Euodia Fruit is a crude drug used to treat migraine and headaches and is well-known to contain indole alkaloids, which may contribute to the observed pharmacological activities. A methanolic extract of Euodia Fruit exhibited pancreatic lipase inhibitory activity (IC₅₀ 13.9 mg/mL). Bioassay-guided fractionation of the extract led to the isolation of 14 quinolone alkaloids (1-14), three indole alkaloids: rutaecarpine (15), evodiamine (16), and dehydroevodiamine (17), and a limonoid: rutaevine acetate (18), among which three quinolone alkaloids (12-14) have been previously undescribed. The structures of 12-14 were determined by extensive spectroscopic analyses, including two-dimensional (2D) NMR. Compounds 2, 3, 6-9, 13, and 14 exhibited pancreatic lipase inhibitory activity, with IC₅₀ values ranging from 1.40 to 7.37 mM. The results revealed that the length of the aliphatic side chain and the presence of an olefinic bond at the C-2 side chain of the quinolone alkaloids could impact lipase inhibitory activity. In soybean oil-loaded mice, orally administered evocarpine (8) reduced serum triglyceride levels in a dose-dependent manner. Furthermore, 8-14 at 5.0 and 50 μM exhibited peroxisome proliferator-activated receptor (PPAR)-γ ligand-binding activity.

01 Jan 2025·Hormones and Behavior

Oral administration of ethinyl estradiol and the brain-selective estrogen prodrug DHED in a female common marmoset model of menopause: Effects on cognition, thermoregulation, and sleep

Article

Author: Prokai, Laszlo ; Mong, Jessica A ; Rothwell, Emily S ; Lacreuse, Agnès ; Viechweg, Shaun S

Menopausal symptoms of sleep disturbances, cognitive deficits, and hot flashes are understudied, in part due to the lack of animal models in which they co-occur. Common marmosets (Callithrix jacchus) are valuable nonhuman primates for studying these symptoms, and we examined changes in cognition (reversal learning), sleep (48 h/wk of sleep recorded by telemetry), and thermoregulation (nose temperature in response to mild external warming) in middle-aged, surgically-induced menopausal marmosets studied at baseline, during 3-week phases of ethinyl estradiol (EE₂, 4 μg/kg/day, p.o.) treatment and after EE₂ withdrawal. We also assessed a brain-selective hormonal therapy devoid of estrogenic effects in peripheral tissues on the same measures (cognition, sleep, thermoregulation) after treatment with the estrogen prodrug 10β,17β-dihydroxyestra-1,4-dien-3-one (DHED, 100 μg/kg/day, p.o) and DHED withdrawal. Reversal learning performance was improved with EE₂ or DHED treatment relative to phases without hormone administration, as indicated by a faster reversal of the stimulus/reward contingencies. Both EE₂ and DHED increased non-REM sleep and reduced nighttime awakenings relative to baseline, but to the detriment of REM sleep which was highest at baseline. Nasal temperature in response to mild external warming was highest, and overnight core body temperature lowest, in the DHED treatment phase compared to both the EE₂ and baseline phases. These results suggest that low dose estradiol, delivered either peripherally or centrally via DHED, benefits selective aspects of cognition and sleep in a marmoset menopause model. DHED appears a promising therapeutic candidate for alleviating the cognitive and sleep disruptions associated with estrogen deficiency in primates.

31 Dec 2024·Bioengineered

Statement of Retraction: Dehydroevodiamine suppresses inflammatory responses in adjuvant-induced arthritis rats and human fibroblast-like synoviocytes

100 Deals associated with Dehydroevodiamine hydrochloride

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 1	-	The University of Seoul	-
Alzheimer Disease	Phase 1	-	Jeil Pharmaceutical Co., Ltd.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

Dehydroevodiamine hydrochloride

Overview

Basic Info

Structure/Sequence

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation