Ginsenosides Conversion and Anti-Oxidant Activities in Puffed Cultured Roots of Mountain Ginseng

CRMG (Cultured Roots of Mountain Ginseng) have the advantages in scale-up production, safety, and pharmacological efficacies. Though several methods are available for the conversion of major to minor ginsenosides, which has more pharmacological activities, a single step process with high temperature and pressure as a puffing method took place in this study to gain and produce more pharmacologically active compounds. Puffed CRMG exhibited an acceleration of major ginsenosides to minor ginsenosides conversions, and released more phenolic and flavonoid compounds. HPLC analysis was used to detect a steep decrease in the contents of major ginsenosides (Re, Rf, Rg1, Rg2, Rb1, Rb2, Rb3, Rc and Rd) with increasing pressure; on the contrary, the minor ginsenosides (20 (S, R)-Rg3, Rg5, Rk1, Rh1, Rh2, Rg6, F4 and Rk3) contents increased. Minor ginsenosides, such as Rg6, F4 and Rk3, were firstly reported to be produced from puffed CRMG. After the puffing process, phenolics, flavonoids, and minor ginsenoside contents were increased, and also, the antioxidant properties, such as DPPH inhibition and reducing the power of puffed CRMG, were significantly enhanced. Puffed CRMG at 490.3 kPa and 588.4 kPa had a low toxicity on HaCaT (immortalized human epidermal keratinocyte) cells at 200 μg/mL, and could significantly reduce ROS by an average of 60%, compared to the group treated with H2O2. Therefore, single step puffing of CRMG has the potential to be utilized for functional food and cosmeceuticals.

Synthesis and Applications of Carbohydrate-Based Organocatalysts

Organocatalysis is a very useful tool for the asymmetric synthesis of biologically or pharmacologically active compounds because it avoids the use of noxious metals, which are difficult to eliminate from the target products. Moreover, in many cases, the organocatalysed reactions can be performed in benign solvents and do not require anhydrous conditions. It is well-known that most of the above-mentioned reactions are promoted by a simple aminoacid, l-proline, or, to a lesser extent, by the more complex cinchona alkaloids. However, during the past three decades, other enantiopure natural compounds, the carbohydrates, have been employed as organocatalysts. In the present exhaustive review, the detailed preparation of all the sugar-based organocatalysts as well as their catalytic properties are described.

Ethyl Acetate Fractions of Papaver rhoeas L. and Papaver nudicaule L. Exert Antioxidant and Anti-Inflammatory Activities

Abnormal inflammation and oxidative stress are involved in various diseases. Papaver rhoeas L. possesses various pharmacological activities, and a previously reported analysis of the anti-inflammatory effect of P. nudicaule ethanol extracts and alkaloid profiles of the plants suggest isoquinoline alkaloids as potential pharmacologically active compounds. Here, we investigated anti-inflammatory and antioxidant activities of ethyl acetate (EtOAc) fractions of P. nudicaule and P. rhoeas extracts in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. EtOAc fractions of P. nudicaule and P. rhoeas compared to their ethanol extracts showed less toxicity but more inhibitory activity against LPS-induced nitric oxide production. Moreover, EtOAc fractions lowered the LPS-induced production of proinflammatory molecules and cytokines and inhibited LPS-activated STAT3 and NF-κB, and additionally showed significant free radical scavenging activity and decreased LPS-induced reactive oxygen species and oxidized glutathione. EtOAc fractions of P. nudicaule increased the expression of HO-1, GCLC, NQO-1, and Nrf2 in LPS-stimulated cells and that of P. rhoeas enhanced NQO-1. Furthermore, metabolomic and biochemometric analyses of ethanol extracts and EtOAc fractions indicated that EtOAc fractions of P. nudicaule and P. rhoeas have potent anti-inflammatory and antioxidant activities, further suggesting that alkaloids in EtOAc fractions are potent active molecules of tested plants.

Therapeutic potential of naturally occurring benzofuran derivatives and hybrids of benzofurans with other pharmacophores as antibacterial agents

: Gram-positive and Gram-negative pathogens are able to evade the host immune system, persist within the human host, and lead to severe disease and even death. At present, bacterial infections are one of the leading causes of morbidity and mortality across the world. Development of novel antibacterial agents still represents a challenging endeavor, which is mainly attributed to the continuous emergence of more virulent and drug-resistant pathogens. Benzofuran constitutes the core of diverse pharmacologically active compounds, and there are a variety of approved benzofuran-based drugs in the market or currently going through different clinical phases or registration statuses. Benzofurans could exert antibacterial activity through various mechanisms and possess pronounced activity, so benzofuran is a useful skeleton for the discovery of novel antibacterial agents. This review focuses on the recent advancement of naturally occurring benzofuran derivatives and hybrids of benzofurans with other pharmacophores as antibacterial agents, covering articles published between January 2015 and July 2021. The chemical structures and structure-activity relationships are also discussed.

