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19 pages, 2243 KiB

Open AccessArticle

Design and Synthesis of Brefeldin A-Isothiocyanate Derivatives with Selectivity and Their Potential for Cervical Cancer Therapy

by Mingying Wang, Xiaoyuan Chen, Ying Qu, Qingyinglu Ma, Huaqi Pan, Haonan Li, Huiming Hua and Dahong Li

Molecules 2023, 28(11), 4284; https://doi.org/10.3390/molecules28114284 - 23 May 2023

Cited by 1 | Viewed by 1381

Abstract

Brefeldin A has a wide range of anticancer activity against a variety of tumor cells. Its poor pharmacokinetic properties and significant toxicity seriously hinder its further development. In this manuscript, 25 brefeldin A-isothiocyanate derivatives were designed and synthesized. Most derivatives showed good selectivity [...] Read more.

Brefeldin A has a wide range of anticancer activity against a variety of tumor cells. Its poor pharmacokinetic properties and significant toxicity seriously hinder its further development. In this manuscript, 25 brefeldin A-isothiocyanate derivatives were designed and synthesized. Most derivatives showed good selectivity between HeLa cells and L-02 cells. In particular, 6 exhibited potent antiproliferative activity against HeLa cells (IC₅₀ = 1.84 μM) with no obvious cytotoxic activity to L-02 (IC₅₀ > 80 μM). Further cellular mechanism tests indicated that 6 induced HeLa cell cycle arrest at G1 phase. Cell nucleus fragmentation and decreased mitochondrial membrane potential suggested 6 could induce apoptosis in HeLa cells through the mitochondrial-dependent pathway. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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12 pages, 2801 KiB

Open AccessArticle

Novel Vulgarin Derivatives: Chemical Transformation, In Silico and In Vitro Studies

by Hanan G. Sary, Mohammed A. Khedr and Khaled Y. Orabi

Molecules 2023, 28(8), 3421; https://doi.org/10.3390/molecules28083421 - 13 Apr 2023

Viewed by 1643

Abstract

Vulgarin, an eudesmanolide sesquiterpene isolated from Artemisia judaica, was refluxed with iodine to produce two derivatives (1 and 2), which were purified and spectroscopically identified as naproxen methyl ester analogs. The reaction mechanism by which 1 and 2 were formed [...] Read more.

Vulgarin, an eudesmanolide sesquiterpene isolated from Artemisia judaica, was refluxed with iodine to produce two derivatives (1 and 2), which were purified and spectroscopically identified as naproxen methyl ester analogs. The reaction mechanism by which 1 and 2 were formed is explained using a sigmatropic reaction with a 1,3 shift. The scaffold hopping via lactone ring opening enabled the new derivatives of vulgarin (1 and 2) to fit well inside the COX-2 active site with ΔG of −7.73 and −7.58 kcal/mol, respectively, which was better than that of naproxen (ΔG of −7.04 kcal/mol). Moreover, molecular dynamic simulations showed that 1 was able to achieve a faster steady-state equilibrium than naproxen. The novel derivative 1 showed promising cytotoxic activities against HepG-2, HCT-116, MCF-7, and A-549 cancer cell lines compared to those of vulgarin and naproxen. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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11 pages, 2229 KiB

Open AccessCommunication

Permethrin as a Potential Furin Inhibitor through a Novel Non-Competitive Allosteric Inhibition

by Dongyan Feng, Le Ren, Jiaqi Wu, Lingling Guo, Zhitao Han, Jingjing Yang, Wei Xie, Yanbing Wang, Fanxing Xu, Xin Su, Dahong Li and Hao Cao

Molecules 2023, 28(4), 1883; https://doi.org/10.3390/molecules28041883 - 16 Feb 2023

Cited by 1 | Viewed by 1930

Abstract

Furin is a potential target protein associated with numerous diseases; especially closely related to tumors and multiple viral infections including SARS-CoV-2. Most of the existing efficient furin inhibitors adopt a substrate analogous structure, and other types of small molecule inhibitors need to be [...] Read more.

