Guar gum micro-vehicle mediated delivery strategy and synergistic activity of thymoquinone and piperine: An in vitro study on bacterial and hepatocellular carcinoma cells

Das, Sankha Subhra; Bera, Debabrata; Pal, Kunal; Mondal, Dheeraj; Karmakar, Parimal; Das, Sukhen; Dey, Anindita

doi:10.1016/j.jddst.2020.101994

Cited by 13 publications

(6 citation statements)

References 43 publications

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“…A TQ-capped magnetic nanoparticle of iron oxide improved endocytotic internalization in breast cancer cells (MDA-MB-231 cells) and displayed a potent synergistic chemo-photothermal effect compared with free TQ [ 205 ]. Guar gum microvehicles rapidly release TQ in the intracellular acidic environment of cancer cells (pH~ 5.5) compared to physiological pH (~7.4), due to breakdown of the interlinking bonds in an acidic environment, leading to prolonged TQ release, with synergistic anticancer activity, as investigated in HepG2 cell line [ 206 ].…”

Section: Neoplasm and Its Pathogenesismentioning

confidence: 99%

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

et al. 2021

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Cancer causes a considerable amount of mortality in the world, while arthritis is an immunological dysregulation with multifactorial pathogenesis including genetic and environmental defects. Both conditions have inflammation as a part of their pathogenesis. Resistance to anticancer and disease-modifying antirheumatic drugs (DMARDs) happens frequently through the generation of energy-dependent transporters, which lead to the expulsion of cellular drug contents. Thymoquinone (TQ) is a bioactive molecule with anticancer as well as anti-inflammatory activities via the downregulation of several chemokines and cytokines. Nevertheless, the pharmacological importance and therapeutic feasibility of thymoquinone are underutilized due to intrinsic pharmacokinetics, including short half-life, inadequate biological stability, poor aqueous solubility, and low bioavailability. Owing to these pharmacokinetic limitations of TQ, nanoformulations have gained remarkable attention in recent years. Therefore, this compilation intends to critically analyze recent advancements in rheumatoid arthritis and cancer delivery of TQ. This literature search revealed that nanocarriers exhibit potential results in achieving targetability, maximizing drug internalization, as well as enhancing the anti-inflammatory and anticancer efficacy of TQ. Additionally, TQ-NPs (thymoquinone nanoparticles) as a therapeutic payload modulated autophagy as well as enhanced the potential of other drugs when given in combination. Moreover, nanoformulations improved pharmacokinetics, drug deposition, using EPR (enhanced permeability and retention) and receptor-mediated delivery, and enhanced anti-inflammatory and anticancer properties. TQ’s potential to reduce metal toxicity, its clinical trials and patents have also been discussed.

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Section: Neoplasm and Its Pathogenesismentioning

confidence: 99%

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

et al. 2021

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“…Interestingly, TQ was found to play the major role in inducing the caspase-mediated apoptosis[ 149 ]. In another study, the encapsulation of TQ and piperine in micro-vehicles made of a natural polymer guar gum extracted from the seeds of Cymompsis tetraganolobus plant[ 150 ] synergistically reduced the viability of hepatocellular carcinoma cells[ 151 ]. This was associated with ROS generation as indicated by an enhanced decrease in the level of intracellular antioxidant glutathione and nicotinamide-adenine dinucleotide phosphate[ 151 ].…”

Section: Tq Effects Against Cancer Cellsmentioning

confidence: 99%

“…In another study, the encapsulation of TQ and piperine in micro-vehicles made of a natural polymer guar gum extracted from the seeds of Cymompsis tetraganolobus plant[ 150 ] synergistically reduced the viability of hepatocellular carcinoma cells[ 151 ]. This was associated with ROS generation as indicated by an enhanced decrease in the level of intracellular antioxidant glutathione and nicotinamide-adenine dinucleotide phosphate[ 151 ]. Two studies assessed the anticancer effectiveness of combining TQ with resveratrol, a stilbene polyphenolic compound extracted from over 70 plants including Polygonum cuspidatum[ 152 ].…”

Section: Tq Effects Against Cancer Cellsmentioning

confidence: 99%

Therapeutic potential of thymoquinone in combination therapy against cancer and cancer stem cells

