Advances in metabolism pathways of theaflavins: digestion, absorption, distribution and degradation.

Theaflavins, a major kind of component in black tea, have been reported to show a variety of biological activities and health effects. However, the unstable chemical properties, low bioavailability and unclear metabolism pathways of theaflavins have left much to be desired in terms of its specific efficacy and applications. This paper provides a comprehensive knowledge on the digestion, absorption, metabolism, distribution and excretion of theaflavins.

Exploration and validation of m7G-related genes as signatures in the immune microenvironment and prognostic indicators in low-grade glioma.

Objectives: Currently, an increasing number of studies are focusing on the impact of m7G modification in cancer. This study aims to investigate the prognostic value of m7G-related genes in low-grade glioma (LGG).

Methods: LGG samples were obtained from the CGGA database, and normal samples were obtained from GTEx.

Integrative analysis of CBR1 as a prognostic factor associated with IDH-mutant glioblastoma in the Chinese population.

Background: Glioblastoma multiforme (GBM) is a common primary intracranial tumor with poor prognosis. Common indicators in the clinical diagnosis of glioma include MGMT promoter methylation, isocitrate dehydrogenase (IDH) mutation, 1p/19q codeletion, and TERT mutation. Among these, IDH mutation is extremely important for GBM diagnosis and treatment.

Understanding the effect of anthocyanins extracted from purple sweet potatoes on alcohol-induced liver injury in mice.

Anthocyanins as antioxidants are potential to protect liver from alcoholic damage, but might be pro-oxidants under certain conditions. In this study, twelve purple sweet potatoes anthocyanins (PSPA) were isolated and their effects on alcohol-induced liver injury were studied. These PSPA were rich in cyanidin derivatives and fed to male C57BL/6 mice as colorants in alcoholic drink with low, median, or high dosages PSPA i.

Design, synthesis, and SAR study of 3-(benzo[d][1,3]dioxol-5-yl)-N-benzylpropanamide as novel potent synergists against fluconazole-resistant Candida albicans.

Based on our previous discovery and SAR study on the lead compounds 7d, 5 and berberine which can significantly enhance the susceptibility of fluconazole against fluconazole-resistant Candida albicans, a series of 3-(benzo[d][1,3]dioxol-5-yl)-N-(substituted benzyl)propanamides were designed, synthesized, and evaluated for their in vitro synergistic activity in combination with fluconazole. The series 2a-f were designed by replacing the amide moiety of the lead compound 7d with retro-amide moiety, and compounds 2a and 2b showed more activity than the lead 7d. Furthermore, introducing biphenyl moiety into series 2d-f afforded series 3a-r, most of which exhibited significantly superior activity to the series 2d-f.

Design, synthesis, and in vitro evaluation of novel antifungal triazoles.

Twenty-nine novel triazole analogues of ravuconazole and isavuconazole were designed and synthesized. Most of the compounds exhibited potent in vitro antifungal activities against 8 fungal isolates. Especially, compounds a10, a13, and a14 exhibited superior or comparable antifungal activity to ravuconazole against all the tested fungi.

Synthesis and Biological Evaluation of Novel 2-Aminonicotinamide Derivatives as Antifungal Agents.

Based on the structures of the reported compounds G884 [N-(3-(pentan-2-yloxy)phenyl)nicotinamide], E1210 [3-(3-(4-((pyridin-2-yloxy)methyl)benzyl)isoxazol-5-yl)pyridin-2-amine], and 10 b [2-amino-N-((5-(3-fluorophenoxy)thiophen-2-yl)methyl)nicotinamide], which inhibit the biosynthesis of glycosylphosphatidylinositol (GPI)-anchored proteins in fungi, a series of novel 2-aminonicotinamide derivatives were designed, synthesized, and evaluated for in vitro antifungal activity. Most of these compounds were found to exhibit potent in vitro antifungal activity against Candida albicans, with MIC values ranging from 0.0313 to 4.

Conventional, ultrasound-assisted, and accelerated-solvent extractions of anthocyanins from purple sweet potatoes.

Purple sweet potatoes (PSPs) are rich in anthocyanins. In this study, we investigated the extraction efficiency of anthocyanins from PSPs using conventional extraction (CE), ultrasound-assisted extraction (UAE), and accelerated-solvent extraction (ASE). Additionally, the effects of these extraction methods on antioxidant activity and anthocyanin composition of PSP extracts were evaluated.

[Derivatization of berberine based on its synergistic antifungal activity with fluconazole against fluconazole-resistant Candida albicans].

Abstract: Our previous work revealed berberine can significantly enhance the susceptibility of fluconazole against fluconazole-resistant Candida albicans, which suggested that berberine has synergistic antifungal activity with fluconazole. Preliminary SAR of berberine needs to be studied for the possibility of investigating its target and SAR, improving its drug-likeness, and exploring new scaffold. In this work, 13-substitutited benzyl berberine derivatives and N-benzyl isoquinoline analogues were synthesized and characterized by 1H NMR and MS.

Design, synthesis, and evaluation of caffeic acid amides as synergists to sensitize fluconazole-resistant Candida albicans to fluconazole.

A series of caffeic acid amides were designed, synthesized, and their synergistic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The title caffeic acid amides 3-30 except 26 exhibited potent activity, and the subsequent SAR study was conducted. Compound 3, 5, 21, and 34c, at a concentration of 1.

Berberine inhibits fluphenazine-induced up-regulation of CDR1 in Candida albicans.

Over-expression of the Candida drug resistance gene CDR1 is a common mechanism generating azole-resistant Candida albicans in clinical isolates. CDR1 is transcriptionally activated through the binding of the transcription factor Tac1p to the cis-acting drug-responsive element (DRE) in its promoter. We previously demonstrated that the combination of fluconazole (FLC) and berberine (BBR) produced significant synergy when used against FLC-resistant C.

Structural optimization of berberine as a synergist to restore antifungal activity of fluconazole against drug-resistant Candida albicans.

We have conducted systematic structural modification, deconstruction, and reconstruction of the berberine core with the aim of lowering its cytotoxicity, investigating its pharmacophore, and ultimately, seeking novel synergistic agents to restore the effectiveness of fluconazole against fluconazole-resistant Candida albicans. A structure-activity relationship study of 95 analogues led us to identify the novel scaffold of N-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)-2-(substituted phenyl)acetamides 7 a-l, which exhibited remarkable levels of in vitro synergistic antifungal activity. Compound 7 d (N-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)-2-(2-fluorophenyl)acetamide) significantly decreased the MIC₈₀ values of fluconazole from 128.

Removal of off-flavours from radish (Raphanus sativus L.) anthocyanin-rich pigments using chitosan and its mechanism(s).

In this paper, we examined the role of chitosan in the removal of off-flavours from radish anthocyanin-rich pigments and studied the mechanisms of the process. Four radish glucosinolates (glucoraphenin, dehydroerucin, glucobrassicin, and glucoerucin) were identified by LC-MSn from root extracts and dehydroerucin was found to be the major glucosinolate in red radish roots. Application of chitosan with 76%, 83% or 89% deacetylation in radish extracts attributed to 26%, 35% or 43% adsorption rate for glucosinolates, and 28%, 26% or 22% for anthocyanins, respectively.

Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.

A phosphate prodrug strategy was investigated to address the problem of poor aqueous solubility of pleuromutilin analogues. Water-soluble phosphate prodrugs 6a, 6b and 6c of pleuromutilin analogues were designed and synthesized. Three compounds all exhibited excellent aqueous solubility (>50mg/mL) at near-neutral pH and sufficient stability in buffer solution.