Furin is a potential target protein associated with numerous diseases; especially closely related to tumors and multiple viral infections including SARS-CoV-2. Most of the existing efficient furin inhibitors adopt a substrate analogous structure, and other types of small molecule inhibitors need to be discovered urgently. In this study, a high-throughput screening combining virtual and physical screening of natural product libraries was performed, coupled with experimental validation and preliminary mechanistic assays at the molecular level, cellular level, and molecular simulation. A novel furin inhibitor, permethrin, which is a derivative from pyrethrin I generated by Pyrethrum cinerariifolium Trev. was identified, and this study confirmed that it binds to a novel allosteric pocket of furin through non-competitive inhibition. It exhibits a very favorable protease-selective inhibition and good cellular activity and specificity. In summary, permethrin shows a new parent nucleus with a new mode of inhibition. It could be used as a highly promising lead compound against furin for targeting related tumors and various resistant viral infections, including SARS-CoV-2. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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16 pages, 4206 KiB

Open AccessArticle

Integration of Two-Dimensional Liquid Chromatography-Mass Spectrometry and Molecular Docking to Characterize and Predict Polar Active Compounds in Curcuma kwangsiensis

by Kaijing Xiang, Weijia Zhou, Tao Hou, Long Yu, Han Zhou, Liangliang Zhou, Yanfang Liu, Jixia Wang, Zhimou Guo and Xinmiao Liang

Molecules 2022, 27(22), 7715; https://doi.org/10.3390/molecules27227715 - 9 Nov 2022

Cited by 2 | Viewed by 1904

Abstract

Curcuma kwangsiensis, one species of Curcumae zedoaria Ros. c, is a commonly used traditional Chinese medicine (TCM) for treating cardiovascular disease, cancer, asthma and inflammation. Polar compounds are abundant in water decoction, which would be responsible for critical pharmacological effects. However, [...] Read more.

Curcuma kwangsiensis, one species of Curcumae zedoaria Ros. c, is a commonly used traditional Chinese medicine (TCM) for treating cardiovascular disease, cancer, asthma and inflammation. Polar compounds are abundant in water decoction, which would be responsible for critical pharmacological effects. However, current research on polar compounds in Curcumae zedoaria Ros. c remains scarce. In this study, the polar fraction from Curcuma kwangsiensis was firstly profiled on G protein-coupled receptor 109A (GPR109A), β2-adrenergic receptor (β2-AR), neurotensin receptor (NTSR), muscarinic-3 acetylcholine receptor (M3) and G protein-coupled receptor 35 (GPR35), which were involved in its clinical indications and exhibited excellent β2-AR and GPR109A receptor activities. Then, an offline two-dimensional reversed-phase liquid chromatography (RPLC) coupled with the hydrophilic interaction chromatography (HILIC) method was developed to separate polar compounds. By the combination of a polar-copolymerized XAqua C18 column and an amide-bonded XAmide column, an orthogonality of 47.6% was achieved. As a result of coupling with the mass spectrometry (MS), a four-dimensional data plot was presented in which 373 mass peaks were detected and 22 polar compounds tentatively identified, including the GPR109A agonist niacin. Finally, molecular docking of these 22 identified compounds to β2-AR, M3, GPR35 and GPR109A receptors was performed to predict potential active ingredients, and compound 9 was predicted to have a similar interaction to the β2-AR partial agonist salmeterol. These results were supplementary to the material basis of Curcuma kwangsiensis and facilitated the bioactivity research of polar compounds. The integration of RPLC×HILIC-MS and molecular docking can be a powerful tool for characterizing and predicting polar active components in TCM. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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12 pages, 1636 KiB

Open AccessArticle

Effects of Different Extraction Methods in Pharmacopoeia on the Content and Structure Transformation of Ginsenosides

by Hui Li, Hua Jiang, Lei Xu, Yaling Deng, Jing Xu and Yuqing Zhao

Molecules 2022, 27(14), 4347; https://doi.org/10.3390/molecules27144347 - 6 Jul 2022

Cited by 10 | Viewed by 2115

Abstract

Ginseng (Panax ginseng C. A. Meyer), a perennial herb, possesses immunostimulatory, anticarcinogenic, antiemetic, and antioxidative biological activities. In recent years, more and more people have paid attention to the extraction methods and quality evaluation of ginseng. China, the United States, Europe, Japan, [...] Read more.

