collected in Almaty region (Southern Kazakhstan). According to RP-HPLC/PDA analysis the leading metabolites of the SSE belonged to polyphenols: chlorogenic acid and its isomers (2.34 mg/g dry extract) and luteolin derivatives (1.49 mg/g dry extract), while HPLC-ESI-QTOF-MS/MS-based qualitative fingerprinting revealed the presence of 17 metabolites, mainly chlorogenic acid and its isomers, flavonoid glycosides, and verbascoside with its derivatives. GC-MS analysis of the volatile metabolites showed mainly the presence of diterpenoids and fatty acid esters. A reduction in the viability of nematodes
sp. was obtained for the SSE concentration of 3.3 mg/mL, while 11.1 mg/mL showed activity comparable to albendazole. The SSE exhibited higher activity against Gram-positive (MIC = 0.5-2 mg/mL) than Gram-negative bacteria and yeast (MIC = 8 mg/mL), exerting bactericidal and fungicidal effects but with no sporicidal activity. The SSE showed some antiviral activity against HCoV-229E replicating in MRC-5 and good protection against the cytopathic effect induced by HHV-1 in VERO. The SSE was moderately cytotoxic towards human cervical adenocarcinoma (H1HeLa) cells (CC
of 0.127 mg/mL after 72 h). This study provides novel information on the SSE extract composition and its biological activity, especially in the context of the SSE as a promising candidate for further antiparasitic studies.
is one of the most frequently used medicinal herbs in Asia. Using rodent seizure models, it was previously shown that
hydroethanolic extract exerts antiseizure activity, but the active constituents ...responsible for this effect have not been determined. In this paper, we demonstrated that
methanolic extract exerts anticonvulsant activity in the pentylenetetrazole (PTZ)-induced hyperlocomotion assay in larval zebrafish. Next, we isolated 6-gingerol (6-GIN)-a major constituent of
. We observed that 6-GIN exerted potent dose-dependent anticonvulsant activity in the PTZ-induced hyperlocomotion seizure assay in zebrafish, which was confirmed electroencephalographically. To obtain further insight into the molecular mechanisms of 6-GIN antiseizure activity, we assessed the concentration of two neurotransmitters in zebrafish, i.e., inhibitory γ-aminobutyric acid (GABA) and excitatory glutamic acid (GLU), and their ratio after exposure to acute PTZ dose. Here, 6-GIN decreased GLU level and reduced the GLU/GABA ratio in PTZ-treated fish compared with only PTZ-bathed fish. This activity was associated with the decrease in
, but not
,
,
,
, and
expression in PTZ-treated fish. Molecular docking to the human NR2B-containing N-methyl-D-aspartate (NMDA) receptor suggests that 6-GIN might act as an inhibitor and interact with the amino terminal domain, the glutamate-binding site, as well as within the ion channel of the NR2B-containing NMDA receptor. In summary, our study reveals, for the first time, the anticonvulsant activity of 6-GIN. We suggest that this effect might at least be partially mediated by restoring the balance between GABA and GLU in the epileptic brain; however, more studies are needed to prove our hypothesis.
By-products of cultivated plants are one of the major environmental concerns worldwide. Due to the high concentration of bioactive chemicals, such waste may be considered hazardous due to the ...interference with the plant growth, deterioration of the drinking water quality or toxic effects on sensitive marine organisms. Moreover, plant-derived by-products, with proper handling, may represent a low-cost source of bioactive compounds potentially important for pharmaceutical and cosmetics industries. The aim of the study was to evaluate the phytochemical composition, antioxidant activity, the influence of tyrosinase activity, in vitro sun protecting factor and cytotoxicity of 15 extracts from peels of five cultivars of Cucurbita maxima and C. moschata. The extracts were prepared using “green solvents” (water, 50% propylene glycol, and 20% ethanol) and ultrasound-assisted extraction. The performed analysis showed that the peel extracts from various cultivars differ significantly in respect to the phytochemical content and activity. The type of solvent also had a significant impact on the extract’s composition and bioactivity. Aqueous peel extracts contained the highest amounts of flavonoids, showed the greatest antioxidant potential and the most significant in vitro SPF values. In vitro studies showed that the analyzed peel extracts are not cytotoxic for human keratinocytes up to the concentration of 1000 µg/mL and thus might be considered as non-irritant for the skin. The study confirms the potential application of peel extracts from Cucurbita spp. cultivars in cosmetic products.
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