Band 72, Heft 11-12

Ginkgetin is known to be an anticancer agent in many studies. However, its effectiveness in treating chronic lymphoblastic leukemia (CLL) remains unknown. The present study aimed to evaluate the effects of ginkgetin on the growth of the K562 cell line. The MTT assay was employed to examine the proliferation of K562, and a terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick end labeling (TUNEL) staining was conducted to detect the apoptotic rates. Furthermore, changes of tumor necrosis factor-α (TNF-α) were detected by Western blot analysis. Ginkgetin inhibited the proliferation of K562 cells in a dose- and time-dependent manner. Concentrations of ginkgetin required to induce 50% death of K562 at 24, 48 and 72 h were 38.9, 31.3 and 19.2 μM, respectively. Moreover, treatment of ginkgetin increased K562 apoptosis in vitro along with increased levels of TNF-α. Interestingly, anti-TNF-α antibody prevented ginkgetin-induced K562 cell apoptosis and growth inhibition via deactivation of caspase-8, caspase-9 and caspase-3. Concomitantly, downregulation of TNF-α by etanercept in vivo attenuated ginkgetin-induced inhibitory effects on the tumor growth in an xenograft mouse model. Our results indicate that ginkgetin effectively inhibits K562 cell proliferation, and TNF-α plays a key role in ginkgetin-induced cell apoptosis.

Lepidium meyenii (Walp.), commonly called maca, is an Andean crop belonging to the Brassicaceae family. Maca hypocotils are habitually consumed as customary food as well as traditional remedies for pathological conditions such as infertility. Moreover, the characterization of maca extracts revealed the presence of compounds that are able to modulate the nervous system. Aimed to evaluate the efficacy of L. meyenii in persistent pain, the present study analyzed the effects of a commercial root extract from maca in different animal models reproducing the most common causes of chronic painful pathologies. A qualitative characterization of this commercial extract by high performance liquid chromatography-mass spectrometry and tandem mass spectrometry analyses allowed us to confirm the presence of some macamides known as bioactive constituents of this root and the absence of the main aromatic glucosinolates. The acute oral administration of maca extract is able to reduce mechanical hypersensitivity and postural unbalance induced by the intra-articular injection of monoiodoacetate and the chronic-constriction injury of the sciatic nerve. Furthermore, L. meyenii extract reverts pain threshold alterations evoked by oxaliplatin and paclitaxel. A good safety profile in mice and rats was shown. In conclusion, the present maca extract could be considered as a therapeutic opportunity to relieve articular and neuropathic pain.

A polypeptide band with an apparent molecular weight of 55,000 was phosphorylated in vitro in whole-cell lysates of Trypanosoma equiperdum . This band corresponds to tubulin as demonstrated by immunoprecipitation of the phosphorylated polypeptide from T. equiperdum extracts when anti-α and anti-β tubulin monoclonal antibodies were employed. A parasite protein kinase CK2 was in charge of modifying tubulin given that common mammalian CK2 inhibitors such as emodin and GTP, hindered the phosphorylation of tubulin and exogenously added casein. Interestingly, a divalent cation-dependent translocation of the T. equiperdum tubulin and the CK2 responsible for its phosphorylation was noticed, suggesting a direct interaction between these two proteins. Additionally, this fraction of tubulin and its kinase coeluted using separations based on parameters as different as charge (DEAE-Sepharose anion-exchange chromatography) and size (Sephacryl S-300 gel filtration chromatography). Analyses by non-denaturing polyacrylamide gel electrophoresis and immunoblot of the purified and radioactively labeled fraction containing both tubulin and the CK2 enzyme, established the phosphorylation of a single band that was recognized by anti-CK2 α-subunit and anti-tubulin antibodies. All these findings revealed a physical association between a pool of tubulin and a CK2 in T. equiperdum .

