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Article ; Online: Pharmacological Basis for the Antidiarrheal and Antispasmodic Effects of Cuminaldehyde in Experimental Animals:

Ansari, Mohd Nazam / Rehman, Najeeb Ur / Samad, Abdul / Ahmad, Wasim

Frontiers in bioscience (Landmark edition)

2024 Volume 29, Issue 1, Page(s) 43

Abstract: Background: Medicinal herbs are frequently used for the management of gastrointestinal disorders because they contain various compounds that can potentially amplify the intended therapeutic effects. Cuminaldehyde is a plant-based constituent found in ... ...

Abstract	Background: Medicinal herbs are frequently used for the management of gastrointestinal disorders because they contain various compounds that can potentially amplify the intended therapeutic effects. Cuminaldehyde is a plant-based constituent found in oils derived from botanicals such as cumin, eucalyptus, myrrh, and cassia and is responsible for its health benefits. Despite the utilization of cuminaldehyde for several medicinal properties, there is currently insufficient scientific evidence to support its effectiveness in treating diarrhea. Hence, the present investigation was carried out to evaluate the antidiarrheal and antispasmodic efficacy of cuminaldehyde, with detailed pharmacodynamics explored. Methods: An Results: Cuminaldehyde, at 10 and 20 mg/kg, exhibited 60 and 80% protection in mice from episodic diarrhea compared to the saline control group, whereas this inhibitory effect was significantly reversed in the pretreated mice with glibenclamide, similar to cromakalim, an ATP-dependent K+ channel opener. In the Conclusions: Present findings support the antidiarrheal and antispasmodic potential of cuminaldehyde, possibly by the predominant activation of ATP-dependent K+ channels followed by voltage-gated Ca++ inhibition. However, further in-depth assays are recommended to know the precise mechanism and to elucidate additional unexplored mechanism(s) if involved.
MeSH term(s)	Rats ; Mice ; Animals ; Antidiarrheals/adverse effects ; Parasympatholytics/adverse effects ; Cromakalim/adverse effects ; Glyburide/adverse effects ; Plant Extracts/pharmacology ; Jejunum ; Diarrhea/chemically induced ; Diarrhea/drug therapy ; Verapamil/adverse effects ; Adenosine Triphosphate ; Cymenes ; Benzaldehydes
Chemical Substances	Antidiarrheals ; Parasympatholytics ; cuminaldehyde (O0893NC35F) ; Cromakalim (0G4X367WA3) ; Glyburide (SX6K58TVWC) ; Plant Extracts ; Verapamil (CJ0O37KU29) ; Adenosine Triphosphate (8L70Q75FXE) ; Cymenes ; Benzaldehydes
Language	English
Publishing date	2024-02-10
Publishing country	Singapore
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2704569-9
ISSN	2768-6698 ; 2768-6698
ISSN (online)	2768-6698
ISSN	2768-6698
DOI	10.31083/j.fbl2901043
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Article ; Online: Calcium Channel Inhibitory Effect of Marjoram (

Rehman, Najeeb Ur / Ansari, Mohd Nazam / Ahmad, Wasim / Ali, Abuzer

Frontiers in bioscience (Landmark edition)

2024 Volume 29, Issue 2, Page(s) 47

Abstract: Background: The leaves of : Methods: Gas chromatography-mass spectrometry (GC-MS) was used to identify the phytochemicals, and Swiss albino mice were used for an : Results: The GC-MS analysis of : Conclusions: Thus, this study conducted an ... ...

Abstract	Background: The leaves of Methods: Gas chromatography-mass spectrometry (GC-MS) was used to identify the phytochemicals, and Swiss albino mice were used for an Results: The GC-MS analysis of Conclusions: Thus, this study conducted an analysis to determine the chemical constituents of the leaf extract of
MeSH term(s)	Rats ; Mice ; Animals ; Antidiarrheals/pharmacology ; Antidiarrheals/therapeutic use ; Antidiarrheals/chemistry ; Origanum ; Jejunum ; Plant Extracts/pharmacology ; Plant Extracts/therapeutic use ; Plant Extracts/chemistry ; Castor Oil/pharmacology ; Castor Oil/therapeutic use ; Diarrhea/drug therapy ; Verapamil/pharmacology ; Verapamil/therapeutic use ; Calcium Channels ; Spasm/drug therapy
Chemical Substances	Antidiarrheals ; Plant Extracts ; Castor Oil (8001-79-4) ; Verapamil (CJ0O37KU29) ; Calcium Channels
Language	English
Publishing date	2024-02-29
Publishing country	Singapore
Document type	Journal Article
ZDB-ID	2704569-9
ISSN	2768-6698 ; 2768-6698
ISSN (online)	2768-6698
ISSN	2768-6698
DOI	10.31083/j.fbl2902047
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Article ; Online: Investigating the Potential Impact of Air Pollution on Alzheimer's Disease and the Utility of Multidimensional Imaging for Early Detection.

