Delving into the Latest Updates on Silibinin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Silibinin (INN), Silibinin A, Silybin A

+ [12]

Target

HSP90

Mechanism

HSP90 inhibitors(Heat shock 90kDa proteins inhibitors)

Therapeutic Areas

Digestive System DisordersCardiovascular DiseasesEndocrinology and Metabolic Disease+ [2]

Active Indication

Liver DiseasesDiabetic RetinopathyCushing Syndrome

Inactive Indication

Beta-ThalassemiaIron Overloadliver function failure+ [1]

Originator Organization-

Active Organization

Augusta UniversityMax-Planck Institute of Psychiatry

Inactive Organization

Nhat Nhat Pharmaceutical Co.，LtdMadaus SA

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC25H22O10

InChIKeySEBFKMXJBCUCAI-HKTJVKLFSA-N

CAS Registry22888-70-6

Background:The reproductive organ, housing spermatogonial stem cells (SSCs), undergoes ongoing division impacted by the irradiation dosage and exposure duration. Within the male reproductive organ, germ stem cells (spermatogonia) and somatic cells (Sertoli and Leydig cells) are present. Lower doses of ionizing (>4-6 Gy) and non-ionizing radiation (radiofrequency and microwave range 900 MHz - 2.45 GHz) may cause sperm-related issues, while higher doses (15 Gy) may affect Leydig cells and testosterone production. Response to radiation varies with age and pubescence. Spermatogonial stem cells, crucial for regenerating the spermatogenic lineage, express molecular markers like Estrogen receptor, FSH (Follicular Stimulating Hormone) receptor, TLR-4 (Toll-like Receptor-4), TLR-5 (Toll-like Receptor-5), FGF2 (Fibroblast Growth Factor-2), KIT (Receptor Tyrosine Kinase), AT-1 (Angiotensin II Type-1 Receptor), LXRs-γ (Liver X Receptor-γ), TNF-β (Tumor Necrosis Factor-β), and PCNA (Proliferating Cell Nuclear Antigen), influencing stem cell activity in testes.Objective:This study aimed to review the various available radioprotective agents and their efficacy in targeting the male reproductive system from the available literature.Result:Various radioprotective herbal/synthetic/microbial/metallic extracts/formulations/ drugs [Septilin, Silymarin, Organic Turmeric, Oestrogen, Melatonin, Febuxostat, SQGD (Semiquinone glucoside derivative), Rapamycin, Entolimod, Zinc, Selenium, etc.] have been investigated up to exposure, but owing to effectiveness issues, they are unable to fulfil the aim to the fullest of restoring male fertility and normal testosterone levels during such eventuality.Conclusion:Further study is needed to optimize these tactics and fill knowledge gaps. Also, the effective components of herbal, synthetic drugs, etc., should be isolated and tested up to clinical levels, paving the way for successful radioprotection and radiomitigation strategies in the male reproductive system.

01 Feb 2025·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Comparison of biochemical changes induced in radioresistant prostate cancer cells by X-rays, radiosensitizing drugs, and a combined therapy using Raman microspectroscopy

Article

Author: Kwiatek, Wojciech M ; Wrobel, Tomasz P. ; Kwiatek, Wojciech M. ; Wrobel, Tomasz P ; Roman, Maciej ; Panek, Agnieszka

Cancer radioresistance is a major problem in radiotherapy. Many strategies have been proposed to overcome this process including the use of radiosensitizing drugs such as C75 or silibinin. The overall result of all treatments (radiotherapy, chemotherapy, and combined treatment) is cancer cell death. On the other hand, each treatment affects cancer cells differently at the molecular level. However, little is known about biochemical changes induced in cancer cells by these treatments (especially in combined therapy) at the submicroscale. In this study, Raman microspectroscopy was applied to follow such changes induced in radioresistant prostate cancer cells by X-rays, radiosensitizing drugs (C75, silibinin), and a combined treatment. The analysis was supported by the Partial Least Squares Regression method to reveal spectral changes induced by an increasing dose of X-rays and concentrations of the drugs. The obtained regression coefficient (β) plots were compared to each other using a correlation coefficient (R). Our results show that PC-3 cells exhibit dose- and concentration-dependent responses to the treatment with different biochemical changes induced by X-rays in the presence of C75 and silibinin. Moreover, both drugs affect the cells differently at the submicroscale and independently from the X-ray's presence. Finally, C75 shows significant efficiency in the reduction of cell radioresistance.

01 Jan 2025·Combinatorial Chemistry & High Throughput Screening

Resveratrol Enhances Anticancer Effects of Silybin on HepG2 Cells and H22 Tumor-bearing Mice via Inducing G2/M Phase Arrest and Increasing Bax/Bcl-2 Ratio

Article

Author: Xing, Yingru ; Lin, Junjie ; Wu, Zhihuan ; Chang, Yuexing ; Jin, Feng ; Wang, Ce ; Guo, Jia ; Deng, Yun ; He, Yu ; Guo, Ailing

Background:Silybin, a major flavonoid extracted from the seeds of milk thistle, has a strong hepatoprotective but weak anti-hepatoma activity. Screening another natural ingredient and combining it with silybin is expected to improve the anti-hepatoma efficacy of silybin.Objective:The objective of this study was to investigate the synergistic anti-hepatoma effect of resveratrol and silybin on HepG2 cells and H22 tumor-bearing mice in hepatocellular carcinoma (HCC) in vitro and in vivo, respectively.Methods:Cell viability, scratch wound, clone formation, cell apoptosis, cell cycle, and western blot analysis of HepG2 cells were used to investigate the synergistic effects in vitro of the combination resveratrol with silybin. Growth rates, tumor weights, organ indexes, and histological pathological examination in H22 tumor-bearing mice were used to investigate the synergistic effects in vivo.Results:The combination of resveratrol (50 μg/mL) and silybin (100 μg/mL) significantly suppressed cell viability, whose combination index (CI) was 1.63 (>1.15), indicating the best synergism. The combination exhibited the synergistic effect in blocking the migration and proliferative capacity of HepG2 cells in the measurement in vitro. In particular, resveratrol enhanced the upregulation of Bcl-2 expression and the downregulation of Bax expression with a concurrent increase in the Bax/Bcl-2 ratio. The combination of resveratrol (50 mg/kg) and silybin (100 mg/kg) reduced the tumor weight, inhibited the growth rate, increased the organ indexes, and destroyed the tumor tissue morphology in H22 tumor-bearing mice.Conclusion:Resveratrol was found to exhibit synergistic anti-cancer effects with silybin on HepG2 cells and H22 tumor-bearing mice.

1

News (Medical) associated with Silibinin

16 Feb 2024

·www.prnewswire.com

Capsulyte Unveils PREGAME: The Ultimate Solution for Party Recovery, Marking Its Debut at DC Fashion Week