Pharmacologic rescue of circadian β-cell failure through P2Y1 purinergic receptor identified by small-molecule screen

The mammalian circadian clock drives daily oscillations in physiology and behavior through an autoregulatory transcription feedback loop present in central and peripheral cells. Ablation of the core clock within the endocrine pancreas of adult animals impairs the transcription and splicing of genes involved in hormone exocytosis and causes hypoinsulinemic diabetes. However, identification of druggable proteins and pathways to ameliorate the burden of circadian metabolic disease remains a challenge. Here, we generated beta cells expressing a nano-luciferase reporter within the proinsulin polypeptide to screen 2,640 pharmacologically-active compounds and identify insulinotropic molecules that bypass the secretory defect in clock mutant beta cells. We validated lead compounds in primary mouse islets and identified known modulators of ligand-gated ion channels and G-protein coupled receptors, including the antihelmintic ivermectin. Single-cell electrophysiology in circadian mutant mouse and human cadaveric islets validated ivermectin as a glucose-dependent secretagogue. Genetic, genomic, and pharmacologic analyses established that the molecular clock controls the expression of the purinergic P2Y1 receptor to mediate the insulinotropic activity of ivermectin. These findings identify the P2Y1 purinergic receptor as a target to rescue circadian beta-cell failure and establish a chemical genetic screen for endocrine therapeutics.

Curcumin: A Systematic Review

Many pharmacologically active compounds can be found in medicinal plants. Phytochemicals are currently being studied by scientists to treat a variety of human illnesses. Turmeric (Curcuma longa), a rhizomatous perennial plant in the Zingiberaceae family, is widely used as a food ingredient and in traditional medicine to cure a variety of diseases. Anti-inflammatory, antifungal, anti-angiogenesis, virucidal, anti-mutagenic, and antioxidant activities are all present in it. Angiogenesis, or the formation of new blood vessels, is an important homeostatic mechanism that controls vascular populations in response to physiological and pathological demands, such as chronic inflammation and cancer. Curcumin, a natural polyphenol compound has an activity to inhibit angiogenesis by suppressing tumor neovasculature formation. This study aims to investigate the anti-angiogenesis effect of curcumin.

Anticancer Mechanisms of Bioactive Compounds from Solanaceae: An Update

Plants continue to provide unlimited pharmacologically active compounds that can treat various illnesses, including cancer. The Solanaceae family, besides providing economically important food plants, such as potatoes and tomatoes, has been exploited extensively in folk medicine, as it provides an array of bioactive compounds. Many studies have demonstrated the anticancer potency of some of the compounds, but the corresponding molecular targets are not well defined. However, advances in molecular cell biology and in silico modelling have made it possible to dissect some of the underlying mechanisms. By reviewing the literature over the last five years, we provide an update on anticancer mechanisms associated with phytochemicals isolated from species in the Solanaceae plant family. These mechanisms are conveniently grouped into cell cycle arrest, transcription regulation, modulation of autophagy, inhibition of signalling pathways, suppression of metabolic enzymes, and membrane disruption. The majority of the bioactive compounds exert their antiproliferative effects by inhibiting diverse signalling pathways, as well as arresting the cell cycle. Furthermore, some of the phytochemicals are effective against more than one cancer type. Therefore, understanding these mechanisms provides paths for future formulation of novel anticancer drugs, as well as highlighting potential areas of research.

NEW PHARMACOLOGICALLY ACTIVE COMPOUNDS BASED ON 5-HYDROXY-7-METHOXY-2-PHENYLCHROMAN-4-ONE

The reaction of 5-hydroxy-7-methoxy-2-phenylchroman-4-one with dibromoalkanes in acetone in the presence of potassium carbonate proceeds according to the Michael’s retro-reaction O-alkylation and leads to the formation of the corresponding 2-(bromo-alkoxy) chalcones. The structure of the synthesized compounds was confirmed by IR-, 1H- and 13C-NMR spectroscopy. The cytotoxic, hepatoprotective and anti-inflammatory effects of chalcone derivatives (2-3) were studied for the first time in vitro and in vivo.