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Article ; Online: 3,5,7-trihydroxyflavone restricts proliferation of androgen-independent human prostate adenocarcinoma cells by inducing ROS-mediated apoptosis and reduces tumour growth.

Raza, Waseem / Meena, Abha / Luqman, Suaib

Journal of biochemical and molecular toxicology

2023 Volume 37, Issue 11, Page(s) e23474

Abstract: Flavonoids are among the largest groups of secondary metabolites. Studies suggest that dietary intake of flavonoids reduces the risk of cancer. 3,5,7-trihydroxyflavone (THF) belongs to the flavone class of flavonoids and potentially inhibits the growth ... ...

Abstract	Flavonoids are among the largest groups of secondary metabolites. Studies suggest that dietary intake of flavonoids reduces the risk of cancer. 3,5,7-trihydroxyflavone (THF) belongs to the flavone class of flavonoids and potentially inhibits the growth of many cancers; however, it is unexplored in prostate cancer. This study reports the antiproliferative potential of THF in prostate cancer cell line via reactive oxygen species (ROS)-mediated cascades and examines the tumour reduction potential in swiss albino mice. The potency of THF was evaluated by employing cytotoxicity assays and wound healing assays. Cell cycle, ROS, mitochondrial membrane potential (MMP), and Annexin-V-FITC assay were performed using a flow cytometer. In vivo, anticancer potential was achieved using the mice Ehrlich Ascites Carcinoma (EAC) model. THF inhibits cell growth with IC
MeSH term(s)	Male ; Animals ; Mice ; Humans ; Reactive Oxygen Species/metabolism ; Androgens ; Fluorescein-5-isothiocyanate ; Prostate/metabolism ; Apoptosis ; Cell Proliferation ; Flavonoids/pharmacology ; Prostatic Neoplasms/drug therapy ; Adenocarcinoma/drug therapy ; Annexins ; Cell Line, Tumor
Chemical Substances	Reactive Oxygen Species ; Androgens ; Fluorescein-5-isothiocyanate (I223NX31W9) ; Flavonoids ; Annexins
Language	English
Publishing date	2023-07-21
Publishing country	United States
Document type	Journal Article
ZDB-ID	1410020-4
ISSN	1099-0461 ; 1095-6670
ISSN (online)	1099-0461
ISSN	1095-6670
DOI	10.1002/jbt.23474
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Article ; Online: Monoterpenoids: An upcoming class of therapeutic agents for modulating cancer metastasis.

Mathur, Anurag / Meena, Abha / Luqman, Suaib

Phytotherapy research : PTR

2023 Volume 38, Issue 2, Page(s) 939–969

Abstract: Monoterpenoids, a sub-class of terpenoids, are secondary metabolites frequently extracted from the essential oils of aromatic plants. Their antitumor properties including antiproliferative, apoptotic, antiangiogenic, and antimetastatic effects along with ...