Singh S, Ankul / Ansari, Mohd Nazam / M Elossaily, Gehan / Vellapandian, Chitra / Prajapati, Bhupendra

ACS omega

2024 Volume 9, Issue 8, Page(s) 8615–8631

Abstract: Pollution is ubiquitous, and much of it is anthropogenic in nature, which is a severe risk factor not only for respiratory infections or asthma sufferers but also for Alzheimer's disease, which has received a lot of attention recently. This Review aims ... ...

Abstract	Pollution is ubiquitous, and much of it is anthropogenic in nature, which is a severe risk factor not only for respiratory infections or asthma sufferers but also for Alzheimer's disease, which has received a lot of attention recently. This Review aims to investigate the primary environmental risk factors and their profound impact on Alzheimer's disease. It underscores the pivotal role of multidimensional imaging in early disease identification and prevention. Conducting a comprehensive review, we delved into a plethora of literature sources available through esteemed databases, including Science Direct, Google Scholar, Scopus, Cochrane, and PubMed. Our search strategy incorporated keywords such as "Alzheimer Disease", "Alzheimer's", "Dementia", "Oxidative Stress", and "Phytotherapy" in conjunction with "Criteria Pollutants", "Imaging", "Pathology", and "Particulate Matter". Alzheimer's disease is not only a result of complex biological factors but is exacerbated by the infiltration of airborne particles and gases that surreptitiously breach the nasal defenses to traverse the brain, akin to a Trojan horse. Various imaging modalities and noninvasive techniques have been harnessed to identify disease progression in its incipient stages. However, each imaging approach possesses inherent limitations, prompting exploration of a unified technique under a single umbrella. Multidimensional imaging stands as the linchpin for detecting and forestalling the relentless march of Alzheimer's disease. Given the intricate etiology of the condition, identifying a prospective candidate for Alzheimer's disease may take decades, rendering the development of a multimodal imaging technique an imperative. This research underscores the pressing need to recognize the chronic ramifications of invisible particulate matter and to advance our understanding of the insidious environmental factors that contribute to Alzheimer's disease.
Language	English
Publishing date	2024-02-15
Publishing country	United States
Document type	Journal Article ; Review
ISSN	2470-1343
ISSN (online)	2470-1343
DOI	10.1021/acsomega.3c06328
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Article ; Online: Novel furan chalcone modulates PHD-2 induction to impart antineoplastic effect in mammary gland carcinoma.

Rastogi, Shubham / Ansari, Mohd Nazam / Saeedan, Abdulaziz S / Singh, Sunil Kumar / Mukerjee, Alok / Kaithwas, Gaurav

Journal of biochemical and molecular toxicology

2024 Volume 38, Issue 4, Page(s) e23679

Abstract: Normoxic inactivation of prolyl hydroxylase-2 (PHD-2) in tumour microenvironment paves the way for cancer cells to thrive under the influence of HIF-1α and NF-κB. Henceforth, the present study is aimed to identify small molecule activators of PHD-2. A ... ...

Abstract	Normoxic inactivation of prolyl hydroxylase-2 (PHD-2) in tumour microenvironment paves the way for cancer cells to thrive under the influence of HIF-1α and NF-κB. Henceforth, the present study is aimed to identify small molecule activators of PHD-2. A virtual screening was conducted on a library consisting of 265,242 chemical compounds, with the objective of identifying molecules that exhibit structural similarities to the furan chalcone scaffold. Further, PHD-2 activation potential of screened compound was determined using in vitro 2-oxoglutarate assay. The cytotoxic activity and apoptotic potential of screened compound was determined using various staining techniques, including 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide, 4',6-diamidino-2-phenylindole (DAPI), 1,1',3,3'-tetraethylbenzimi-dazolylcarbocyanine iodide (JC-1), and acridine orange/ethidium bromide (AO/EB), against MCF-7 cells. 7,12-Dimethylbenz[a]anthracene (DMBA) model of mammary gland cancer was used to study the in vivo antineoplastic efficacy of screened compound. [(E)-1-(4-fluorophenyl)-3-(furan-2-yl) prop-2-en-1-one] (BBAP-7) was screened and validated as a PHD-2 activator by an in vitro 2-oxo-glutarate assay. The IC
MeSH term(s)	Humans ; Prolyl Hydroxylases ; Chalcones/pharmacology ; Antineoplastic Agents/pharmacology ; Acridine Orange ; Apoptosis ; Chalcone ; Carcinoma ; Tumor Microenvironment ; Benzimidazoles ; Carbocyanines
Chemical Substances	Prolyl Hydroxylases (EC 1.14.11.-) ; Chalcones ; 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolocarbocyanine (21527-78-6) ; Antineoplastic Agents ; Acridine Orange (F30N4O6XVV) ; Chalcone (5S5A2Q39HX) ; Benzimidazoles ; Carbocyanines
Language	English
Publishing date	2024-03-15
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.23679
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Article: An Overview of Nanoemulgels for Bioavailability Enhancement in Inflammatory Conditions via Topical Delivery.

