scholarly journals Withaferin A: From Ancient Remedy to Potential Drug Candidate

Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7696
Author(s):  
Tahira Sultana ◽  
Mohammad K. Okla ◽  
Madiha Ahmed ◽  
Nosheen Akhtar ◽  
Abdulrahman Al-Hashimi ◽  
...  

Withaferin A (WA) is a pivotal withanolide that has conquered a conspicuous place in research, owning to its multidimensional biological properties. It is an abundant constituent in Withania somnifera Dunal. (Ashwagandha, WS) that is one of the prehistoric pivotal remedies in Ayurveda. This article reviews the literature about the pharmacological profile of WA with special emphasis on its anticancer aspect. We reviewed research publications concerning WA through four databases and provided a descriptive analysis of literature without statistical or qualitative analysis. WA has been found as an effective remedy with multifaceted mechanisms and a broad spectrum of pharmacological profiles. It has anticancer, anti-inflammatory, antiherpetic, antifibrotic, antiplatelet, profibrinolytic, immunosuppressive, antipigmentation, antileishmanial, and healing potentials. Evidence for wide pharmacological actions of WA has been established by both in vivo and in vitro studies. Further, the scientific literature accentuates the role of WA harboring a variable therapeutic spectrum for integrative cancer chemoprevention and cure. WA is a modern drug from traditional medicine that is necessary to be advanced to clinical trials for advocating its utility as a commercial drug.

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.


Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7546
Author(s):  
Heba A. S. El-Nashar ◽  
Mariam I. Gamal El-Din ◽  
Lucian Hritcu ◽  
Omayma A. Eldahshan

Tyrosinase is a multifunctional copper-containing oxidase enzyme that initiates melanin synthesis in humans. Excessive accumulation of melanin pigments or the overexpression of tyrosinase may result in skin-related disorders such as aging spots, wrinkles, melasma, freckles, lentigo, ephelides, nevus, browning and melanoma. Nature expresses itself through the plants as a source of phytochemicals with diverse biological properties. Among these bioactive compounds, flavonoids represent a huge natural class with different categories such as flavones, flavonols, isoflavones, flavan-3-ols, flavanones and chalcones that display antioxidant and tyrosinase inhibitor activities with a diversity of mechanistic approaches. In this review, we explore the role of novel or known flavonoids isolated from different plant species and their participation as tyrosinase inhibitors reported in the last five years from 2016 to 2021. We also discuss the mechanistic approaches through the different studies carried out on these compounds, including in vitro, in vivo and in silico computational research. Information was obtained from Google Scholar, PubMed, and Science Direct. We hope that the updated comprehensive data presented in this review will help researchers to develop new safe, efficacious, and effective drug or skin care products for the prevention of and/or protection against skin-aging disorders.


Blood ◽  
1990 ◽  
Vol 76 (4) ◽  
pp. 655-663 ◽  
Author(s):  
SA Weitzman ◽  
LI Gordon

Abstract We have reviewed some of the data that link the reactive oxygen species produced by inflammatory phagocytes to cancer development. While it is clear that these substances induce phenotypic changes characteristic of those produced by known carcinogens, the precise mechanisms by which these effects are produced require much further study. In vitro, it would appear that phagocyte-generated oxidants could be complete carcinogens, ie, could cause both tumor initiation and promotion. In vivo, however, these substances appear usually to function as tumor promoters or cocarcinogens perhaps because of high levels of endogenous antioxidant defenses. This suggests that there may be even more reason to be optimistic about the potential for positive results in cancer chemoprevention trials in humans, and provides further rationale for the continuing interest in the use of antioxidants and anti- inflammatory drugs in current and future trials. For example, the Chemoprevention Branch of the National Cancer Institute is currently sponsoring seven extramural human efficacy intervention trials testing whether the antioxidant beta carotene can prevent cancer.