Ginseng (Panax ginseng C. A. Meyer), a perennial herb, possesses immunostimulatory, anticarcinogenic, antiemetic, and antioxidative biological activities. In recent years, more and more people have paid attention to the extraction methods and quality evaluation of ginseng. China, the United States, Europe, Japan, and Korea have all had the quality standards and content determination methods of ginseng. The different treatment methods are adopted before the determination of ginseng samples and the content limits of the index components, such as ginsenoside Rb₁, ginsenoside Rg₁, and ginsenoside Re exist differences. The similarities and differences of ginseng content detection methods in pharmacopoeias of different countries have been analyzed by a research group, but the comparison of the effects of different methods on the ginsenoside content and structural transformation has not been reported. In this paper, ginsenosides in ginseng were extracted according to four national pharmacopoeias and analyzed quantitatively and qualitatively by UPLC-Q-Exactive-MS and HPLC-UV. It was illustrated that the pretreatment method has a significant influence on the content determination of ginseng. The yield of rare saponins was increased by heating concluded from both the qualitative and quantitative comparison. Finally, a simple and feasible extraction method was optimized by response surface method at room temperature. The analysis of the preparation method and process optimization of the four pharmacopoeias can provide important reference information for the revision of ginseng standards. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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14 pages, 3120 KiB

Open AccessArticle

Identification of a Hydrogen-Sulfide-Releasing Isochroman-4-One Hybrid as a Cardioprotective Candidate for the Treatment of Cardiac Hypertrophy

by Yu Wang, Yuechen Liu, Hongyu Wu, Shengtao Xu and Fenfen Ma

Molecules 2022, 27(13), 4114; https://doi.org/10.3390/molecules27134114 - 27 Jun 2022

Cited by 1 | Viewed by 1783

Abstract

Cardiac pathological hypertrophy is associated with undesirable epigenetic changes and causes maladaptive cardiac remodeling and heart failure, leading to high mortality rates. Specific drugs for the treatment of cardiac hypertrophy are still in urgent need. In the present study, a hydrogen-sulfide-releasing hybrid 13-E [...] Read more.

Cardiac pathological hypertrophy is associated with undesirable epigenetic changes and causes maladaptive cardiac remodeling and heart failure, leading to high mortality rates. Specific drugs for the treatment of cardiac hypertrophy are still in urgent need. In the present study, a hydrogen-sulfide-releasing hybrid 13-E was designed and synthesized by appending p-hydroxythiobenzamide (TBZ), an H₂S-releasing donor, to an analog of our previously discovered cardioprotective natural product XJP, 7,8-dihydroxy-3-methyl-isochromanone-4. This hybrid 13-E exhibited excellent H₂S-generating ability and low cellular toxicity. The 13-E protected against cardiomyocyte hypertrophy In Vitro and reduced the induction of Anp and Bnp. More importantly, 13-E could reduce TAC-induced cardiac hypertrophy In Vivo, alleviate cardiac interstitial fibrosis and restore cardiac function. Unbiased transcriptomic analysis showed that 13-E regulated the AMPK signaling pathway and influenced fatty acid metabolic processes, which may be attributed to its cardioprotective activities. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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19 pages, 4484 KiB

Open AccessArticle

UPLC-G2Si-HDMS Untargeted Metabolomics for Identification of Yunnan Baiyao’s Metabolic Target in Promoting Blood Circulation and Removing Blood Stasis

by Qingyu Zhang, Aihua Zhang, Fangfang Wu and Xijun Wang

Molecules 2022, 27(10), 3208; https://doi.org/10.3390/molecules27103208 - 17 May 2022

Cited by 5 | Viewed by 2637

Abstract

Yunnan Baiyao is a famous Chinese patent medicine in Yunnan Province. However, its mechanism for promoting blood circulation and removing blood stasis is not fully explained. Our study used metabonomics technology to reveal the regulatory effect of Yunnan Baiyao on small molecular metabolites [...] Read more.