Lal, Diwya Kumar / Kumar, Bhavna / Saeedan, Abdulaziz S / Ansari, Mohd Nazam

Pharmaceutics

2023 Volume 15, Issue 4

Abstract: The anti-inflammatory drugs that are generally available possess the disadvantage of hydrophobicity, which leads to poor permeability and erratic bioavailability. Nanoemulgels (NEGs) are novel drug delivery systems that aim to improve the solubility and ... ...

Abstract	The anti-inflammatory drugs that are generally available possess the disadvantage of hydrophobicity, which leads to poor permeability and erratic bioavailability. Nanoemulgels (NEGs) are novel drug delivery systems that aim to improve the solubility and permeability of drugs across the biological membrane. The nano-sized droplets in the nanoemulsion enhance the permeation of the formulation, along with surfactants and co-surfactants that act as permeation enhancers and can further improve permeability. The hydrogel component of NEG helps to increase the viscosity and spreadability of the formulation, making it ideal for topical application. Moreover, oils that have anti-inflammatory properties, such as eucalyptus oil, emu oil and clove oil, are used as oil phases in the preparation of the nanoemulsion, which shows a synergistic effect with active moiety and enhances its overall therapeutic profile. This leads to the creation of hydrophobic drugs that possess enhanced pharmacokinetic and pharmacodynamic properties, and simultaneously avoid systemic side effects in individuals with external inflammatory disorders. The nanoemulsion's effective spreadability, ease of application, non-invasive administration, and subsequent ability to achieve patient compliance make it more suitable for topical application in the combat of many inflammatory disorders, such as dermatitis, psoriasis, rheumatoid arthritis, osteoarthritis and so on. Although the large-scale practical application of NEG is limited due to problems regarding its scalability and thermodynamic instability, which arise from the use of high-energy approaches during the production of the nanoemulsion, these can be resolved by the advancement of an alternative nanoemulsification technique. Considering the potential advantages and long-term benefits of NEGs, the authors of this paper have compiled a review that elaborates the potential significance of utilizing nanoemulgels in a topical delivery system for anti-inflammatory drugs.
Language	English
Publishing date	2023-04-07
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics15041187
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Article ; Online: The Detailed Pharmacodynamics of the Gut Relaxant Effect and GC-MS Analysis of the

Rehman, Najeeb Ur / Ansari, Mohd Nazam / Ahmad, Wasim / Amir, Mohd

Molecules (Basel, Switzerland)

2022 Volume 27, Issue 24

Abstract: The study was performed to assess and rationalize the traditional utilization of the fruit part of Grewia tenax (G. tenax). The phytoconstituents present in the methanolic extract were analyzed using Gas-Chromatography-Mass Spectroscopy (GC-MS), while ... ...

