Flavonoids are a class of natural substances present in plants, fruits, vegetables, wine, bulbs, bark, stems, roots, and tea. Several attempts are being made to isolate such natural products, which are popular for their health benefits. Flavonoids are now seen as an essential component in a number of cosmetic, pharmaceutical, and medicinal formulations. Quercetin is the major polyphenolic flavonoid found in food products, including berries, apples, cauliflower, tea, cabbage, nuts, and onions that have traditionally been treated as anticancer and antiviral, and used for the treatment of allergic, metabolic, and inflammatory disorders, eye and cardiovascular diseases, and arthritis. Pharmacologically, quercetin has been examined against various microorganisms and parasites, including pathogenic bacteria, viruses, and Plasmodium, Babesia, and Theileria parasites. Additionally, it has shown beneficial effects against Alzheimer's disease (AD), and this activity is due to its inhibitory effect against acetylcholinesterase. It has also been documented to possess antioxidant, antifungal, anti-carcinogenic, hepatoprotective, and cytotoxic activity. Quercetin has been documented to accumulate in the lungs, liver, kidneys, and small intestines, with lower levels seen in the brain, heart, and spleen, and it is extracted through the renal, fecal, and respiratory systems. The current review examines the pharmacokinetics, as well as the toxic and biological activities of quercetin.

The Pharmacological Activity, Biochemical Properties, and Pharmacokinetics of the Major Natural Polyphenolic Flavonoid: Quercetin.

Numerous natural products originated from Chinese herbal medicine exhibit anti-cancer activities, including anti-proliferative, pro-apoptotic, anti-metastatic, anti-angiogenic effects, as well as regulate autophagy, reverse multidrug resistance, balance immunity, and enhance chemotherapy in vitro and in vivo. To provide new insights into the critical path ahead, we systemically reviewed the most recent advances (reported since 2011) on the key compounds with anti-cancer effects derived from Chinese herbal medicine (curcumin, epigallocatechin gallate, berberine, artemisinin, ginsenoside Rg3, ursolic acid, silibinin, emodin, triptolide, cucurbitacin B, tanshinone I, oridonin, shikonin, gambogic acid, artesunate, wogonin, β-elemene, and cepharanthine) in scientific databases (PubMed, Web of Science, Medline, Scopus, and Clinical Trials). With a broader perspective, we focused on their recently discovered and/or investigated pharmacological effects, novel mechanism of action, relevant clinical studies, and their innovative applications in combined therapy and immunomodulation. In addition, the present review has extended to describe other promising compounds including dihydroartemisinin, ginsenoside Rh2, compound K, cucurbitacins D, E, I, tanshinone IIA and cryptotanshinone in view of their potentials in cancer therapy. Up to now, the evidence about the immunomodulatory effects and clinical trials of natural anti-cancer compounds from Chinese herbal medicine is very limited, and further research is needed to monitor their immunoregulatory effects and explore their mechanisms of action as modulators of immune checkpoints.

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Naturally occurring anti-cancer compounds: shining from Chinese herbal medicine.

An insight into anti-inflammatory effects of natural polysaccharides.

Metabolomics highlights pharmacological bioactivity and biochemical mechanism of traditional Chinese medicine.

Nucleophilic Ring Opening of Donor–Acceptor Cyclopropanes Catalyzed by a Brønsted Acid in Hexafluoroisopropanol

Catalyst-free dehydrative SN1-type reaction of indolyl alcohols with diverse nucleophiles “on water”

This paper describes an efficient SN1-type reaction of 3-indolylmethanols with miscellaneous nucleophiles, featuring a catalyst-free procedure, low cost, wide substrate scope and mild reaction conditions. This approach provides green and efficient methods for the synthesis of diverse 3-substituted indolyl derivatives as well as unsymmetrical bisindolylmethanes and triarylmethanes.