Abstract	Monoterpenoids, a sub-class of terpenoids, are secondary metabolites frequently extracted from the essential oils of aromatic plants. Their antitumor properties including antiproliferative, apoptotic, antiangiogenic, and antimetastatic effects along with other biological activities have been the subject of extensive study due to their diverse characteristics. In recent years, numerous investigations have been conducted to understand its potential anticancer impacts, specifically focusing on antiproliferative and apoptotic mechanisms. Metastasis, a malignancy hallmark, can exert either protective or destructive influences on tumor cells. Despite this, the potential antimetastatic and antiangiogenic attributes of monoterpenoids need further exploration. This review focuses on specific monoterpenoids, examining their effects on metastasis and relevant signaling pathways. The monoterpenoids exhibit a high level of complexity as natural products that regulate metastatic proteins through various signaling pathways, including phosphoinositide 3-kinase/protein kinase B/mammalian target of rapamycin, mitogen-activated protein kinase/extracellular signal-regulated kinase/jun N-terminal kinase, nuclear factor kappa B, vascular endothelial growth factor, and epithelial mesenchymal transition process. Additionally, this review delves into the biosynthesis and classification of monoterpenoids, their potential antitumor impacts on cell lines, the plant sources of monoterpenoids, and the current status of limited clinical trials investigating their efficacy against cancer. Moreover, monoterpenoids depict promising potential in preventing cancer metastasis, however, inadequate clinical trials limit their drug usage. State-of-the-art techniques and technologies are being employed to overcome the challenges of utilizing monoterpenoids as an anticancer agent.
MeSH term(s)	Humans ; Vascular Endothelial Growth Factor A/metabolism ; Monoterpenes/pharmacology ; Monoterpenes/therapeutic use ; Phosphatidylinositol 3-Kinases/metabolism ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Neoplasms/drug therapy
Chemical Substances	Vascular Endothelial Growth Factor A ; Monoterpenes ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; Antineoplastic Agents
Language	English
Publishing date	2023-12-15
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	639136-9
ISSN	1099-1573 ; 0951-418X
ISSN (online)	1099-1573
ISSN	0951-418X
DOI	10.1002/ptr.8081
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Zs.B 3092: Show issues

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Article ; Online: Cinchonine: A Versatile Pharmacological Agent Derived from Natural Cinchona Alkaloids.

Parveen, Shahnaz / Maurya, Nidhi / Meena, Abha / Luqman, Suaib

Current topics in medicinal chemistry

2023

Abstract: Background: Cinchonine is one of the Cinchona alkaloids that is commercially extracted from the Peruvian bark of Cinchona officinalis L. (Family: Rubiaceae). It is also obtained in much lower quantities from other species of Cinchona, such as Cinchona ... ...

Abstract	Background: Cinchonine is one of the Cinchona alkaloids that is commercially extracted from the Peruvian bark of Cinchona officinalis L. (Family: Rubiaceae). It is also obtained in much lower quantities from other species of Cinchona, such as Cinchona calisaya, Cinchona succirubra, and Cinchona pubescens, and in some other plants, such as Remijia peruviana. Cinchonine has been historically used as an anti-malarial agent. It also has a wide range of other biological properties, including anti-cancer, anti-obesity, anti-inflammatory, anti-parasitic, antimicrobial, anti-platelet aggregation, and anti-osteoclast differentiation. Aim and objective: This review discusses the pharmacological activity of cinchonine under different experimental conditions, including in silico, in vitro, and in vivo. It also covers the compound's physicochemical properties, toxicological aspects, and pharmacokinetics. Methodology: A comprehensive literature search was conducted on multiple online databases, such as PubMed, Scopus, and Google Scholar. The aim was to retrieve a wide range of review/research papers and bibliographic sources. The process involved applying exclusion and inclusion criteria to ensure the selection of relevant and high-quality papers. Results: Cinchonine has numerous pharmacological properties, making it a promising compound for various therapeutic applications. It induces anticancer activity by activating caspase-3 and PARP-1, and triggers the endoplasmic reticulum stress response. It up-regulates GRP78 and promotes the phosphorylation of PERK and ETIF-2α. Cinchonine also inhibits osteoclastogenesis, inhibiting TAK1 activation and suppressing NFATc1 expression by regulating AP-1 and NF-κB. Its potential anti-inflammatory effects reduce the impact of high-fat diets, making it suitable for targeting obesity-related diseases. However, research on cinchonine is limited, and further studies are needed to fully understand its therapeutic potential. Further investigation is needed to ensure its safety and efficacy in clinical applications. Conclusion: Overall, this review article explains the pharmacological activity of cinchonine, its synthesis, and physicochemical properties, toxicological aspects, and pharmacokinetics.
Language	English
Publishing date	2023-11-27
Publishing country	United Arab Emirates
Document type	Journal Article
ZDB-ID	2064823-6
ISSN	1873-4294 ; 1568-0266
ISSN (online)	1873-4294
ISSN	1568-0266
DOI	10.2174/0115680266270796231109171808
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Zs.A 5572: Show issues

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Article ; Online: New frontiers in the design and discovery of therapeutics that target calcium ion signaling: a novel approach in the fight against cancer.