Capsulyte PREGAME, a doctor formulated supplement to aid alcohol recovery, launches at DC Fashion Week as the hangover recovery market is set to grow over the next decade. CRANBURY, N.J., Feb. 16, 2024 /PRNewswire/ -- Capitalizing on cutting-edge ingredients, Capsulyte's PREGAME has emerged as the most advanced product to aid in party recovery and address symptoms often associated with hangovers. As a significant milestone for the brand, Capsulyte has been invited to participate in the prestigious DC Fashion Week, a testament to the company's alignment with premium lifestyles and the fashion industry's elite. This invitation further underscores Capsulyte's commitment to excellence and positions PREGAME as the preferred choice for discerning individuals seeking to enjoy social occasions to the fullest, without the next-day regrets. Many individuals face the unpleasant reality of hangover symptoms such as headaches, fatigue, and nausea, resulting from alcohol consumption. These effects can be primarily attributed to acetaldehyde, a toxic compound that is created when the liver metabolizes alcohol. According to Persistence Market Research, the global hangover recovery market is estimated to reach $4.2 billion by the year 2030. PREGAME is uniquely situated to help solve the issue of acetaldehyde accumulation among individuals who want to live healthy, balanced lives while also maintaining their productivity. PREGAME addresses the challenge of party recovery head-on with a formulation enriched with the scientifically backed ingredients Siliphos® and Clovinol® to support liver detoxification, overall liver health, and acetaldehyde metabolism. Siliphos®, a patented botanical derivative from milk thistle, has been clinically shown to improve liver function, inhibit fibrotic cells, and shield against oxidative stress. Its unique Phytosome technology enhances the bioavailability of silybin, a key component for liver health that is otherwise poorly absorbed by the body. This innovative approach ensures marked improvement over standard milk thistle extracts, offering comprehensive liver protection and recovery. Clovinol®, sourced from the potent spice clove, is distinguished by its capacity to increase the potent antioxidant, glutathione. It's also a robust liver protector that accelerates the elimination of acetaldehyde from the body up to 2.5 times faster than usual, thereby reducing alcohol's negative effects and the severity of symptoms associated with hangovers. With the synergy of Siliphos® and Clovinol®, combined with Dihydromyricetin (DHM) and N-Acetyl Cysteine (NAC), PREGAME represents the pinnacle of a doctor-formulated, research-backed solution for those seeking to mitigate the aftereffects of alcohol consumption. As the brand marks its presence at DC Fashion Week, Capsulyte is set to redefine the standards of social indulgence and wellness. Its participation not only highlights the efficacy and luxury associated with PREGAME but also solidifies Capsulyte's stance as a trailblazer in the dietary supplement industry. Unlock the ability to embrace a healthier, more vibrant lifestyle with Capsulyte's PREGAME, where premium care meets unparalleled social experiences. Capsulyte's PREGAME and HYDRATION are available on the store site and Amazon. FDA Disclaimer: The statements made regarding this product have not been evaluated by the Food and Drug Administration. These products are not intended to diagnose, treat, cure or prevent any disease. All information presented here is not meant as a substitute for or alternative to information from healthcare practitioners. Please consult your doctor. The news site hosting this press release is not associated with Capsulyte. It is merely publishing a press release announcement submitted by a company, without any stated or implied endorsement of the product or service. About Capsulyte Capsulyte is a doctor-founded dietary supplement company dedicated to enhancing the health and wellbeing of individuals through scientifically backed, innovative products. Specializing in alcohol and party recovery solutions, Capsulyte is committed to delivering superior quality, efficacy, and safety in every product, supporting people in living their best lives. For more information, visit Press Contact Dan Nguyen 908-292-3110 SOURCE Capsulyte

100 Deals associated with Silibinin

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External Link

KEGG	Wiki	ATC	Drug Bank
D08515	Silibinin	A05BA03	DB09298

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Liver Diseases	-	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
liver function failure	Phase 2	VN	Nhat Nhat Pharmaceutical Co.，Ltd	15 Jun 2017
Beta-Thalassemia	Phase 2	IR	Madaus SA	01 Mar 2009
Iron Overload	Phase 2	IR	Madaus SA	01 Mar 2009
Nonalcoholic Steatohepatitis	Phase 2	US	Madaus SA	01 Apr 2008
Diabetic Retinopathy	Preclinical	US	Augusta University	01 May 2022
Cushing Syndrome	Preclinical	DE	Max-Planck Institute of Psychiatry	09 Feb 2015