Fluorinated Alcohol‐Mediated SN1‐Type Reaction of Indolyl Alcohols with Diverse Nucleophiles

The present study compared the effects of soybean meal fermented by three different probiotics organisms with non-fermented soybean meal on growth performance, serum parameters, immune chemistry and intestinal morphology in weaned piglets. One hundred and forty-four 35-day old crossbred (Duroc × Landrace × Yorkshire) piglets were randomly allocated into four different dietary treatments (n = 36 per group) containing 0, 5, 10 and 15% fermented soybean meal. The piglets fed fermented soybean meal showed an increase (p < 0.05) in average daily weight gain and a reduction in feed consumption (p < 0.05).The piglets fed 10 and 15% fermented soybean meal showed the greatest growth improvement with higher levels of serum alkaline phosphatase and total serum proteins. Serum urea nitrogen in the experimental group was significantly lower than control whereas serum IgG, IgM and IgA levels were all significantly higher. Moreover, villus height in the duodenum, jejunum, and ileum was significantly higher (p < 0.05) and the crypt depth was significantly lower (p < 0.05). The levels of the autophagy factor LC3B in piglets showed a downward trend in the jejunum and ileum compared to control. Fermented soybean meal could significantly improve the growth, immune function and intestinal health in weaned piglets, and the best effective benefits showed in 10% FSBM group.

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Effects of soybean meal fermented by L. plantarum, B. subtilis and S. cerevisieae on growth, immune function and intestinal morphology in weaned piglets.

Treatment of multi-drug resistant (MDR) Escherichia coli intestinal infections are being hampered by the presence of the mcr-1 (colistin) and tet (tetracycline) resistance genes in these strains. We screened seven traditional Chinese medicines for their ability to synergize with tetracycline to provide an effective new drug for the treatment of animal intestinal diseases caused by MDR E. coli. Our primary screen identified quercetin as a compound that reduced the minimum inhibitory concentration (MIC) of tetracycline against the E. coli standard test strain American Type Culture Collection (ATCC) 25922 and clinical isolates fourfold from 4 and 256 μg/mL to 1 and 64 μg/mL, respectively. Low levels of quercetin in combination with tetracycline were bactericidal for clinical E. coli isolates and after 24 h, the differences between this combination and each drug singly were 108 CFU/mL. We used this combination therapy in a mouse infection model and found 100% survival after 48 h compared with <50% for each drug alone. This drug combination also synergized to disrupt the bacterial cell envelope resulting in increased permeability and cell lysis. These data demonstrate that combinatorial screening at low concentrations constitutes an efficient approach to identify clinically relevant quercetin/tetracycline combinations and is a valuable prototypical combination that has a high clinical potential against E. coli infections.

Mechanism of Synergy Between Tetracycline and Quercetin Against Antibiotic Resistant Escherichia coli.

Atherosclerosis, a chronic inflammatory disease, is a major contributor to cardiovascular diseases. Ursolic acid (UA) is a phytonutrient with widely biological effects including anti-oxidative, anti-inflammatory, and so on. At present, the effect of UA on atherosclerosis and the mechanism of action are still obscure. This study focused on investigating the effects of UA on atherosclerosis both in vivo and in vitro. We first selected LOX-1 as our target, which was reckoned as a new promising receptor for treating atherosclerosis. The evaluation in vitro suggested that UA significantly decreased endothelial LOX-1 expression induced by LPS both in mRNA and protein levels. Pre-treatment of UA also inhibited TLR4/MyD88 signaling activated by LPS. Moreover, UA reduced ROS production and suppressed the activation of NF-κB stimulated by LPS. Particularly, the evaluation in vivo further verified the conclusion obtained in vitro. In ApoE−/− mice fed with an atherogenic diet, both UA (100 mg/kg/day) and simvastatin significantly attenuated atherosclerotic plaque formation and shrunk necrotic core areas. The enhanced expression of LOX-1 in atherosclerotic aorta was also dramatically decreased by administration of UA. Taken together, these results suggested that UA, with anti-atherosclerotic activity through inhibition of LOX-1 mediated by ROS/NF-κB signaling pathways, may become a valuable vascular protective candidate for the treatment of atherosclerosis.

https://www.mdpi.com/1420-3049/23/5/1101/pdf

Zhihui Hao

Papers

Catalyst-free dehydrative SN1-type reaction of indolyl alcohols with diverse nucleophiles “on water”

Fluorinated Alcohol‐Mediated SN1‐Type Reaction of Indolyl Alcohols with Diverse Nucleophiles

Effects of soybean meal fermented by L. plantarum, B. subtilis and S. cerevisieae on growth, immune function and intestinal morphology in weaned piglets.

Mechanism of Synergy Between Tetracycline and Quercetin Against Antibiotic Resistant Escherichia coli.

Ursolic Acid Attenuates Atherosclerosis in ApoE-/- Mice: Role of LOX-1 Mediated by ROS/NF-κB Pathway.