Yunnan Baiyao is a famous Chinese patent medicine in Yunnan Province. However, its mechanism for promoting blood circulation and removing blood stasis is not fully explained. Our study used metabonomics technology to reveal the regulatory effect of Yunnan Baiyao on small molecular metabolites in promoting blood circulation and removing blood stasis, and exploring the related urine biomarkers. The coagulation function, blood rheology, and pathological results demonstrated that after Yunnan Baiyao treatment, the pathological indexes in rats with epinephrine hydrochloride-induced blood stasis syndrome improved and returned to normal levels. This is the basis for the effectiveness of Yunnan Baiyao. UPLC-G2Si-HDMS was used in combination with multivariate statistical analysis to conduct metabonomic analysis of urine samples. Finally, using mass spectrometry technology, 28 urine biomarkers were identified, clarifying the relevant metabolic pathways that play a vital role in the Yunnan Baiyao treatment. These were used as the target for Yunnan Baiyao to promote blood circulation and remove blood stasis. This study showed that metabolomics strategies provide opportunities and conditions for a deep and systematic understanding of the mechanism of action of prescriptions. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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20 pages, 2586 KiB

Open AccessArticle

Novel and Potent Acetylcholinesterase Inhibitors for the Treatment of Alzheimer’s Disease from Natural (±)-7,8-Dihydroxy-3-methyl-isochroman-4-one

by Xinnan Li, Yilin Jia, Junda Li, Pengfei Zhang, Tiantian Li, Li Lu, Hequan Yao, Jie Liu, Zheying Zhu and Jinyi Xu

Molecules 2022, 27(10), 3090; https://doi.org/10.3390/molecules27103090 - 11 May 2022

Cited by 5 | Viewed by 2156

Abstract

Alzheimer’s disease (AD) is a neurodegenerative disease that causes memory and cognitive decline as well as behavioral problems. It is a progressive and well recognized complex disease; therefore, it is very urgent to develop novel and effective anti-AD drugs. In this study, a [...] Read more.

Alzheimer’s disease (AD) is a neurodegenerative disease that causes memory and cognitive decline as well as behavioral problems. It is a progressive and well recognized complex disease; therefore, it is very urgent to develop novel and effective anti-AD drugs. In this study, a series of novel isochroman-4-one derivatives from natural (±)-7,8-dihydroxy-3-methyl-isochroman-4-one [(±)-XJP] were designed and synthesized, and their anti-AD potential was evaluated. Among them, compound 10a [(Z)-3-acetyl-1-benzyl-4-((6,7-dimethoxy-4-oxoisochroman-3-ylidene)methyl)pyridin-1-ium bromide] possessed potent anti-acetylcholinesterase (AChE) activity as well as modest antioxidant activity. Further molecular modeling and kinetic investigations revealed that compound 10a was a dual-binding inhibitor that binds to both catalytic anionic site (CAS) and peripheral anionic site (PAS) of the enzyme AChE. In addition, compound 10a exhibited low cytotoxicity and moderate anti-Aβ aggregation efficacy. Moreover, the in silico screening suggested that these compounds could pass across the blood–brain barrier with high penetration. These findings show that compound 10a was a promising lead from a natural product with potent AChE inhibitory activity and deserves to be further developed for the prevention and treatment of AD. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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20 pages, 6425 KiB

Open AccessArticle

Phytochemical Composition and Protective Effect of Vernonanthura polyanthes Leaf against In Vivo Doxorubicin-Mediated Toxicity

by Jamira Dias Rocha, Marilia Elias Gallon, Abel Vieira de Melo Bisneto, Vanessa Cristiane Santana Amaral, Luciane Madureira de Almeida, Leonardo Luiz Borges, Lee Chen-Chen, Leonardo Gobbo-Neto and Elisa Flávia Luiz Cardoso Bailão

Molecules 2022, 27(8), 2553; https://doi.org/10.3390/molecules27082553 - 15 Apr 2022

Cited by 2 | Viewed by 1918

Abstract

Vernonanthura polyanthes (Spreng.) A.J. Vega & Dematt. (syn.: Vernonia polyanthes Less) is popularly known as “assa-peixe” and its leaves are used in folk medicine mainly to treat respiratory diseases. In this study, we evaluated the cytogenotoxic and anticytogenotoxic potential of the V. polyanthes [...] Read more.