Singh, Jyoti / Meena, Abha / Luqman, Suaib

Expert opinion on drug discovery

2023 Volume 18, Issue 12, Page(s) 1379–1392

Abstract: Introduction: The Ca: Areas covered: This review highlights the existing research on the role of Ca: Expert opinion: Targeting specific ... ...

Abstract	Introduction: The Ca Areas covered: This review highlights the existing research on the role of Ca Expert opinion: Targeting specific Ca
MeSH term(s)	Humans ; Calcium Signaling ; Calcium/metabolism ; Neoplasms/drug therapy ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use
Chemical Substances	Calcium (SY7Q814VUP) ; Antineoplastic Agents
Language	English
Publishing date	2023-09-01
Publishing country	England
Document type	Journal Article ; Review ; Research Support, Non-U.S. Gov't
ZDB-ID	2259618-5
ISSN	1746-045X ; 1746-0441
ISSN (online)	1746-045X
ISSN	1746-0441
DOI	10.1080/17460441.2023.2251887
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Zs.A 6388: Show issues

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Article ; Online: Suppression of Molecular Targets and Antiproliferative Effect of Citronellal on Triple-Negative Breast Cancer Cells.

Fatima, Kaneez / Luqman, Suaib

Current molecular pharmacology

2021 Volume 14, Issue 6, Page(s) 1156–1166

Abstract: Background: Triple-Negative Breast Cancer (TNBC) requires targeted therapies to better manage and prevent metastatic mammary gland tumors. Due to the resistance problem associated with the approved drugs, researchers are now focusing on phytochemicals ... ...

Abstract	Background: Triple-Negative Breast Cancer (TNBC) requires targeted therapies to better manage and prevent metastatic mammary gland tumors. Due to the resistance problem associated with the approved drugs, researchers are now focusing on phytochemicals for the treatment of TNBC as they possess pleiotropic mode of action and fewer side effects. Objective: To investigate the antiproliferative effect of citronellal on triple-negative breast cancer cells. Methods: Anticancer potential of citronellal was explored by employing SRB, MTT, and NRU antiproliferative assay. Further, the effect of citronellal was observed on molecular targets (Tubulin, COX-2, and LOX-5) utilizing in vitro and in silico methods. Furthermore, the efficacy of citronellal was examined on Ehrlich Ascites Carcinoma cells. In addition, the safety profiling of it was observed at 300 and 1000 mg/kg of body weight in mice. Results: Citronellal suppresses the growth of MDA-MB-231 cells by more than 50% in NRU assay and ~41% and 32% in SRB and MTT assay, respectively. Further, citronellal's effect was observed on molecular targets wherein it suppressed LOX-5 activity (IC50 40.63±2.27 μM) and prevented polymerization of microtubule (IC50 63.62 μM). The result was more prominent against LOX-5 as supported by molecular docking interaction studies, but a non-significant effect was observed at the transcriptional level. The efficacy of citronellal was also determined in Ehrlich Ascites Carcinoma (EAC) model, wherein it inhibited the growth of tumor cells (45.97%) at 75 mg/kg of body weight. It was non-toxic up to 1000 mg/kg of body weight in mice and did not cause significant lysis of erythrocytes. Conclusion: These observations could provide experimental support for citronellal to be used as a chemopreventive agent for breast cancer.
MeSH term(s)	Acyclic Monoterpenes/pharmacology ; Aldehydes ; Animals ; Cell Line, Tumor ; Humans ; Mice ; Molecular Docking Simulation ; Triple Negative Breast Neoplasms/drug therapy ; Triple Negative Breast Neoplasms/pathology
Chemical Substances	Acyclic Monoterpenes ; Aldehydes ; citronellal (QB99VZZ7GZ)
Language	English
Publishing date	2021-04-09
Publishing country	United Arab Emirates
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1874-4702
ISSN (online)	1874-4702
DOI	10.2174/1874467214666210309120626
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Article: Citronellal suppress the activity of ornithine decarboxylase in hypopharyngeal carcinoma cells

