Inhibitory Activity and Mechanism Investigation of Hypericin as a Novel α-Glucosidase Inhibitor

Dong, Qi; Hu, Na; Yue, Huilan; Wang, Honglun

doi:10.3390/molecules26154566

Cited by 31 publications

(20 citation statements)

References 53 publications

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“…Another compound that has been studied due to its potential anticancer properties [ 61 ] is hypericin, a polycyclic aromatic naphthodianthrone that occurs naturally. It has been previously shown that hypericin induced cell death of human and bovine isolated RPE cells [ 62 , 63 ].…”

Section: Natural Productsmentioning

confidence: 99%

Retinal Toxicity Induced by Chemical Agents

Araújo

Brito

Pereira-Figueiredo

et al. 2022

IJMS

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Vision is an important sense for humans, and visual impairment/blindness has a huge impact in daily life. The retina is a nervous tissue that is essential for visual processing since it possesses light sensors (photoreceptors) and performs a pre-processing of visual information. Thus, retinal cell dysfunction or degeneration affects visual ability and several general aspects of the day-to-day of a person’s lives. The retina has a blood–retinal barrier, which protects the tissue from a wide range of molecules or microorganisms. However, several agents, coming from systemic pathways, reach the retina and influence its function and survival. Pesticides are still used worldwide for agriculture, contaminating food with substances that could reach the retina. Natural products have also been used for therapeutic purposes and are another group of substances that can get to the retina. Finally, a wide number of medicines administered for different diseases can also affect the retina. The present review aimed to gather recent information about the hazard of these products to the retina, which could be used to encourage the search for more healthy, suitable, or less risky agents.

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Section: Natural Productsmentioning

confidence: 99%

Retinal Toxicity Induced by Chemical Agents

Araújo

Brito

Pereira-Figueiredo

et al. 2022

IJMS

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“…Further, hypericin and other bioactive components in the extract from Hypericum humifusum may inhibit acetylcholinesterase and some key enzymes linked to T2D, or downregulate homeobox‐1 (PDX1) expression and Erk activity 87,88 . In addition, hypericin is found to be an effective inhibitor of α‐glucosidase, a major enzyme that is involved in T2D, by altering its structure and microenvironment and reducing its activity 89 …”

Section: Discussionmentioning

confidence: 99%

Hypericin as a potential drug for treating Alzheimer's disease and type 2 diabetes with a view to drug repositioning

et al. 2023

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AimsAlzheimer's disease (AD) and type 2 diabetes (T2D) are two of the most common diseases in elderly population and they have a high rate of comorbidity. Study has revealed that T2D is a major risk factor of AD, and thus exploring therapeutic approaches that can target both diseases has drawn much interest in recent years. In this study, we tried to explore drugs that could be potentially used to prevent or treat both AD and T2D via a drug repositioning approach.MethodsWe first searched the known drugs that may be effective to T2D treatment based on the network distance between the T2D‐associated genes and drugs deposited in the DrugBank database. Then, via molecular docking, we further screened these drugs by examining their interaction with islet amyloid polypeptide (IAPP) and Aβ42 peptide, the key components involved in the pathogenesis of T2D or AD. Finally, the binding between the selected drug candidates and the target proteins was verified by molecular dynamics (MD) simulation; and the potential function of the drug candidates and the corresponding targets were analyzed.ResultsFrom multiple resources, 734 T2D‐associated genes were collected, and a list of 1109 drug candidates for T2D was obtained. We found that hypericin had the lowest binding energy and the most stable interaction with either IAPP or Aβ42 peptide. In addition, we also found that the target genes regulated by hypericin were differentially expressed in the tissues related to the two diseases.ConclusionOur results show that hypericin may be able to bind with IAPP and Aβ42 stably and prevent their accumulation, and thus could be a promising drug candidate for treating the comorbidity of AD and T2D.

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“…In vivo, Hyp suppressed islet β‐cell apoptosis and improved the antioxidative ability of pancreatic tissue, thus ameliorating the function of islet β‐cell. Besides the protective effect on islet β‐cell both in vitro and in vivo, Dong, Hu, et al (2021) found the binding affinities of Hyp with α‐glucosidase were strong and fast, with a maximum IC50 of 4.66 ± 0.27 mg/L. Moreover, hydrogen bonding occurred between Hyp and α‐glucosidase amino acid residues Lys‐156, Ser‐157, Gly‐160, Ser‐240, His‐280, Asp‐242, and Asp‐307, revealing that Hyp could be applied as a novel α‐glucosidase inhibitor to treat diabetes.…”

Section: Pharmacological Effects Of Hypericinmentioning

confidence: 99%

Hypericin as a promising natural bioactive naphthodianthrone: A review of its pharmacology, pharmacokinetics, toxicity, and safety

Peng,

Lu,

Liu

et al. 2023

Phytotherapy Research

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Hypericin can be derived from St. John's wort, which is widely spread around the world. As a natural product, it has been put into clinical practice such as wound healing and depression for a long time. In this article, we review the pharmacology, pharmacokinetics, and safety of hypericin, aiming to introduce the research advances and provide a full evaluation of it. Turns out hypericin, as a natural photosensitizer, exhibits an excellent capacity for anticancer, neuroprotection, and elimination of microorganisms, especially when activated by light, potent anticancer and antimicrobial effects are obtained after photodynamic therapy. The mechanisms of its therapeutic effects involve the induction of cell death, inhibition of cell cycle progression, inhibition of the reuptake of amines, and inhibition of virus replication. The pharmacokinetics properties indicate that hypericin has poor water solubility and bioavailability. The distribution and excretion are fast, and it is metabolized in bile. The toxicity of hypericin is rarely reported and the conventional use of it rarely causes adverse effects except for photosensitization. Therefore, we may conclude that hypericin can be used safely and effectively against a variety of diseases. We hope to provide researchers with detailed guidance and enlighten the development of it.

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Inhibitory Activity and Mechanism Investigation of Hypericin as a Novel α-Glucosidase Inhibitor

Cited by 31 publications

References 53 publications

Retinal Toxicity Induced by Chemical Agents

Retinal Toxicity Induced by Chemical Agents

Hypericin as a potential drug for treating Alzheimer's disease and type 2 diabetes with a view to drug repositioning

Hypericin as a promising natural bioactive naphthodianthrone: A review of its pharmacology, pharmacokinetics, toxicity, and safety

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