A new series of heterocyclic Schiff bases 2–9 containing indole moiety were synthesized by facile and efficient condensation of indole-3/2/5-carboxaldehyde ( 1a / 1b / 1c ) with different aromatic and heterocyclic primary amines using conventional and/or microwave irradiation methods. The structures of the obtained compounds were assigned by sophisticated spectroscopic and spectrometric techniques (1D-NMR, 2D-NMR and MS). The synthesized compounds were screened for their cytotoxicity and antibacterial activities. In vitro cytotoxicity screening revealed that compound 5 exhibited moderate activity against KB-3-1 cell line (IC 50 =57.7 μM) while 5-indolylimino derivative 7 indicated close to the activity (IC 50 =19.6 μM) in comparison with the positive control (+)-Griseofulvin (IC 50 =19.2 μM), while the tested compounds 5 , 6b , 7 and 9 revealed good or moderate antibacterial activity. In addition, molecular docking study of Schiff bases 2–9 was performed by Molecular Operating Environment (MOE 2014.09) program on the matrix metalloproteinase-8 (MMP-8) (Protein Data Bank (PDB) ID: 1MNC) in an attempt to explore their mode of action as anticancer drugs.

Phytochemical investigation of the aerial parts of Sansevieria trifasciata , one of the most common Dracaenaceae plants, has resulted in the isolation of a new dihydrochalcone derivative named trifasciatine C ( 1 ), four previously unreported steroidal saponins as two pairs of inseparable regioisomers: trifasciatosides K/L ( 2/3 ), M/N ( 4/5 ), together with the known 1,2-(dipalmitoyl)-3- O - β -D-galactopyranosylglycerol ( 6 ), aconitic acid ( 7 ), and 1-methyl aconitic acid ( 8 ). Their structures were elucidated mainly by extensive spectroscopic analysis (1D and 2D nuclear magnetic resonance) and high-resolution electronspray ionization-mass spectrometry, as well as chemical methods and comparison of their spectral data with those of related compounds. Compounds 2/3 and 4/5 were evaluated for their antiproliferative activity on Hela cells, and no significant effect was observed.

The chemical composition of the essential oils from the leaves and fruit of Eucalyptus camaldulensis grown in Mersin, Turkey was analyzed using gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) techniques. The biological activities (antibacterial and antifungal) were examined using the agar well diffusion method. The main leaf oil constituents were p -cymene (42.1%), eucalyptol (1,8-cineole) (14.1%), α-pinene (12.7%) and α - terpinol (10.7%). The main constituents of the fruit oil were eucalyptol (1,8-cineole) (34.5%), p -cymene (30.0%), α-terpinol (15.1%) and α-pinene (9.0%). Our results showed that both types of oils are rich in terms of monoterpene hydrocarbons and oxygenated monoterpenes. The leaf and fruit essential oils of E. camaldulensis significantly inhibited the growth of Gram-positive ( Staphylococcus aureus and Bacillus subtilis ) and Gram-negative ( Escherichia coli and Streptococcus sp.) bacteria (p<0.05). The oils also showed fungicidal activity against Candida tropicalis and C. globrata . Leaf essential oils showed more activity than fruit essential oils, probably due to the higher p-cymene concentration in leaves.

The ability of the fungus Aureobasidium pullulans ATCC 42023 to produce pullulan from hydrolysates of the native grass known as prairie cordgrass was investigated and examined relative to polysaccharide and cell biomass production, yield, and pullulan content of the polysaccharide. A pullulan concentration of 9.7 g l −1 and yield of 0.78 g g −1 was produced by ATCC 42023 when grown for 168 h at 30°C on a phosphate-buffered hydrolysate. The highest biomass level of 7.7 g l −1 was produced by ATCC 42023 after 168 h on a hydrolysate-containing complete medium. The pullulan content of the polysaccharide produced by ATCC 42023 after 168 h on the hydrolysate medium alone was 77%. Unlike what has been observed for other biomass substrates, a polysaccharide with a high pullulan content can be produced at a relatively high yield by a fungus grown on a grass hydrolysate indicating that pullulan could be produced using a biomass-based process.

In plants, the presence and distribution of specialized metabolites during the early stages of development are not documented enough, even though their biosynthesis is one of the most important strategies for survival. In this study, five alkaloids and four acetogenins were detected in Annona muricata L. during early development seedling, including three phases of root emergence and three of seedling formation. Hexane and alkaloid extracts were obtained from each organ, which were analyzed in a gas-mass chromatograph and in a high-performance liquid chromatograph coupled with a photodiode array UV detector (HPLC-DAD). This research shows the presence of the acetogenins cis -uvarimicin IV, mosinone, muricina B, and cis -annonacin-10-one, as well as of the alkaloids reticuline, coreximine, anonaine, asimilobine, and nornuciferine, both groups with a variable organ-specific distribution, related with the formation of organs and tissues.