Study of the Anti-MYC Potential of Lanostane-Type Triterpenes.

One of the most investigated molecular targets for anticancer therapy is the proto-oncogene , which is amplified and thus overexpressed in many types of cancer. Due to its structural characteristics, developing inhibitors for the target has proven to be challenging. In this study, the anti-MYC potential of lanostane-type triterpenes was investigated for the first time, using computational approaches that involved ensemble docking, prediction of structural properties and pharmacokinetic parameters, molecular dynamics (MD), and binding energy calculation using the molecular mechanics-generalized born surface area (MM-GBSA) method.

Exploring the osteogenic potential of semisynthetic triterpenes from Combretum leprosum: An in vitro and in silico study.

Combretum leprosum Mart. is a plant of the Combretaceae family, widely distributed in the Northeast region of Brazil, popularly used as an anti-inflammatory agent, and rich in triterpenes. This study evaluated in vitro and in silico potential osteogenic of two semisynthetic triterpenes (CL-P2 and CL-P2A) obtained from the pentacyclic triterpene 3β,6β,16β-trihydroxylup-20(29)-ene (CL-1) isolated from C.

Pentacyclic triterpene-loaded emulsion stabilized by Agaricus blazei Murill polysaccharides: Factorial design and cytoprotection study.

In this study, pentacyclic triterpene-loaded emulsions were stabilized by polysaccharides from Agaricus blazei Murill mushroom (PAb). The drug-excipient compatibility results by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) showed the absence of physicochemical incompatibilities. The use of these biopolymers at 0.

Biological and Molecular Docking Evaluation of a Benzylisothiocyanate Semisynthetic Derivative From in a Pre-clinical Study of Temporomandibular Joint Pain.

Objective: possesses multiple biological effects and the 4-[(4'--acetyl-α-L- rhamnosyloxy) benzyl] isothiocyanate accounts for them. Based on the original isothiocyanate molecule we obtained a semisynthetic derivative, named 4-[(2',3',4'--triacetyl-α-L-rhamnosyloxy) -benzyl] hydrazine carbothioamide (MC-H) which was safe and effective in a temporomandibular joint (TMJ) inflammatory hypernociception in rats. Therefore, considering that there is still a gap in the knowledge concerning the mechanisms of action through which the MC-H effects are mediated, this study aimed to investigate the involvement of the adhesion molecules (ICAM-1, CD55), the pathways heme oxygenase-1 (HO-1) and NO/cGMP/PKG/K , and the central opioid receptors in the efficacy of the MC-H in a pre-clinical study of TMJ pain.

Whole cells of recombinant CYP153A6-E. coli as biocatalyst for regioselective hydroxylation of monoterpenes.

Optimized recombinant whole cells of E. coli bearing CYP153A6 were employed for catalyzing the hydroxylation of different monoterpene derivatives. In most cases, high selectivity was observed with exclusive hydroxylation of the allylic methyl group bound to the aliphatic ring.

Biocatalytic Approaches for an Efficient and Sustainable Preparation of Polyphenols and Their Derivatives.

Many sectors of industry, such as food, cosmetics, nutraceuticals, and pharmaceuticals, have increased their interest in polyphenols due to their beneficial properties. These molecules are widely found in Nature (plants) and can be obtained through direct extraction from vegetable matrices. Polyphenols introduced through the diet may be metabolized in the human body via different biotransformations leading to compounds having different bioactivities.

Nanoencapsulation of triterpene 3β,6β,16β-trihydroxylup-20(29)-ene from Combretum leprosum as strategy to improve its cytotoxicity against cancer cell lines.

The pentacyclic triterpene 3β,6β,16β-tri-hydroxilup-20(29)-ene is a natural product produced by the Brazilian medicinal plant Combretum leprosum. Its cytotoxicity has been previously reported against breast cancer cell lines. The low water solubility of this natural product, that hampers its bioavailability, motivated the investigation of a new nanoparticle formulation containing the triterpene in order to improve its bioactivity.

Antinociceptive, anti-inflammatory and toxicological evaluation of semi-synthetic molecules obtained from a benzyl-isothiocyanate isolated from Moringa oleifera Lam. in a temporomandibular joint inflammatory hypernociception model in rats.

Inflammation is a key component of many clinical conditions that affect the temporomandibular joint (TMJ) and Moringa oleifera Lam. has been used to treat inflammatory diseases. Here, we evaluated the toxicological effects on mice of a naturally-occurring isothiocyanate from M.

Thiocarbamates from Seeds Bioactive against Virulent and Multidrug-Resistant Species.

Prospect of antibacterial agents may provide an alternative therapy for diseases caused by multidrug-resistant bacteria. This study aimed to evaluate the in vitro bioactivity of seed extracts against 100 vibrios isolated from the marine shrimp . Ethanol extracts at low (MOS-E) and hot (MOS-ES) temperature are shown to be bioactive against 92% and 90% of the strains, respectively.

Stereo and regioselective microbial reduction of the clerodane diterpene 3,12-dioxo-15,16-epoxy-4-hydroxycleroda-13(16),14-diene.

The biotransformation of the clerodane diterpene, 3,12-dioxo-15,16-epoxy-4-hydroxy-cleroda-13(16),14-diene (1), obtained from Croton micans var. argyroglossum (Baill.) Mill.

Secondary metabolite production by the basidiomycete, Lentinus strigellus, under different culture conditions.

The basidiomycete Lentinus strigellus was cultivated in three different culture media and the secondary metabolites produced under different culture conditions were isolated and identified. When cultivated in a liquid medium with peptone, L. strigellus afforded the benzopyrans, 2,2-dimethyl-6-methoxychroman-4-one, 4-hydroxy-2,2-dimethyl-6-methoxychromane and (3R,4S)-3,4-dihydroxy-2,2-dimethyl-6-methoxychromane.

Total NMR assignments of new [C7-O-C7'']-biflavones from leaves of the limonene-carvone chemotype of Lippia alba (Mill) N. E. Brown.

Phytochemical analysis of leaves of the limonene-carvone chemotype of Lippia alba led to the isolation of two biflavonoids with a new structural pattern with an ether linkage: 5,5''-dihydroxy-6,4',6'',3''',4'''-pentamethoxy-[C(7)--O--C(7'')]-biflavone (1) and 4',4,5,5''-tetrahydroxy-6,6'',3'''-trimethoxy-[C(7)--O--C(7'')]-biflavone (2). Structural elucidation of the new compounds was established on the basis of spectral data, through the use of 1D NMR and several 2D shift correlated NMR pulse sequences (COSY, HMQC, HMBC and NOESY).