Fatima, Kaneez / Luqman, Suaib

SAAB South African journal of botany. 2021 Dec., v. 143

2021

Abstract: Citronellal, an acyclic monoterpene with an aldehyde group, is present in many plants, including species of Eucalyptus, Corymbia, Cymbopogon, Coriandrum. It is also known as rhodinol and possesses strong insect repellant and antifungal properties. In ... ...

Abstract	Citronellal, an acyclic monoterpene with an aldehyde group, is present in many plants, including species of Eucalyptus, Corymbia, Cymbopogon, Coriandrum. It is also known as rhodinol and possesses strong insect repellant and antifungal properties. In this study, we investigated the antiproliferative action of citronellal on hypopharyngeal carcinoma (FaDu) and normal (HEK-293) cell lines. Citronellal suppresses the activity of ornithine decarboxylase (ODC: 77.12±10.73 µM) and inhibits the proliferation of FaDu cells with an IC₅₀ of 71.81±3.37 µM. The qRT-expression analysis depicts citronellal down-regulate the expression of ODC, and a robust binding interaction of citronellal with ODC was observed in molecular docking studies. Further, it also arrests the G2/M phase of FaDu cells, followed by an increase in the number of sub-diploid cells but was non-toxic to normal cell line. The toxicity prediction studies revealed citronellal follows the Lipinski rule of 5 and the Ghose rule. These observations provide experimental evidence for citronellal to be used as a new prototype for designing ODC inhibitors.
Keywords	Coriandrum ; Corymbia ; Cymbopogon ; Eucalyptus ; botany ; carcinoma ; cell lines ; citronellal ; insects ; ornithine decarboxylase ; prediction ; prototypes ; toxicity
Language	English
Dates of publication	2021-12
Size	p. 443-448.
Publishing place	Elsevier B.V.
Document type	Article
ZDB-ID	2126918-X
ISSN	0254-6299
ISSN	0254-6299
DOI	10.1016/j.sajb.2021.07.043
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Exploration of selected monoterpenes as potential TRPC channel family modulator in lung cancer, an

Singh, Akanksha / Mishra, Anamika / Meena, Abha / Mishra, Nidhi / Luqman, Suaib

Journal of biomolecular structure & dynamics

2023 , Page(s) 1–17

Abstract: Lung cancer is still the most frequent cause of cancer-related death, accounting for nearly two million cases yearly. As cancer is a multifactorial disease, developing novel molecular therapeutics that can simultaneously target multiple associated ... ...

Abstract	Lung cancer is still the most frequent cause of cancer-related death, accounting for nearly two million cases yearly. As cancer is a multifactorial disease, developing novel molecular therapeutics that can simultaneously target multiple associated cellular processes has become necessary. Ion channels are diverse regulators of cancer-related processes such as abnormal proliferation, invasion, migration, tumor progression, inhibition of apoptosis, and chemoresistance. Among the various families of ion channels, the transient receptor potential canonical channel family steps out in the context of lung cancer, as several members have been postulated as prognostic markers for lung cancer. Phytochemicals have been found to have health benefits in the treatment of a variety of diseases and disorders. Among phytochemicals, monoterpenes are effective in treating both the early and late stages of cancer. The molecular docking interaction analysis was conducted to evaluate the binding potential of selected monoterpenes with TRPC3, TRPC4, TRPC5, and TRPC6 involved in different phases of carcinogenesis. Amongst the selected monoterpenes, thymoquinone exhibited the highest binding energy of -6.7 kcal/mol against the TRPC4 channel, and all amino acid binding residues were similar to those of the known inhibitor for TRPC4. In addition, molecular-dynamic simulation results parameters, such as RMSD, RMSF, and Rg, indicated that thymoquinone did not impact the protein compactness and exhibited stability during the interaction. The average interaction energy between thymoquinone and TRPC4 protein was -26.85 kJ/mol.
Language	English
Publishing date	2023-08-01
Publishing country	England
Document type	Journal Article
ZDB-ID	49157-3
ISSN	1538-0254 ; 0739-1102
ISSN (online)	1538-0254
ISSN	0739-1102
DOI	10.1080/07391102.2023.2241900
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Article: Carvacrol Arrests the Proliferation of Hypopharyngeal Carcinoma Cells by Suppressing Ornithine Decarboxylase and Hyaluronidase Activities.