Vernonanthura polyanthes (Spreng.) A.J. Vega & Dematt. (syn.: Vernonia polyanthes Less) is popularly known as “assa-peixe” and its leaves are used in folk medicine mainly to treat respiratory diseases. In this study, we evaluated the cytogenotoxic and anticytogenotoxic potential of the V. polyanthes leaf aqueous extract (VpLAE) and its n-butanol fraction (n-BF) in the presence or absence of doxorubicin (DXR) (pre-, co-, and post-treatments) on a murine model for 24 h or 120 h. The micronucleus test (MN) and the comet assay were used to assess the cytogenotoxic and anticytogenotoxic potential of VpLAE and n-BF (250, 500, and 1000 mg/kg) administered via gavage to Swiss Webster mice. The chemical profiles of VpLAE and n-BF were assessed by liquid chromatography coupled to mass spectrometry, and their metabolites were putatively identified. Lastly, the possible biological activities related to the (anti) cytogenotoxicity of the compounds were predicted using the PASS online webserver. The in vivo results showed that different doses of VpLAE and n-BF did not present cytotoxic activity; however, the MN test revealed a slight mutagenic activity for the 24 h treatments. Moderate genotoxic effects were demonstrated for all treatments in the comet assay. Regarding anticytotoxicity and antimutagenicity, VpLAE and n-BF presented a high cytoprotective potential against DXR toxic effects. In the co-treatment, VpLAE reduced the DXR genotoxicity by ~27%, and n-BF did not demonstrate antigenotoxic potential. In contrast, an antigenotoxic effect was observed for both VpLAE and n-BF in the pre- and post-treatments, reducing DXR genotoxicity by ~41% and ~47%, respectively. Chemical analysis of VpLAE and n-BF showed the presence of eight phenolic compounds, including seven chlorogenic acids and a flavonoid. The PASS online tool predicted antimutagenic, anticancer, antineoplastic, chemoprotective, antioxidant, and radical scavenging activities for all constituents identified in VpLAE and n-BF. V. polyanthes leaves presented a protective effect against DXR cytogenotoxicity. In general, VpLAE and n-BF showed a greater antigenotoxic potential in the pre- and post-treatments. The metabolites putatively identified in VpLAE and n-BF exhibited antioxidant and chemoprotective potential according to computational prediction analysis. Altogether, our results highlight the potential application of V. polyanthes to protect against toxic manifestations induced by DXR. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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Review

Jump to: Research

22 pages, 2820 KiB

Open AccessReview

A Review: Pharmacological Effect of Natural Compounds in Diospyros kaki Leaves from the Perspective of Oxidative Stress

by Chong Hong, Xu Wang, Jianjian Xu, Jianxing Guo, Houlin Peng and Yan Zhang

Molecules 2024, 29(1), 215; https://doi.org/10.3390/molecules29010215 - 30 Dec 2023

Viewed by 1428

Abstract

Oxidative stress is caused by an imbalance between reactive oxygen species and antioxidant levels. Current research suggests that oxidative stress is one of the key factors in the development of many chronic diseases, and it has been a concern for many years. Many [...] Read more.

Oxidative stress is caused by an imbalance between reactive oxygen species and antioxidant levels. Current research suggests that oxidative stress is one of the key factors in the development of many chronic diseases, and it has been a concern for many years. Many natural compounds have been studied for their special free-radical-scavenging properties. The major chemical constituents of the leaves of Diospyros kaki are flavonoids and triterpenoids, both of which are potential antioxidants that can prevent damage caused by reactive oxygen species or reactive nitrogen species and ameliorate diseases associated with oxidative stress. In addition to the major constituents such as flavonoids and triterpenoids, the leaves of Diospyros kaki include compounds such as phenylpropanoids, alkaloids, phenolic acids, and terpenes. Studies have shown these compounds have certain antioxidant and neuroprotective activities. Experiments have shown that flavonoids or the extracts from the leaves of Diospyros kaki have a variety of good pharmacological activities, which could activate oxidative stress and mitochondrial apoptosis, inhibit the proliferation of human prostate cancer cells and induce apoptosis. It also could achieve the effect of anti-cancer cell proliferation and induce apoptosis by regulating oxidative stress. The main chemical substance of the leaves of Diospyros kaki regulating oxidative stress may be these multi-hydroxyl structure compounds. These natural products exhibit significant antioxidant activity and are an important basis for the leaves of Diospyros kaki to treat human diseases by regulating oxidative stress. This review summarizes the structural types of natural products in the leaves of Diospyros kaki and elaborates the mechanism of the leaves of Diospyros kaki in neuroprotection, anti-diabetes, renal protection, retinal degenerative diseases, and anti-cancer from a new perspective of oxidative stress, including how it supplements other pharmacological effects. The chemical constituents and pharmacological effects of the leaves of Diospyros kaki are summarized in this paper. The relationship between the chemical components in the leaves of Diospyros kaki and their pharmacological effects is summarized from the perspective of oxidative stress. This review provides a reference for the study of natural anti-oxidative stress drugs. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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13 pages, 1782 KiB

