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Shikonin and its derivatives are excellent representatives of biologically active naphthoquinones. A wide range of investigations carried out in the last few decades validated their pharmacological efficacy. Besides having magnificent therapeutic potential, shikonin and its derivatives suffer from various pharmacokinetic, toxicity, and stability issues like poor bioavailability, nephrotoxicity, photodegradation, etc. Recently, various research groups have developed an extensive range of formulations to tackle these issues to ease their path to clinical practice. The latest formulation approaches have been focused on exploiting the unique features of novel functional excipients, which in turn escalate the therapeutic effect of shikonin. Moreover, the codelivery approach in various drug delivery systems has been taken into consideration in a recent while to reduce toxicity associated with shikonin and its derivatives. This review sheds light on the essential reports and patents published related to the array of formulations containing shikonin and its derivatives.
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http://dx.doi.org/10.2174/2667387816666220302112201 | DOI Listing |
Bioorg Med Chem Lett
August 2025
Natural Medicine Research Center, Department of Pharmacy, Sichuan Agricultural University, Chengdu 611130, China. Electronic address:
Acute lung injury (ALI) is a serious and prevalent clinical condition with limited treatments. Recent research has highlighted the potential of targeting inflammatory pathways as a therapeutic strategy for ALI. In this study, a series of shikonin ester derivatives were synthesized by introducing various acyl groups into shikonin.
View Article and Find Full Text PDFChem Biodivers
August 2025
College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian, China.
Diabetic foot ulcers (DFUs) exhibit impaired healing due to disrupted macrophage polarization, wherein persistent hyperglycemia inhibits the critical M1-to-M2 phenotypic transition, sustaining a pro-inflammatory microenvironment. This investigation elucidates the therapeutic potential of L-shikonin (L-SK), a bioactive phytochemical derived from comfrey with established immunomodulatory properties. In a streptozotocin-induced diabetic murine model, L-SK treatment significantly enhanced wound closure through coordinated anti-inflammatory effects (downregulation of CD86 and tumor necrosis factor-α) and pro-regenerative outcomes (increased collagen deposition and CD31-mediated angiogenesis).
View Article and Find Full Text PDFChem Biodivers
July 2025
Department of Second Affiliated Hospital, Dalian Medical University, Dalian, China.
Innovative therapeutic strategies for pancreatic cancer have become an increasingly prominent area of biomedical research. Natural compounds, prized for their structural complexity and diverse bioactivities, remain a valuable source for drug discovery. Shikonin (SHK), a naturally occurring naphthoquinone, has demonstrated potent anti-tumor properties across various cancer types.
View Article and Find Full Text PDFPhytomedicine
September 2025
Shanghai University of Traditional Chinese Medicine, Cailun Road 1200, Shanghai 201203, China; Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Haike Road #501, Shanghai 201203, China; School of Pharmacy, Hangzhou Normal University, Zhejiang, 311121, Hangzhou, China. Electronic add
Background: The "one-to-multiple" phenomenon and counterfeiting are prevalent in herbal medicines. Accurately identifying these issues in both crude herbs and commercial formulated products is crucial for ensuring drug safety and efficacy. However, this task remains inherently challenging due to the complex nature of the matrices involved.
View Article and Find Full Text PDFSci Rep
July 2025
Amway Corporation, Ada, MI, 49301, USA.
The main protease (M) of SARS-CoV-2 plays a crucial role in viral replication and is a prime target for therapeutic interventions. Phytochemicals, known for their antiviral properties, have been previously identified as potential M inhibitors in several in silico studies. However, the efficacy of these remains in question owing to the inherent flexibility of the M binding site, posing challenges in selecting suitable protein structures for virtual screening.
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