Fatima, Kaneez / Luqman, Suaib / Meena, Abha

Frontiers in nutrition

2022 Volume 9, Page(s) 857256

Abstract: Carvacrol, a monoterpene known for its pharmacological activities, is present in the essential oil ... ...

Abstract	Carvacrol, a monoterpene known for its pharmacological activities, is present in the essential oil of
Language	English
Publishing date	2022-04-08
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2776676-7
ISSN	2296-861X
ISSN	2296-861X
DOI	10.3389/fnut.2022.857256
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Article ; Online: Promising Essential Oils/Plant Extracts in the Prevention and Treatment of Dandruff Pathogenesis.

Kumari, K M Uma / Yadav, Narayan Prasad / Luqman, Suaib

Current topics in medicinal chemistry

2022 Volume 22, Issue 13, Page(s) 1104–1133

Abstract: Background: Dandruff is a scalp disorder affecting the male populace predominantly. Topical agents and synthetic drugs used for dandruff treatment have specific side effects including burning at the application site, depression, dizziness, headache, ... ...

Abstract	Background: Dandruff is a scalp disorder affecting the male populace predominantly. Topical agents and synthetic drugs used for dandruff treatment have specific side effects including burning at the application site, depression, dizziness, headache, itching or skin rash, nausea, stomach pain, vision change, vomiting, discoloration of hair, dryness or oiliness of the scalp and increased loss of hair. Thus, essential oils and extracts from plants could be valuable in the treatment and prevention of dandruff. Aims & objectives: This review aims to highlight current findings in dandruff occurrence, its etiology, promising plant essential oils/extracts, and novel treatment strategies. The main emphasis has been given on the anti-dandruff effect of essential oils and plant extracts to disrupt microbial growth. The proposed mechanism(s) of action, novel approaches used to perk up its biopharmaceutical properties, and topical application have been discussed. Results: The literature survey was done, and bibliographic sources and research papers were retrieved from different search engines and databases, including SciFinder, PubMed, NCBI, Scopus, and Google Scholar. The selection of papers was accomplished based on exclusion and inclusion criteria. The scalp of diverse populations revealed an association of dandruff with microbial symbiosis, including Staphylococcus, Propionibacterium, Malassezia, and Candida as the pathogens responsible for the cause of dandruff. Topical antifungals are considered the first line of treatment for dandruff including azoles, with clotrimazole (1%), ketoconazole (2%), and miconazole (2%). Other commonly used therapies integrate benzoyl peroxide, coal tar, glycerin, zinc pyrithione, lithium succinate/gluconate, salicylic acid, selenium disulfide/sulfide, sodium sulfacetamide, etc. However, these medicaments and chemicals are known to cause specific side effects. Alternative therapies, including tea tree oil, thyme, Aloe vera, Mentha have been reported to demonstrate anti-dandruff activity by disrupting the microbial growth associated with dandruff formation. Conclusion: Overall, this review explains the occurrence of dandruff, its pathogenesis, and the potential applicability of promising plant essential oils/extracts and their novel treatment strategies. Further studies based on pre-clinical and clinical research are essential before making any conclusion about its efficacy in humans.
MeSH term(s)	Antifungal Agents/pharmacology ; Dandruff/drug therapy ; Dandruff/microbiology ; Humans ; Malassezia ; Oils, Volatile/pharmacology ; Plant Extracts/pharmacology ; Plant Extracts/therapeutic use
Chemical Substances	Antifungal Agents ; Oils, Volatile ; Plant Extracts
Language	English
Publishing date	2022-06-01
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	2064823-6
ISSN	1873-4294 ; 1568-0266
ISSN (online)	1873-4294
ISSN	1568-0266
DOI	10.2174/1568026622666220531120226
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Article ; Online: Carvacrol as a Prospective Regulator of Cancer Targets/Signalling Pathways.

