Delving into the Latest Updates on Kakonein with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Puerarin

Target

BK channel x L-type calcium channel

Action

agonists, blockers

Mechanism

BK channel agonists(Calcium-activated potassium channel alpha/beta 1 agonists), L-type calcium channel blockers(Voltage-gated L-type calcium channel blockers)

Therapeutic Areas

Cardiovascular DiseasesOther Diseases

Active Indication

Cardiovascular DiseasesAlcoholism

Inactive Indication-

Originator Organization

Natural Pharmacia International

Active Organization

Natural Pharmacia International

Yantai Luyin Pharmaceutical Co. Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

China (01 Jan 1993),

Cardiovascular Diseases

Regulation-

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Structure/Sequence

Molecular FormulaC21H20O9

InChIKeyHKEAFJYKMMKDOR-VPRICQMDSA-N

CAS Registry3681-99-0

Flavonoid glycosides are formed by dehydration condensation of aglycones and sugar molecules. Therefore, discrimination of flavonoid glycosides from their corresponding aglycones is a challenging task because they contain the same aglycone part in their molecular structures. Herein, boric acid-functional Eu(III)-organic framework (BA-Eu-MOF) was applied to discriminate flavonoid glycosides including baicalin (Bai), wogonoside (Wog), rutin (Rut), puerarin (Pue), quercitrin (Que) and astragalin (Ast) from their corresponding aglycones for the first time. Besides as organic ligand to sensitize the luminescence of Eu³⁺ through "antenna" effect, 5-boronobenzene-1,3 dicarboxylic acid provided recognition site for flavonoid glycosides. Infrared, fluorescence, UV-vis, and mass spectra were used to investigate the recognition reaction between BA-Eu-MOF and flavonoid glycosides. The data indicated that the cis-diols of flavonoid glycosides from sugars covalently bonded to boric acid group to form cyclic boronic esters, which quenched the fluorescence of BA-Eu-MOF at 620 nm through decreasing the intersystem efficiency, inner filter effect and photoelectron transfer. In contrast, aglycones could not alter the fluorescence of BA-Eu-MOF because of no covalent bond between them. This probe exhibited high sensitivity towards flavonoid glycosides with the low detection limits of 3.3 nM, 3.5 nM, 33 nM, 56 nM, 5.1 nM and 5.5 nM for Bai, Que, Wog, Ast, Pue and Rut, respectively. The unique recognition ability of boric acid group enables selective and sensitive detection of flavonoid glycosides without the interference of their corresponding aglycones.

01 May 2025·European Journal of Pharmacology

Treatment of glaucoma with drug-loaded contact lenses: A systematic review and meta-analysis

Review

Author: Xu, Zihang ; Yu, Mingkun ; Wang, Xuan ; Ren, Cong ; Cao, Wenbo ; Zhang, Diya ; Guo, Bin ; Li, Jia ; Bi, Hongsheng

OBJECTIVEThis study is a systematical review regarding the glaucoma treatment with drug-loaded contact lenses. The effectiveness and safety about that were summarized, which providing effective suggestions and guidance for clinical research.METHODSThe studies published up to May 1, 2024 on the treatment of glaucoma with sustained-release contact lenses were searched from CNKI, Wanfang Data, VIP, PubMed, Embase, Cochrane Library, and Medline. CAMARADES was used to evaluate literature quality. The safety, endpoints of intraocular pressure reduction (IOPR) and duration of intraocular pressure (IOP) decline during glaucoma treatment were analyzed by means of qualitative and quantitative methods. The protocol registration number is CRD42024487157.RESULTS47 studies were included. In clinical trials, glaucoma patients showed a 50% reduction in IOP and no corneal tissue destruction after wearing contact lenses. In animal experiments, the endpoint IOPR [MD = 0.58, 95%CI (0.37, 0.80), P < 0.00001] of the medicated contact lenses group was significantly better than that of the eye drops group. Subgroup analysis showed that contact lenses loaded with timolol (TML), with TML + dorzolamide, and with TML + latanoprost, which compared to eye drops, had a better effect on reducing IOP, while contact lenses loaded with puerarin, latanoprost, and TML + bimatoprost showed no statistical difference. Most studies demonstrated the duration of IOP reduction and drugs release in vitro for ≥3 days during contact lenses treatment.CONCLUSIONMost drug-loaded contact lenses exhibit excellent effectiveness and safety. The nanoparticle-loaded contact lenses containing TML for glaucoma treatment is recommended in future clinical research.

01 Apr 2025·Talanta

Integration of feature-based molecular networking and high-definition data-dependent acquisition for the comprehensive multicomponent characterization of Honghua Xiaoyao Tablet

Article

Author: Ma, Siyi ; Zeng, Huawu ; Ye, Ji ; Zhang, Weidong ; Wu, Shiyu ; Zhang, Shiyu ; Zhu, Renwen ; Zhang, Yuhao

Systematically identifying the chemical constituents in complex matrices is a challenge due to the inherent characteristics of compounds. The combination of liquid chromatography-tandem mass spectrometry (LC-MS) and classical molecular networking (CLMN) is a powerful technology for annotating small molecules. However, the low coverage from inappropriate acquisition modes and the inseparability of isomeric compound nodes still hinders the comprehensive metabolite characterization. A novel strategy that integrated high-definition data-dependent acquisition (HDDDA) from traveling-wave ion mobility mass spectrometry (TWIMS) and feature-based molecular networking (FBMN) was developed to improve chemical component characterization and enhance isomeric component discernment. The data-dependent acquisition (DDA) and HDDDA, were effectively and visually evaluated by CLMN and FBMN via the number of nodes, clustered nodes and clusters. Moreover, the efficiency of the three strategies was validated. The results strongly demonstrated that the HDDDA-FBMN strategy improves MS coverage and offers significant advantages for isomer identification. With the assistance of the UNIFI platform, the developed strategy was successfully applied to systematically investigate the chemical profile of Honghua Xiaoyao Tablet (HHXYT), a traditional folk empirical prescription for treating various gynecological diseases. 184 compounds were unambiguously identified or tentatively characterized, including 12 pairs of isomers, and two unreported compounds. In conclusion, this hybrid approach achieves dimensionally enhanced MS data acquisition and visual recognition of isomeric compounds, accelerating the structural characterization in complex systems. We anticipate that HDDDA-FBMN strategies will be a flexible and versatile tool for the chemical components in a complex system of TCMs.

100 Deals associated with Kakonein

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12290

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Cardiovascular Diseases	China	Yantai Luyin Pharmaceutical Co. Ltd.	01 Jan 1993

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Alcoholism	Phase 2	-	Natural Pharmacia International	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00854724 (PAD, CTgov)	Phase 2	Alcoholism	16	Placebo+Puerarin (Placebo, Then Puerarin)	rkuoxubycx(ijnickrzyc) = dytqimsmln qbefcwakcd (dsaamndlkv, vntwosjneb - hcgenfappp) View more	-	12 Aug 2011
				Placebo+Puerarin (Puerarin, Then Placebo)	rkuoxubycx(ijnickrzyc) = emktvxewvn qbefcwakcd (dsaamndlkv, sxobmeqeea - nyaslgrdyn) View more
ARVO2009	Not Applicable	-	-	Microemulsion with ion-triggered in situ gelling system for puerarin (ME-G-PU)	(yqmgopksme) = gxbvpzpnep wtumksoack (kwacfdtcvj ) View more	-	01 Apr 2009
				Microemulsion containing 1% PU (ME-PU)	(yqmgopksme) = hnogsutnvv wtumksoack (kwacfdtcvj ) View more