2020 ◽  
Vol 66 (1) ◽  
pp. 52-64
Author(s):  
Mariola Dreger ◽  
Artur Adamczak ◽  
Katarzyna Seidler-Łożykowska ◽  
Karolina Wielgus

SummaryFireweed (Epilobium angustifolium L.) is a well-known medicinal plant traditionally used in the treatment of urogenital diseases, stomach and liver disorders, skin problems, etc. E. angustifolium extracts show anti-androgenic, antiproliferative, cytotoxic, antioxidant, anti-inflammatory, immunomodulatory, and antimicrobial activities. The unique combination of biological properties demonstrated by the results of some studies indicates that fireweed has a positive effect in benign prostatic hyperplasia (BPH) and potentially in the prostate cancer chemoprevention. However, the efficacy of E. angustifolium phytotherapy is still poorly tested in clinical trials, while numerous beneficial effects of extracts have been documented in the in vitro and in vivo tests. Fireweed is rich in polyphenolic compounds, particularly ellagitannins. Currently, polyphenols are considered to be modulators of beneficial gut microbiota. The literature data support the use of ellagitannins in the prostate cancer chemoprevention, but caution is advised due to the highly variable production of urolithins by the individual microbiota. A better understanding of the microbiota’s role and the mechanisms of its action are crucial for an optimal therapeutic effect. This paper aims to summarize and discuss experimental data concerning pharmacological properties of E. angustifolium and bioavailability of ellagitannins – important bioactive compounds of this plant.


PPAR Research ◽  
2008 ◽  
Vol 2008 ◽  
pp. 1-10 ◽  
Author(s):  
Yumiko Yasui ◽  
Mihye Kim ◽  
Takuji Tanaka

Peroxisome proliferators-activated receptors (PPARs) that are members of the nuclear receptor superfamily have three different isoforms: PPARα, PPARδ, and PPARγ. PPARs are ligand-activated transcription factors, and they are implicated in tumor progression, differentiation, and apoptosis. Activation of PPAR isoforms lead to both anticarcinogenesis and anti-inflammatory effect. It has so far identified many PPAR ligands including chemical composition and natural occurring. PPAR ligands are reported to activate PPAR signaling and exert cancer prevention and treatment in vitro and/or in vivo studies. Although the effects depend on the isoforms and the types of ligands, biological modulatory activities of PPARs in carcinogenesis and disease progression are attracted for control or combat cancer development. This short review summarizes currently available data on the role of PPAR ligands in carcinogenesis.


Crystals ◽  
2021 ◽  
Vol 11 (6) ◽  
pp. 674
Author(s):  
Silvia Balhuc ◽  
Radu Campian ◽  
Anca Labunet ◽  
Marius Negucioiu ◽  
Smaranda Buduru ◽  
...  

Hydroxyapatite is one of the most studied biomaterials in the medical and dental field, because of its biocompatibility; it is the main constituent of the mineral part of teeth and bones. In dental science, hydroxyapatite nanoparticles (HAnps) or nano-hydroxyapatite (nano-HA) have been studied, over the last decade, in terms of oral implantology and bone reconstruction, as well in restorative and preventive dentistry. Hydroxyapatite nanoparticles have significant remineralizing effects on initial enamel lesions, and they have also been used as an additive material in order to improve existing and widely used dental materials, mainly in preventive fields, but also in restorative and regenerative fields. This paper investigates the role of HAnps in dentistry, including recent advances in the field of its use, as well as their advantages of using it as a component in other dental materials, whether experimental or commercially available. Based on the literature, HAnps have outstanding physical, chemical, mechanical and biological properties that make them suitable for multiple interventions, in different domains of dental science. Further well-designed randomized controlled trials should be conducted in order to confirm all the achievements revealed by the in vitro or in vivo studies published until now.


Author(s):  
Anna Notaro ◽  
Angelo Frei ◽  
Riccardo Rubbiani ◽  
Marta Jakubaszek ◽  
Uttara Basu ◽  
...  

