Juniperus sabina L. as a Source of Podophyllotoxins: Extraction Optimization and Anticholinesterase Activities

Juniperus sabina L. (J. sabina) has been an important plant in traditional medicine since ancient times. Its needles are rich in podophyllotoxin, a precursor compound to anti-tumor drugs. However, no systematic research has been done on J. sabina as a source of podophyllotoxins or their biological action. Hence, extracts of podophyllotoxin and deoxypodophyllotoxin were the main optimization targets using the Box–Behnken design (BBD) and response surface methodology (RSM). The total phenol content and antioxidant activity of J. sabina needle extract were also optimized. Under the optimal process conditions (ratio of material to liquid (RLM) 1:40, 90% methanol, and ultrasonic time 7 min), the podophyllotoxin extraction rate was 7.51 mg/g DW, the highest level reported for Juniperus spp. distributed in China. To evaluate its biological potential, the neuroprotective acetyl- and butyrylcholinease (AChE and BChE) inhibitory abilities were tested. The needle extract exhibited significant anti-butyrylcholinesterase activity (520.15 mg GALE/g extract), which correlated well with the high levels of podophyllotoxin and deoxypodophyllotoxin. This study shows the potential medicinal value of J. sabina needles.     

Lingonberry (Vaccinium vitis-idaea L.) Fruit as a Source of Bioactive Compounds with Health-Promoting Effects—A Review

Berries, especially members of the Ericaceae family, are among the best dietary sources of bioactive compounds with beneficial health effects. The most popular berries are in the genus Vaccinium, such as bilberry (Vaccinium myrtillus), cranberry (Vaccinium macrocarpon, V. oxycoccos), and blueberry (Vaccinium corymbosum). Lingonberry (Vaccinium vitis-idaea) is less prevalent in the daily human diet because they are collected from the wild, and plant breeding of lingonberry is still on a small scale. Lingonberries are classed as “superfruits” with the highest content of antioxidants among berries and a broad range of health-promoting effects. Many studies showed various beneficial effects of lingonberries, such as anti-inflammatory, antioxidant, and anticancer activities. Lingonberries have been shown to prevent low-grade inflammation and diet-induced obesity in diabetic animals. Moreover, lingonberry intake has been associated with a beneficial effect on preventing and treating brain aging and neurodegenerative disorders. The consumption of berries and their health-promoting activity is a subject receiving a great deal of attention. Many studies investigated the natural compounds found in berries to combat diseases and promote healthy aging. This article’s scope is to indicate the potential beneficial effect of lingonberry consumption on health, to promote well-being and longevity.     

Functional Studies of Plant Latex as a Rich Source of Bioactive Compounds: Focus on Proteins and Alkaloids

Latex, a sticky emulsion produced by specialized cells called laticifers, is a crucial part of a plant’s defense system against herbivory and pathogens. It consists of a broad spectrum of active compounds, which are beneficial not only for plants, but for human health as well, enough to mention the use of morphine or codeine from poppy latex. Here, we reviewed latex’s general role in plant physiology and the significance of particular compounds (alkaloids and proteins) to its defense system with the example of Chelidonium majus L. from the poppy family. We further attempt to present latex chemicals used so far in medicine and then focus on functional studies of proteins and other compounds with potential pharmacological activities using modern techniques such as CRISPR/Cas9 gene editing. Despite the centuries-old tradition of using latex-bearing plants in therapies, there are still a lot of promising molecules waiting to be explored.     

Annona muricata (Annonaceae): A Review of Its Traditional Uses,Isolated Acetogenins and Biological Activities

Annona muricata is a member of the Annonaceae family and is a fruit tree with a long history of traditional use. A. muricata, also known as soursop, graviola and guanabana, is an evergreen plant that is mostly distributed in tropical and subtropical regions of the world. The fruits of A. muricata are extensively used to prepare syrups, candies, beverages, ice creams and shakes. A wide array of ethnomedicinal activities is contributed to different parts of A. muricata, and indigenous communities in Africa and South America extensively use this plant in their folk medicine. Numerous investigations have substantiated these activities, including anticancer, anticonvulsant, anti-arthritic, antiparasitic, antimalarial, hepatoprotective and antidiabetic activities. Phytochemical studies reveal that annonaceous acetogenins are the major constituents of A. muricata. More than 100 annonaceous acetogenins have been isolated from leaves, barks, seeds, roots and fruits of A. muricata. In view of the immense studies on A. muricata, this review strives to unite available information regarding its phytochemistry, traditional uses and biological activities.     

Chemical,Pharmacological, and in vitro Metabolic Stability Studies on Enantiomerically Pure RC‐33 Compounds: Promising Neuroprotective Agents Acting as σ1 Receptor Agonists

Our recent research efforts identified racemic RC‐33 as a potent and metabolically stable σ₁ receptor agonist. Herein we describe the isolation of pure RC‐33 enantiomers by chiral chromatography, assignment of their absolute configuration, and in vitro biological studies in order to address the role of chirality in the biological activity of these compounds and their metabolic processing. The binding of enantiopure RC‐33 to the σ₁ receptor was also investigated in silico by molecular dynamics simulations. Both RC‐33 enantiomers showed similar affinities for the σ₁ receptor and appeared to be almost equally effective as σ₁ receptor agonists. However, the R‐configured enantiomer showed higher in vitro hepatic metabolic stability in the presence of NADPH than the S enantiomer. Overall, the results presented herein led us to select (R)‐RC‐33 as the optimal candidate for further in vivo studies in an animal model of amyotrophic lateral sclerosis.