Evening primrose oil: a comprehensive review of its bioactives, extraction, analysis, oil quality, therapeutic merits, and safety.

Oil crops have become increasingly farmed worldwide because of their numerous functions in foods and health. In particular, oil derived from the seeds of evening primrose () (EPO) comprises essential fatty acids of the omega-6 (ω-6) series. It is well recognized to promote immune cells with a healthy balance and management of female ailments.

Design, biological evaluation, and molecular modelling insights of cupressic acid derivatives as promising anti-inflammatory agents.

The major labdanes in the oleogum resin of (Salisb.) Franco, 13-epi-cupressic acid () and acetyl-13-epi-cupressic acid () were used to prepare seven new (-), along with one known () derivatives. RAW264.

Development of novel isatin thiazolyl-pyrazoline hybrids as promising antimicrobials in MDR pathogens.

Microbial Multidrug Resistance (MDR) is an emerging global crisis. Derivatization of natural or synthetic scaffolds is among the most reliable strategies to search for and obtain novel antimicrobial agents for the treatment of MDR infections. Here, we successfully manipulated the synthetically flexible isatin moieties to synthesize 22 thiazolyl-pyrazolines hybrids, and assessed their potential antimicrobial activities against various MDR pathogens, using the broth microdilution calorimetric XTT reduction method.

Discovery of 2,4-thiazolidinedione-tethered coumarins as novel selective inhibitors for carbonic anhydrase IX and XII isoforms.

Different 2,4-thiazolidinedione-tethered coumarins , and were synthesised and evaluated for their inhibitory action against the cancer-associated CAs IX and XII, as well as the physiologically dominant CAs I and II to explore their selectivity. Un-substituted phenyl-bearing coumarins , , and 2-thienyl/furyl-bearing coumarins exhibited the best CA IX (Ks between 0.48 and 0.

Natural inspired piperine-based ureas and amides as novel antitumor agents towards breast cancer.

In this work, the natural piperine moiety was utilised to develop two sets of piperine-based amides () and ureas () as potential anticancer agents. The anticancer action was assessed against triple negative breast cancer (TNBC) MDA-MB-231, ovarian A2780CP and hepatocellular HepG2 cancer cell lines. In particular, stood out as the most potent anti-proliferative analogue against TNBC MDA-MB-231 cells with IC equals 18.

Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors.

Ligustrazine is the principle bioactive alkaloid in the widely-used Chinese herb Chuan Xiong rhizome. Herein, a series of novel derivatives has been designed as human carbonic anhydrases inhibitors (hCAIs) starting from the natural product Ligustrazine inserted as a tail instead of the 4-fluorophenyl tail of SLC-0111, a front-runner selective hCA IX inhibitor currently in clinical trials as antitumor/antimetastatic agent. Other derivatives were designed via incorporation of different linkers, of amide and ester type, or incorporation of different zinc anchoring groups such as secondary sulfamoyl and carboxylic acid functionalities.

Natural inspired piperine-based sulfonamides and carboxylic acids as carbonic anhydrase inhibitors: Design, synthesis and biological evaluation.

The natural product piperine, the major bioactive alkaloid present in black pepper fruits, has the ability to modulate the functional activity of several biological targets. In this study, we have utilized the natural piperine as a tail moiety to develop new SLC-0111 analogues (6a-d, 8 and 9) as potential carbonic anhydrase inhibitors. Thereafter, different functionalities, free carboxylic acid (11a-c), acetyl (13a) and ethyl ester (13b-c), were exploited as bioisosteres of the sulfamoyl functionality.

Derivatization, molecular docking and acetylcholinesterase inhibitory activity of glycyrrhizin as a selective anti-Alzheimer agent.

Acetylcholinesterase inhibitors (AChE-Is) increase both level and duration of action of acetylcholine (ACh); thus, alleviate symptoms of Alzheimer's disease (AD). Glycyrrhizin, is the main active compound in liquorice root. Its aglycone, glycyrrhetinic acid, has shown several beneficial pharmacological activities.

Olive and ginkgo extracts as potential cataract therapy with differential inhibitory activity on aldose reductase.

Aldose reductase (AR) has been the leading target in the treatment of diabetic cataract. Although numerous synthetic AR inhibitors (ARI) have been identified, their adverse side effects currently preclude their use. Olive leaf extract (OLE) as well as ginkgo leaf extract (GLE) are natural supplements that have wide therapeutic indices and a plethora of salutary effects during diabetes that so far untested on sugar cataract progression.