Flavanone 8-dimethylallyltransferase in Sophora flavescens cell suspension cultures
摘要:
Dimethylallyl diphosphate: naringenin 8-dimethylallyltransferase (EC 2.5.1) was characterized. The enzyme was enantiospecific for (-)-(2S)-naringenin and utilized 3,3-dimethylallyl diphosphate as sole prenyl donor. It required Mg2+ (optimum concentration, 10 mM), and has an optimum pH of 9-10. The apparent K-m values for 3,3-dimethylallyl diphosphate and naringenin were 120 and 36 mu M, respectively. The microsomal fraction prenylated several other flavanones at the C-8 position less effectively as compared with naringenin. Interestingly, when 2'-hydroxynaringenin was used as a prenyl acceptor, the 8-lavandulyl (sophoraflavanone G) and the 6-dimethylallyl derivatives were formed, together with the 8-dimethylallyl derivative, leachianone G. These results suggest that the 2'-hydroxy group of naringenin plays an important role for the formation of a lavandulyl group. (C) 2000 Elsevier Science Ltd. All rights reserved.
The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1), a pharmaceutically acceptable salt of this compound or a solvate of this compound. The present invention also provides: this T-type calcium channel inhibitor; a pharmaceutical product containing this T-type calcium channel inhibitor; and a therapeutic agent or prophylactic agent for diseases, the effective action of which is a T-type calcium channel inhibitory action. (In formula (1), each of R
1
and R
2
independently represents H, —OH or —OR
11
, wherein R
11
represents a C
1-3
alkyl group; each of R
3
and R
4
independently represents H, —OH or —OR
12
, wherein R
12
represents a C
1-3
alkyl group; and each of R
5
and R
6
independently represents H, a halogen atom, a C
1-10
alkyl group, a C
2-6
alkenyl group, a C
2-6
alkynyl group, a phenyl group (which may be substituted by a C
1-6
alkoxy group or a halogen atom), a —C
1-3
alkyl-phenyl group (which may be substituted by a C
1-6
alkyloxy group or a halogen atom) or a C
10-50
prenyl group.)
The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1), a pharmaceutically acceptable salt of this compound or a solvate of this compound. The present invention also provides: this T-type calcium channel inhibitor; a pharmaceutical product containing this T-type calcium channel inhibitor; and a therapeutic agent or prophylactic agent for diseases, the effective action of which is a T-type calcium channel inhibitory action. (In formula (1), each of R1 and R2 independently represents H, —OH or —OR11 wherein R11 represents a C1-3 alkyl group; each of R3 and R4 independently represents H, —OH or —OR12, wherein R12 represents a C1-3 alkyl group; and each of R5 and R6 independently represents H, a halogen atom, a C1-10 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a phenyl group (which may be substituted by a C1-6 alkoxy group or a halogen atom), a —C1-3 alkyl-phenyl group (which may be substituted by a C1-6 alkyloxy group or a halogen atom) or a C10-50 prenyl group.)
本发明提供了一种 T 型钙通道抑制剂,它是由式(1)代表的化合物、该化合物的药学上可接受的盐或该化合物的溶液。本发明还提供:这种 T 型钙通道抑制剂;含有这种 T 型钙通道抑制剂的药品;以及一种治疗剂或疾病预防剂,其有效作用为 T 型钙通道抑制作用。式(1)中,R1 和 R2 各自独立地代表 H、-OH 或-OR11,其中 R11 代表 C1-3 烷基;R3 和 R4 各自独立地代表 H、-OH 或-OR12,其中 R12 代表 C1-3 烷基;R5和R6各自独立地代表H、卤素原子、C1-10烷基、C2-6烯基、C2-6炔基、苯基(可被C1-6烷氧基或卤素原子取代)、-C1-3烷基苯基(可被C1-6烷氧基或卤素原子取代)或C10-50链烯基。)
Chemosensory receptor ligand-based therapies
申请人:Anji Pharma (US) LLC
公开号:US10610500B2
公开(公告)日:2020-04-07
Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.