[Translation] A randomized, double-blind, single-dummy, multicenter clinical trial of limonin capsules versus placebo in the treatment of hemorrhoids (damp-heat syndrome)

以安慰剂对照，初步评价柠檬苦素胶囊治疗痔疮(湿热下注证)的安全性、有效性

[Translation]

A placebo-controlled trial to evaluate the safety and efficacy of limonin capsules in the treatment of hemorrhoids (damp-heat syndrome)

Start Date-

Sponsor / Collaborator

China Pharmaceutical University

[+1]

100 Clinical Results associated with Limonin

100 Translational Medicine associated with Limonin

100 Patents (Medical) associated with Limonin

328

Literatures (Medical) associated with Limonin

01 Dec 2024·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Effect of the presence of berberine/curcumin on the binding of limonin to human serum albumin and antitumor activity in vitro

Article

Author: Wang, Xin ; Ge, Ying-Di ; Xing, Mei-Yi ; Xu, Liang ; Ju, Wan-Ting ; Zhou, Xin-Yi

The competition among drugs for binding to plasma proteins is regarded as a pharmacokinetic drug interaction. Competition between antitumor agents and other drugs for plasma protein binding can alter the free concentration of the drug, potentially impacting its efficacy and increasing the risk of toxic side effects. Through a range of spectroscopic techniques, this study examined the interaction between limonin and human serum albumin (HSA) in the context of berberine (Ber) and curcumin (Cur) under physiological conditions to clarify the binding mechanisms of binary and ternary systems at the molecular level. As demonstrated by fluorescence quenching experiments, Static quenching was identified as the mechanism of interaction between HSA and limonin. The results of site competition experiments indicated that the binding site between limonin and HSA was site I, a result further supported by molecular docking simulations. Through the use of thermodynamic data calculations, it was determined that limonin forms a stable complex with HSA by establishing hydrogen bonds and van der Waals forces. Circular dichroism (CD) spectroscopy, three-dimensional (3D) fluorescence spectroscopy, and synchronous fluorescence spectroscopy (SFS) employed to validate the notion that limonin perturbed the microenvironment of amino acids and induced conformational changes in HSA. What's more, the presence of Ber or Cur was found to have further modified the alterations observed in the interaction between the original HSA-limonin binary system. In vitro cellular experiments showed that interaction with HSA reduced the antitumor activity of limonin. In contrast, adding Ber or Cur increased the inhibition rate of tumor cells. The coexistence of both Ber and Cur significantly diminished limonin's binding affinity to HSA. The current investigation enhances comprehension regarding the binding characteristics and interaction mechanisms involving limonin, Ber, Cur, and HSA. It explores the potential of HSA as a versatile drug carrier and furnishes theoretical underpinnings for co-administrative strategies.

01 Oct 2024·Fitoterapia

Limonin (LM) and its derivatives: Unveiling the neuroprotective and anti-inflammatory potential of LM and V-A-4 in the management of Alzheimer's disease and Parkinson's disease

Review

Author: Mayank ; Kesharwani, Adarsh ; Mallick, Sarada Prasanna ; Guru, Ajay ; Panda, Siva Prasad ; Singh, Mansi ; Kumar, Sanjesh

Neuroinflammation and neuronal apoptosis are central pathogenic consequences associated with Alzheimer's Disease (AD) and Parkinson's Disease (PD). Limonin (LM), a tetracyclic triterpenoid available in citrus fruits, has anti-tumor, antioxidant, anti-inflammatory, hepatoprotective, and neuroprotective actions. LM derivative, V-A-4 emerged as a potential neuroprotective drug due to their ability to target multiple molecular pathways intertwined with neuroinflammation and neuronal apoptosis. To date, the treatment of AD and PD is not successful even though the understanding of the mechanism of neuroinflammation and neuronal apoptosis is vast in the literature. Thus, there is an urgent need to identify novel neuroprotective drugs that could target the multiple molecular pathways associated with neuroinflammation and neuronal apoptosis. The various online databases (Google scholar, Pubmed, Scopus) were searched via keywords: limonin, limonin derivatives and neuroprotection. This review highlights the multifunctional nature of LM and derivatives in combating neuroinflammation and neuronal apoptosis by stimulating PI3K/AKT and downregulating TLR4/NF-κB critical pathways. By intervening in the secretion of NO and TNF-α from glial cells, V-A-4 attenuates the damaging cascade of neuroinflammation by suppressing IKK-α and IKK-β. Furthermore, V-A-4 demonstrates its versatility by suppressing the manifestation of miR-146a and miR-155, both intimately linked to neuroinflammation, this review summarized the activities of LM and its derivatives against AD and PD, with a special focus on V-A-4 as an effective neuroprotective drug. V-A-4's ability to stimulate PI3K/AKT signaling further underscores its neuroprotective effect in combating AD and PD. More in-vitro cell line studies are needed to develop V-A-4 as an upcoming neuroprotective compound.

01 Sep 2024·Naunyn-Schmiedeberg's Archives of Pharmacology

Retraction Note: Hepatoprotective effect of limonin, a natural limonoid from the seed of Citrus aurantium var. bigaradia, on D-galactosamine-induced liver injury in rats

Author: El-Shazly, Assem M ; Hamdan, Dalia I ; Mahmoud, Mona F ; Wink, Michael

100 Deals associated with Limonin

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Hemorrhoids	Phase 2	CN	China Pharmaceutical University	-
Hemorrhoids	Phase 2	-	Taizhou Bomeile Technology Co., Ltd.	-
Acute Kidney Injury	Preclinical	CN	Southern Medical University	29 May 2023

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