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SUSTAIN (ASCO2023) Manual	Phase 2	Brain metastases	30	silibinin	(htsmxxayfw) = Two pts discontinued silibinin-based nutraceutical assumption due to G1 nausea. No other adverse events were reported. gwswfzeaam (ydtwxsxzpk )	Positive	31 May 2023
NCT00915681 (CTgov)	Phase 2	Poisoning \| liver function failure \| Mushroom Poisoning	148	Silibinin	bwvxhdwzdp(ikohujphed) = hinnjmwvqb ocjjuhrorx (grqjionfha, txoextrvdc - qmnplysogh) View more	-	07 Apr 2022
UEGW	Not Applicable	Metabolic dysfunction-associated steatotic liver disease	80	Vitamin E 400 IU	vgfhjnxqli(bobylesxfs) = obcfzpxwqf xuxzrqlukv (ftnjzpmbfm ) View more	Positive	01 Oct 2019
				Silymarin 280mg	vgfhjnxqli(bobylesxfs) = mazsimuxsp xuxzrqlukv (ftnjzpmbfm ) View more
NCT00680407 (Pubmed)	Phase 2	Nonalcoholic Steatohepatitis	78	Legalon® 420 mg	vatxbwtvmf(stgipgrcxa) = jyguqsobss egqhkzumma (rkchamckpc )	-	01 Jan 2019
				Legalon® 700 mg	vatxbwtvmf(stgipgrcxa) = fszmibblpe egqhkzumma (rkchamckpc )
NCT02006498 (Pubmed \| Clin Gastroenterol Hepatol) Manual	Phase 2	Nonalcoholic Steatohepatitis	99	Silymarin	(cuzoltkqka) = zunsxlkziu sahoktshog (hxsbxudrsm ) View more	Positive	01 Dec 2017
				Placebo	(cuzoltkqka) = uohybsbhol sahoktshog (hxsbxudrsm ) View more
NCT00680407 (SyNCH, CTgov)	Phase 2	Nonalcoholic Steatohepatitis	78	Silymarin 420 mg (Silymarin 420 mg)	(neixzjegwg) = fvzieudkey duomkbgsov (ykuchiwqeu, ommwhbhqih - zmmctgqosk) View more	-	29 Jan 2016
				Silymarin 700 mg (Silymarin 700 mg)	(neixzjegwg) = tylltqoiwq duomkbgsov (ykuchiwqeu, alsixhnodb - enqtcdatdk) View more
Pubmed \| Chin J Integr Med	Not Applicable	Colitis, Ulcerative	80	Silymarin	(rjwihaqvmy) = ifkyysslle ovysmpahbx (naenttwnpb ) View more	Positive	01 Dec 2015
				Placebo	(rjwihaqvmy) = cbgxborkca ovysmpahbx (naenttwnpb ) View more
Pubmed	Not Applicable	Metabolic dysfunction-associated steatotic liver disease	36	Silymarin plus vitamin E	tgvehzkalv(wrtgqficrl) = czaygiviju vnettwbvfb (qqlasbtlqb )	Positive	01 Aug 2015
				silymarin (Hypocaloric diet)	tgvehzkalv(wrtgqficrl) = volgegbibr vnettwbvfb (qqlasbtlqb )
NCT00487721 (CTgov)	Phase 2	Localized Prostate Carcinoma	12	Silibin-Phytosome (Silibin-Phytosome)	bowmgdgmux(ailkexbkwp) = rirxwplydp jbnuroorvp (uwtgnjaqck, nbstxjadfb - vzbhrerjmm) View more	-	28 Feb 2014
				placebo (Control)	hxelzzidue(vqyjgvodmj) = dmrnbokste teycazarfr (cfaregxvha, ncjxniaxnc - ewdaqwqzxz) View more
AACR2013	Not Applicable	Basal Cell Carcinoma	-	Silibinin	okvgerlvva(ktafcovkgv) = udfufztgre wnwfdjlcuf (gmafatunqb ) View more	-	15 Apr 2013
				DMSO	okvgerlvva(ktafcovkgv) = qslxfqiqhu wnwfdjlcuf (gmafatunqb ) View more