Chemotherapy remains one of the dominant treatments to cure cancer. However, due to the many inherent drawbacks, there is a surge for new chemotherapeutic drugs. More specifically, the discovery of new drug candidates able to overcome severe side effects, the occurrence of resistance and the inefficacy toward metastatic tumours is highly desirable. In this work, we designed a new chemotherapeutic drug candidate against cancer, namely [Ru(DIP)2(sq)]PF6 (Ru-sq) (DIP = 4,7-diphenyl-1,10-phenanthroline; sq = semiquinonate ligand). The aim was to combine the great potential expressed by Ru(II) polypyridyl complexes and the singular redox and biological properties associated to the catecholate moiety. Several pieces of experimental evidence (e.g., X-ray crystallography, electron paramagnetic resonance, electrochemistry) demonstrate that the semiquinonate is the preferred oxidation state of the dioxo ligand in this complex. The biological activity of Ru-sq was then scrutinised in vitro and in vivo, and the results highlight the tremendous potential of this complex as a chemotherapeutic agent against cancer. Ru-sq was notably found have a much higher cytotoxic activity than cisplatin on several cell lines (i.e. in the nanomolar range), and, contrary to cisplatin, to have mitochondrial disfunction as one of its modes of action. The multicellular targets of Ru-sq could potentially be the key to overcome one of the main drawbacks of cisplatin i.e. the occurrence of resistance. Moreover, Ru-sq exhibited impressing activity on Multi Cellular Tumour Spheroids (MCTS) model, leading to a growth inhibition of the tumour even 13 days after treatment (20 μM). Very importantly, using two different in vivo models, it could be demonstrated that this compound is extremely well-tolerated by mice and has a very promising activity, curing, in some cases, tumour-bearing mice.<br>


Blood ◽  
1990 ◽  
Vol 76 (4) ◽  
pp. 655-663 ◽  
Author(s):  
SA Weitzman ◽  
LI Gordon

We have reviewed some of the data that link the reactive oxygen species produced by inflammatory phagocytes to cancer development. While it is clear that these substances induce phenotypic changes characteristic of those produced by known carcinogens, the precise mechanisms by which these effects are produced require much further study. In vitro, it would appear that phagocyte-generated oxidants could be complete carcinogens, ie, could cause both tumor initiation and promotion. In vivo, however, these substances appear usually to function as tumor promoters or cocarcinogens perhaps because of high levels of endogenous antioxidant defenses. This suggests that there may be even more reason to be optimistic about the potential for positive results in cancer chemoprevention trials in humans, and provides further rationale for the continuing interest in the use of antioxidants and anti- inflammatory drugs in current and future trials. For example, the Chemoprevention Branch of the National Cancer Institute is currently sponsoring seven extramural human efficacy intervention trials testing whether the antioxidant beta carotene can prevent cancer.


2015 ◽  
Vol 5 (1) ◽  
Author(s):  
Yingfeng Tu ◽  
Li Liu ◽  
Dongliang Zhao ◽  
Youbin Liu ◽  
Xiaowei Ma ◽  
...  

Abstract Recent studies reported miR-497 exhibited inhibitory effects in various cancers. However, whether miR-497 is involved in inhibiting angiogenesis, which is critical for tumor growth and metastasis, is still unknown. The purpose of this study was to investigate the potential role of miR-497 in tumor angiogenesis. In this work, cell proliferation and apoptosis analyses were conducted to explore the potential function of miR-497 in HUVECs by using MTT and TUNEL assays. Western blotting (WB) was employed to validate the downstream targets of miR-497. Furthermore, in order to disclose the role of miR-497 on angiogenesis, VEGFR2-luc transgenic mice were treated with miR-497 mimic and applied to monitor tumor angiogenesis and growth by in vivo bioluminescent imaging (BLI). The results demonstrated that overexpression of miR-497 showed inhibitory effects on VEGFR2 activation and downstream Raf/MEK/ERK signal pathways in vitro and in vivo. Moreover, overexpression of miR-497 effectively induced HUVECs apoptosis by targeting VEGFR2 and downstream PI3K/AKT signaling pathway. Furthermore, miR-497 exhibited anti-angiogenesis and anti-tumor effects in the VEGFR2-luc breast tumor model proven by BLI, WB and immunohistochemistry analysis. In summary, miR-497 inhibits tumor angiogenesis and growth via targeting VEGFR2, indicating miR-497 can be explored as a potential drug candidate for cancer therapy.


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