Garlic polysaccharide-Cr (III) complexes with enhanced in vitro and in vivo hypoglycemic activities.

This study aimed to prepare a complex of Cr (III) and garlic polysaccharides (GPs) and evaluate the in vitro and in vivo hypoglycemic activities of GPs and GP-Cr (III) complexes. The chelation of GPs with Cr (III) increased molecular weight, modified crystallinity, and altered morphological characteristics, through targeting the OH of hydroxyl groups and involving the C-O/O-C-O structure. The GP-Cr (III) complex had a higher thermal stability over 170-260 °C and higher stability throughout the gastrointestinal digestion. In vitro, the GP-Cr (III) complex exhibited a significantly stronger inhibitory effect against α-glucosidase compared with the GP. In vivo, the GP-Cr (III) complex at a high dose (4.0 mg Cr/kg body weight) generally had a higher hypoglycemic activity than the GP in (pre)-diabetic mice induced by a high-fat and high-fructose diet, based on indices like body weight, blood glucose levels, glucose tolerance, insulin resistance, insulin sensitivity, blood lipid levels, and hepatic morphology and function. Therefore, GP-Cr (III) complexes could be a potential Cr (III) supplement with an enhanced hypoglycemic activity.

Exploration of Fungicidal Activity and Mode of Action of Ferimzone Analogs.

Lead discovery and molecular target identification are important for developing novel pesticides. Scaffold hopping, an effective approach of modern medicinal and agrochemical chemistry for a rational design of target molecules, is aiming to design novel molecules with similar structures and similar/better biological performance. Herein, 24 new ferimzone derivatives were designed and synthesized by a scaffold-hopping strategy. In vitro bioassays indicated that compound 5o showed similar potency to ferimzone against Cercospora arachidicola and 2-fold higher potency than ferimzone against Alternaria solani. Compounds 5q, 6a, and 6d displayed fungicidal activity with EC50 values ranging from 1.17 to 3.84 µg/mL against Rhizoctonia solani, and compounds 5q and 6a displayed 1.6-1.8-fold higher activity than ferimzone against Fusarium graminearum. The in vivo bioassays at 200 µg/mL indicated that compound 5q was more potent than ferimzone against Pyricularia oryzae (90% vs 70% efficacy, respectively). Density functional theory (DFT) calculations elucidated the structure-energy relationship. Although the mode of action of ferimzone is still unclear, studies suggested that compound 5q significantly inhibited the growth and reproduction of R. solani, and its energy metabolism pathways (e.g., starch, sucrose, lipids, and glutathione) were seriously downregulated after a 5q treatment.

Preparation and characterization of garlic polysaccharide-Zn (II) complexes and their bioactivities as a zinc supplement in Zn-deficient mice.

This study explored the potential of garlic polysaccharides (GPs) as a carrier for synthesizing GP-Zn (II) complexes to supplement Zn. According to the response surface analysis, the optimal preparation conditions were: mass ratio of GPs to Zn2+ 1:0.21, temperature 53 °C, pH 5.9 and time 148.75 min, with the maximum chelation rate of 90.11%. The chelation of GPs and Zn2+ involved O-H/C-O/O-C-O groups, increased crystallinity and altered absorption peaks of circular dichroism spectra, with a higher thermal stability, particle size and negative zeta potential. Compared with inorganic zinc salts, supplementation of GP-Zn (II) complexes showed enhance zinc supplementation effects in Zn-deficient mice model: increased body weight, organ index and Zn (II) levels in serum and liver, enhanced Superoxidedismutase (SOD) activity and alkaline phosphatase activity, decreased NO content and Malondialdehyde (MDA) content and improved colon and testicular morphology. Therefore, GP-Zn (II) complex can be used as a potential zinc supplement for Zn-deficient individuals.