The invention relates to flavanone derivatives, and preparation method and use thereof, particularly relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for preventing or treating a mental disorder or a nervous system disease. The compound of the invention exerts significant activity of inhibiting microglial activation and neuroinflammation, can antagonize dopamine D2 receptor, improve the ethological change in multiple animal models for mental disorders, effectively inhibit neuroinflammation and demyelination, and can be used to prevent or treat a mental disorder and a nervous system disease. ##STR00001##

An embodiment of the invention provides a cannabis-based flavonoid pharmaceutical composition including any one or more selected, from among the group of Apigenin, Cannflavin. A. Cannflavin B, Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside, Kaempferol, Luteolin, Myricetin, Orientin, Isoorientin (Homoorientin), Quercetin (+)-Taxifolin, Vitexin, and Isovitexin, or their synthases, for the prevention and treatment of certain cancers that can be treated by therapeutically targeting oncogenic factors including kinases, sirtuins, bromodomains, matrix metalloproteinases and BCL-2. Some of the cancers that can be treated by use of cannabis flavonoids based on the inhibition of these therapeutic targets include brain, breast, colon, renal, liver, lung, pancreatic, prostate, leukemia, melanoma as well as any other cancers that overexpress the oncogenic factors inhibited by the cannabis flavonoids identified herein.

An embodiment of the invention provides a cannabis-based flavonoid pharmaceutical composition including any one or more selected, from among the group of Apigenin, Cannflavin. A. Cannflavin B, Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside, Kaempferol, Luteolin, Myricetin, Orientin, Isoorientin (Homoorientin), Quercetin (+)-Taxifolin, Vitexin, and Isovitexin, or their synthases, for the prevention and treatment of certain cancers that can be treated by therapeutically targeting oncogenic factors including kinases, sirtuins, bromodomains, matrix metalloproteinases and BCL-2. Some of the cancers that can be treated by use of cannabis flavonoids based on the inhibition of these therapeutic targets include brain, breast, colon, renal, liver, lung, pancreatic, prostate, leukemia, melanoma as well as any other cancers that overexpress the oncogenic factors inhibited by the cannabis flavonoids identified herein.

The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (1) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (1).

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The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (1) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (1).

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A method of increasing the self-renewal and/or expansion of hematopoietic stem and/or progenitor cells (HSPCs) is described. Inhibiting the activity and/or expression of cytochrome P450 1B1 (CYP1B1) and/or increasing the expression or activity of Musashi-2 (MSI2) increases the expansion of HSPCs. The HSPCs may be cultured in the presence of a CYP1B1 inhibitor and/or a MSI2 activator. Optionally, the cells may be expanded ex vivo and transplanted into a subject in need thereof.

A method of increasing the self-renewal and/or expansion of hematopoietic stem and/or progenitor cells (HSPCs) is described. Inhibiting the activity and/or expression of cytochrome P450 1B1 (CYP1B1) and/or increasing the expression or activity of Musashi-2 (MSI2) increases the expansion of HSPCs. The HSPCs may be cultured in the presence of a CYP1B1 inhibitor and/or a MSI2 activator. Optionally, the cells may be expanded ex vivo and transplanted into a subject in need thereof.

Methods to access 2-aryl chromene compounds via an asymmetric catalytic process.

Methods to access 2-aryl chromene compounds via an asymmetric catalytic process.

The composition includes a cyclic, unsaturated compound, preferably a polyphenol derivative. It reduces the synthesis of melanin by inhibiting the activity and expression levels of tyrosinase and related proteins, thereby preventing and limiting the content and distribution of melanin in mammalian skin. It also induces autophagy of melanosome, thereby restricting the synthesis, storage and transfer of melanin from melanocyte to keratinocyte. The dual modes of action allow for the efficacy of the composition at low dosage without causing toxicity to lighten skin and treat disorders associated with hyperpigmentation.