Fatfat¹,

Fatfat²,

Gali‐Muhtasib³

2021

WJCO

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The long-term success of standard anticancer monotherapeutic strategies has been hampered by intolerable side effects, resistance to treatment and cancer relapse. These monotherapeutic strategies shrink the tumor bulk but do not effectively eliminate the population of self-renewing cancer stem cells (CSCs) that are normally present within the tumor. These surviving CSCs develop mechanisms of resistance to treatment and refuel the tumor, thus causing cancer relapse. To ensure durable tumor control, research has moved away from adopting the monotreatment paradigm towards developing and using combination therapy. Combining different therapeutic modalities has demonstrated significant therapeutic outcomes by strengthening the anti-tumor potential of monotreatment against cancer and cancer stem cells, mitigating their toxic adverse effects, and ultimately overcoming resistance. Recently, there has been growing interest in combining natural products from different sources or with clinically used chemotherapeutics to further improve treatment efficacy and tolerability. Thymoquinone (TQ), the main bioactive constituent of Nigella sativa, has gained great attention in combination therapy research after demonstrating its low toxicity to normal cells and remarkable anticancer efficacy in extensive preclinical studies in addition to its ability to target chemoresistant CSCs. Here, we provide an overview of the therapeutic responses resulting from combining TQ with conventional therapeutic agents such as alkylating agents, antimetabolites and antimicrotubules as well as with topoisomerase inhibitors and non-coding RNA. We also review data on anticancer effects of TQ when combined with ionizing radiation and several natural products such as vitamin D3, melatonin and other compounds derived from Chinese medicinal plants. The focus of this review is on two outcomes of TQ combination therapy, namely eradicating CSCs and treating various types of cancers. In conclusion, the ability of TQ to potentiate the anticancer activity of many chemotherapeutic agents and sensitize cancer cells to radiotherapy makes it a promising molecule that could be used in combination therapy to overcome resistance to standard chemotherapeutic agents and reduce their associated toxicities.

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“…Multidrug-resistant cancers were targeted and treated by curcumin–piperine dual drug-loaded nanoparticles [ 85 ]. Guar gum microvehicle loaded with thymoquinone and piperine exhibited low median lethal dose (LD50) value against human hepatocellular carcinoma cell lines [ 86 ]. Piperine-free extract of Piper nigrum exhibited anticancer effects on cholangiocarcinoma cell lines [ 87 ].…”

Section: Main Textmentioning

confidence: 99%

Molecular and pharmacological aspects of piperine as a potential molecule for disease prevention and management: evidence from clinical trials

Tripathi

Ray

Mishra

2022

Beni-Suef Univ J Basic Appl Sci

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Background Piperine is a type of amide alkaloid that exhibits pleiotropic properties like antioxidant, anticancer, anti-inflammatory, antihypertensive, hepatoprotective, neuroprotective and enhancing bioavailability and fertility-related activities. Piperine has the ability to alter gastrointestinal disorders, drug-metabolizing enzymes, and bioavailability of several drugs. The present review explores the available clinical and preclinical data, nanoformulations, extraction process, structure–activity relationships, molecular docking, bioavailability enhancement of phytochemicals and drugs, and brain penetration properties of piperine in the prevention, management, and treatment of various diseases and disorders. Main body Piperine provides therapeutic benefits in patients suffering from diabetes, obesity, arthritis, oral cancer, breast cancer, multiple myeloma, metabolic syndrome, hypertension, Parkinson's disease, Alzheimer’s disease, cerebral stroke, cardiovascular diseases, kidney diseases, inflammatory diseases, and rhinopharyngitis. The molecular basis for the pleiotropic activities of piperine is based on its ability to regulate multiple signaling molecules such as cell cycle proteins, anti-apoptotic proteins, P-glycoprotein, cytochrome P450 3A4, multidrug resistance protein 1, breast cancer resistance protein, transient receptor potential vanilloid 1 proinflammatory cytokine, nuclear factor-κB, c-Fos, cAMP response element-binding protein, activation transcription factor-2, peroxisome proliferator-activated receptor-gamma, Human G-quadruplex DNA, Cyclooxygenase-2, Nitric oxide synthases-2, MicroRNA, and coronaviruses. Piperine also regulates multiple signaling pathways such as Akt/mTOR/MMP-9, 5′-AMP-activated protein kinase-activated NLR family pyrin domain containing-3 inflammasome, voltage-gated K+ current, PKCα/ERK1/2, NF-κB/AP-1/MMP-9, Wnt/β-catenin, JNK/P38 MAPK, and gut microbiota. Short conclusion Based on the current evidence, piperine can be the potential molecule for treatment of disease, and its significance of this molecule in the clinic is discussed. Graphical abstract

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Guar gum micro-vehicle mediated delivery strategy and synergistic activity of thymoquinone and piperine: An in vitro study on bacterial and hepatocellular carcinoma cells

Cited by 13 publications

References 43 publications

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

Therapeutic potential of thymoquinone in combination therapy against cancer and cancer stem cells

Molecular and pharmacological aspects of piperine as a potential molecule for disease prevention and management: evidence from clinical trials

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