Singh, Jyoti / Luqman, Suaib / Meena, Abha

Current molecular pharmacology

2022 Volume 16, Issue 5, Page(s) 542–558

Abstract: Background: Carvacrol is a naturally occurring phenolic isopropyl monoterpene isolated from oregano, thyme, pepperwort, ajwain, marjoram, and wild bergamot. It possesses pharmacological activities, including anticancer, anti-genotoxic, and anti- ... ...

Abstract	Background: Carvacrol is a naturally occurring phenolic isopropyl monoterpene isolated from oregano, thyme, pepperwort, ajwain, marjoram, and wild bergamot. It possesses pharmacological activities, including anticancer, anti-genotoxic, and anti-inflammation associated with antioxidant properties. The antioxidant property of carvacrol is found to be accountable for its anticancer property. Thus, the present review summarizes and discusses the anticancer potential of carvacrol, revealing its target, signalling pathways, efficacy, pharmacokinetics, and toxicity. Objective: Carvacrol showed promising activity to be considered in more detail for cancer treatment. This review aims to summarize the evidence concerning the understanding of anticancer potential of carvacrol. However, the mode of action of carvacrol is not yet fully explored and hence requires detailed exploratory studies. This review consists of carvacol's in vitro, in vivo, preclinical and clinical studies. Methods: A literature search was done by searching various online databases like Pubmed, Scopus, and Google Scholar with the specific keyword "Carvacrol," along with other keywords, such as "antioxidant properties," "oncology research," "genotoxicity," and "anti-inflammatory property". Results: Carvacrol possesses weak mutagenic and genotoxic potential at non-toxic doses. Carvacrol alone shows the potential to target cancerous cells and significantly deter the growth of cancer cells; this is a targeted method. It offers anti-inflammatory effects by decreasing oxidative stress, primarily targeting ER and mitochondria. Carvacrol depicts targeted explicitly ROSdependent and mitochondrial-mediated apoptosis in different cancer cells. Moreover, carvacrol significantly regulates the cell cycle and prevents tumor progression. Few reports also suggest its significant role in inhibiting cell migration, invasion, and angiogenesis in tumor cells. Hence, carvacrol affects cell survival and cell-killing activity by targeting key biomarkers and major signalling pathways, including PI3K/AKT/mTOR, MAPK, STAT3, and Notch. Conclusion: Until now, its anticancer mechanism is not yet fully explored. A limited number of research studies have been conducted on carvacrol. It possesses both cancer prevention and cancer therapeutic properties. This molecule needs more validatory research so that it can be analyzed precisely.
MeSH term(s)	Humans ; Antioxidants/pharmacology ; Antioxidants/therapeutic use ; Phosphatidylinositol 3-Kinases ; Prospective Studies ; Neoplasms/drug therapy ; Anti-Inflammatory Agents/pharmacology
Chemical Substances	carvacrol (9B1J4V995Q) ; Antioxidants ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; Anti-Inflammatory Agents
Language	English
Publishing date	2022-07-06
Publishing country	United Arab Emirates
Document type	Review ; Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1874-4702
ISSN (online)	1874-4702
DOI	10.2174/1874467215666220705142954
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