Fraxinellone, a naturally occurring degraded limonoid, is mainly isolated from Dictamnus dasycarpus and Melia azedarach. In continuation of our program aimed at the discovery of plant natural products-based insecticid...Fraxinellone, a naturally occurring degraded limonoid, is mainly isolated from Dictamnus dasycarpus and Melia azedarach. In continuation of our program aimed at the discovery of plant natural products-based insecticidal agents, twenty-two new ethers from furyl-ring-based acylation derivatives were prepared by structural modifications of fraxinellone. Their insecticidal activity was evaluated against the pre-thirdinstar larvae of Mythimna separata Walker in vivo. Among them, compounds 5 e and 5 j exhibited more potent insecticidal activity than toosendanin with the final mortality rates greater than 60%. Their structure-activity relationships were also discussed.展开更多
The effect of a-mercapto-β-(2-furyl) acrylic acid (MFA, 200 mg/kg, oral) administered 30 min or 24 h post cadmium (1 mg/kg, i.p.) exposure on cadmium toxicity, was investigated in rats. The Cd induced hepatic metallo...The effect of a-mercapto-β-(2-furyl) acrylic acid (MFA, 200 mg/kg, oral) administered 30 min or 24 h post cadmium (1 mg/kg, i.p.) exposure on cadmium toxicity, was investigated in rats. The Cd induced hepatic metallothionein was reduced by MFA treatment parallel to the depletion of hepatic Cd. However, in renal tissue,MFA caused only redistribution of metal from the paniculate to the soluble fraction. Hepatic and renal Zn and renal Cu were significantly increased on Cd exposure. MFA therapy, however, lowered the hepatic Zn and increased the renal Cu levels. The action of MFA appears to be via metal chelation rather than by MT induction.展开更多
The efficacy of α mercapto β (2_furyl) acrylic acid (MFA), α mercapto β (5_sodiumsulfonate, 2_furyl) acrylic acid (MSFA) and α mercapto β (5_acetoxymethyl, 2_furyl) acrylic acid (MAFA) to mobilize intra...The efficacy of α mercapto β (2_furyl) acrylic acid (MFA), α mercapto β (5_sodiumsulfonate, 2_furyl) acrylic acid (MSFA) and α mercapto β (5_acetoxymethyl, 2_furyl) acrylic acid (MAFA) to mobilize intracellularly bound cadmium in liver and kidney was investigated in rats pre_exposed to cadmium. MFA was effective in reducing cadmium levels of hepatic and renal supernatant cytosolic fraction (SCF) while MSFA and MAFA were effective in lowering cadmium levels of renal SCF and hepatic SCF respectively. All the chelating agents also enhanced the excretion of cadmium more in feces than in urine. However, substitution on the furan ring lowered cadmium mobilizing efficacy of the parent compound, MFA. The treatment with MFA did not affect the status of endogenous zinc and copper while the treatment with MSFA and MAFA enhanced their excretion. MSFA increased hepatic and renal zinc and renal copper while MAFA increased their copper levels.展开更多
Naturally occurring 9-(5-pentyl-2-furyl) nonanoic acid which was synthesized through five steps in about 20% overall yield by using 5-trimethylsilyl-2-furancarboxaldehyde as a starling material.
A facile and efficient one-pot three-component synthesis of bis（5-methyl-2-furyl）methanes has been achieved via the reaction of 2-methylfuran with a series of aliphatic and aromatic aldehydes and aliphatic ketones i...A facile and efficient one-pot three-component synthesis of bis（5-methyl-2-furyl）methanes has been achieved via the reaction of 2-methylfuran with a series of aliphatic and aromatic aldehydes and aliphatic ketones in presence of copper（II） triflate under solvent free conditions. The bis（5-methyl-2-furyl）methanes were obtained in 34%--72% yields and the catalyst was recycled up to four successive cycles without much loss in catalytic activity.展开更多
基金supported by the National Natural Science Foundation of China (No. 31672071)Special Funds of Central Colleges Basic Scientific Research Operating Expenses (No. 2452015096)
文摘Fraxinellone, a naturally occurring degraded limonoid, is mainly isolated from Dictamnus dasycarpus and Melia azedarach. In continuation of our program aimed at the discovery of plant natural products-based insecticidal agents, twenty-two new ethers from furyl-ring-based acylation derivatives were prepared by structural modifications of fraxinellone. Their insecticidal activity was evaluated against the pre-thirdinstar larvae of Mythimna separata Walker in vivo. Among them, compounds 5 e and 5 j exhibited more potent insecticidal activity than toosendanin with the final mortality rates greater than 60%. Their structure-activity relationships were also discussed.
文摘The effect of a-mercapto-β-(2-furyl) acrylic acid (MFA, 200 mg/kg, oral) administered 30 min or 24 h post cadmium (1 mg/kg, i.p.) exposure on cadmium toxicity, was investigated in rats. The Cd induced hepatic metallothionein was reduced by MFA treatment parallel to the depletion of hepatic Cd. However, in renal tissue,MFA caused only redistribution of metal from the paniculate to the soluble fraction. Hepatic and renal Zn and renal Cu were significantly increased on Cd exposure. MFA therapy, however, lowered the hepatic Zn and increased the renal Cu levels. The action of MFA appears to be via metal chelation rather than by MT induction.
文摘The efficacy of α mercapto β (2_furyl) acrylic acid (MFA), α mercapto β (5_sodiumsulfonate, 2_furyl) acrylic acid (MSFA) and α mercapto β (5_acetoxymethyl, 2_furyl) acrylic acid (MAFA) to mobilize intracellularly bound cadmium in liver and kidney was investigated in rats pre_exposed to cadmium. MFA was effective in reducing cadmium levels of hepatic and renal supernatant cytosolic fraction (SCF) while MSFA and MAFA were effective in lowering cadmium levels of renal SCF and hepatic SCF respectively. All the chelating agents also enhanced the excretion of cadmium more in feces than in urine. However, substitution on the furan ring lowered cadmium mobilizing efficacy of the parent compound, MFA. The treatment with MFA did not affect the status of endogenous zinc and copper while the treatment with MSFA and MAFA enhanced their excretion. MSFA increased hepatic and renal zinc and renal copper while MAFA increased their copper levels.
文摘Naturally occurring 9-(5-pentyl-2-furyl) nonanoic acid which was synthesized through five steps in about 20% overall yield by using 5-trimethylsilyl-2-furancarboxaldehyde as a starling material.
文摘A facile and efficient one-pot three-component synthesis of bis（5-methyl-2-furyl）methanes has been achieved via the reaction of 2-methylfuran with a series of aliphatic and aromatic aldehydes and aliphatic ketones in presence of copper（II） triflate under solvent free conditions. The bis（5-methyl-2-furyl）methanes were obtained in 34%--72% yields and the catalyst was recycled up to four successive cycles without much loss in catalytic activity.