Open AccessReview

Use of Ferulic Acid in the Management of Diabetes Mellitus and Its Complications

by Xu Li, Jingxian Wu, Fanxing Xu, Chun Chu, Xiang Li, Xinyi Shi, Wen Zheng, Zhenzhong Wang, Ying Jia and Wei Xiao

Molecules 2022, 27(18), 6010; https://doi.org/10.3390/molecules27186010 - 15 Sep 2022

Cited by 27 | Viewed by 2878

Abstract

Diabetes mellitus, a metabolic disease mainly characterized by hyperglycemia, is becoming a serious social health problem worldwide with growing prevalence. Many natural compounds have been found to be effective in the prevention and treatment of diabetes, with negligible toxic effects. Ferulic acid (FA), [...] Read more.

Diabetes mellitus, a metabolic disease mainly characterized by hyperglycemia, is becoming a serious social health problem worldwide with growing prevalence. Many natural compounds have been found to be effective in the prevention and treatment of diabetes, with negligible toxic effects. Ferulic acid (FA), a phenolic compound commonly found in medicinal herbs and the daily diet, was proved to have several pharmacological effects such as antihyperglycemic, antihyperlipidemic and antioxidant actions, which are beneficial to the management of diabetes and its complications. Data from PubMed, EM-BASE, Web of Science and CNKI were searched with the keywords ferulic acid and diabetes mellitus. Finally, 28 articles were identified after literature screening, and the research progress of FA for the management of DM and its complications was summarized in the review, in order to provide references for further research and medical applications of FA. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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13 pages, 1492 KiB

Open AccessReview

The Therapeutic Potential of Kaemferol and Other Naturally Occurring Polyphenols Might Be Modulated by Nrf2-ARE Signaling Pathway: Current Status and Future Direction

by Yaseen Hussain, Haroon Khan, Khalaf F. Alsharif, Amjad Hayat Khan, Michael Aschner and Luciano Saso

Molecules 2022, 27(13), 4145; https://doi.org/10.3390/molecules27134145 - 28 Jun 2022

Cited by 13 | Viewed by 2581

Abstract

Kaempferol is a natural flavonoid, which has been widely investigated in the treatment of cancer, cardiovascular diseases, metabolic complications, and neurological disorders. Nrf2 (nuclear factor erythroid 2-related factor 2) is a transcription factor involved in mediating carcinogenesis and other ailments, playing an important [...] Read more.

Kaempferol is a natural flavonoid, which has been widely investigated in the treatment of cancer, cardiovascular diseases, metabolic complications, and neurological disorders. Nrf2 (nuclear factor erythroid 2-related factor 2) is a transcription factor involved in mediating carcinogenesis and other ailments, playing an important role in regulating oxidative stress. The activation of Nrf2 results in the expression of proteins and cytoprotective enzymes, which provide cellular protection against reactive oxygen species. Phytochemicals, either alone or in combination, have been used to modulate Nrf2 in cancer and other ailments. Among them, kaempferol has been recently explored for its anti-cancer and other anti-disease therapeutic efficacy, targeting Nrf2 modulation. In combating cancer, diabetic complications, metabolic disorders, and neurological disorders, kaempferol has been shown to regulate Nrf2 and reduce redox homeostasis. In this context, this review article highlights the current status of the therapeutic potential of kaempferol by targeting Nrf2 modulation in cancer, diabetic complications, neurological disorders, and cardiovascular disorders. In addition, we provide future perspectives on kaempferol targeting Nrf2 modulation as a potential therapeutic approach. Full article

(This article belongs to the Special Issue Natural Compounds: A Lead for Drug Discovery and Development)

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