Abstract	The study was performed to assess and rationalize the traditional utilization of the fruit part of Grewia tenax (G. tenax). The phytoconstituents present in the methanolic extract were analyzed using Gas-Chromatography-Mass Spectroscopy (GC-MS), while the anti-diarrheal activity was investigated in the Swiss albino mice against castor oil-provoked diarrhea in vivo. The antispasmodic effect and the possible pharmacodynamics of the observed antispasmodic effect were determined in an isolated rat ileum using the organ bath setup as an ex vivo model. GC-MS findings indicate that G. tenax is rich in alcohol (6,6-dideutero-nonen-1-ol-3) as the main constituent (20.98%), while 3-Deoxy-d-mannoic lactone (15.36%) was detected as the second major constituents whereas methyl furfural, pyranone, carboxylic acid, vitamin E, fatty acid ester, hydrocarbon, steroids, sesquiterpenes, phytosterols, and ketones were verified as added constituents in the methanolic extract. In mice, the orally administered G. tenax inhibited the diarrheal episodes significantly (p < 0.05) at 200 mg/kg (40% protection), and this protection was escalated to 80% with the next higher dose of 400 mg/kg. Loperamide (10 mg/kg), a positive control drug, imparted 100% protection, whereas no protection was shown by saline. In isolated rat ileum, G. tenax completely inhibited the carbamylcholine (CCh; 1 µM) and KCl (high K+; 80 mM)-evoked spasms in a concentrations-mediated manner (0.03 to 3 mg/mL) by expressing equal potencies (p > 0.05) against both types of evoked spasms, similar to papaverine, having dual inhibitory actions at phosphodiesterase enzyme (PDE) and Ca2+ channels (CCB). Similar to papaverine, the inhibitory effect of G. tenax on PDE was further confirmed indirectly when G. tenax (0.1 and 0.3 mg/mL) preincubated ileal tissues shifted the isoprenaline-relaxation curve towards the left. Whereas, pre-incubating the tissue with 0.3 and 1 mg/mL of G. tenax established the CCB-like effect by non-specific inhibition of CaCl2−mediated concentration-response curves towards the right with suppression of the maximum peaks, similar to verapamil, a standard CCB. Thus, the present investigation revealed the phytochemical constituents and explored the detailed pharmacodynamic basis for the curative use of G. tenax in diarrhea and hyperactive gut motility disorders.
MeSH term(s)	Rats ; Mice ; Animals ; Parasympatholytics/chemistry ; Antidiarrheals/chemistry ; Grewia ; Papaverine/pharmacology ; Jejunum ; Fruit ; Gas Chromatography-Mass Spectrometry ; Plant Extracts/pharmacology ; Plant Extracts/therapeutic use ; Diarrhea/drug therapy ; Phosphoric Diester Hydrolases/pharmacology ; Spasm
Chemical Substances	Parasympatholytics ; Antidiarrheals ; Papaverine (DAA13NKG2Q) ; Plant Extracts ; Phosphoric Diester Hydrolases (EC 3.1.4.-)
Language	English
Publishing date	2022-12-14
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules27248880
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Article ; Online: GC-MS Analysis and In Vivo and Ex Vivo Antidiarrheal and Antispasmodic Effects of the Methanolic Extract of

Rehman, Najeeb Ur / Ansari, Mohd Nazam / Ahmad, Wasim / Amir, Mohd

Molecules (Basel, Switzerland)

2022 Volume 27, Issue 7

Abstract: This present study evaluated and rationalized the medicinal use of the fruit part of Acacia nilotica methanolic extract. The phytochemicals were detected using gas chromatography−mass spectrometry (GC−MS) while the in vivo antidiarrheal test was done ... ...

Abstract	This present study evaluated and rationalized the medicinal use of the fruit part of Acacia nilotica methanolic extract. The phytochemicals were detected using gas chromatography−mass spectrometry (GC−MS) while the in vivo antidiarrheal test was done using Swiss albino mice. To determine the details of the mechanism(s) involved in the antispasmodic effect, isolated rat ileum was chosen using different ex vivo assays by maintaining a physiological environment. GC−MS results showed that A. nilotica contained pyrogallol as the major polyphenol present (64.04%) in addition to polysaccharides, polyphenol, amino acid, steroids, fatty acid esters, and triterpenoids. In the antidiarrheal experiment, A. nilotica inhibited diarrheal episodes in mice significantly (p < 0.05) by 40% protection of mice at 200 mg/kg, while 80% protection was observed at 400 mg/kg by the orally administered extract. The highest antidiarrheal effect was observed with loperamide (p < 0.01), used as a control drug. In the ex vivo experiments, A. nilotica inhibited completely in increasing concentrations (0.3 to 10 mg/mL) the carbachol (CCh; 1 µM) and high K+ (80 mM)-evoked spasms in ileum tissues at equal potencies (p > 0.05), similar to papaverine, a dual inhibitor of the phosphodiesterase enzyme (PDE) and Ca++ channels. The dual inhibitory-like effects of A. nilotica on PDE and Ca++ were further validated when A. nilotica extract (1 and 3 mg/mL)-pre-incubated ileum tissues potentiated and shifted isoprenaline relaxation curves towards lower doses (leftward), similar to papaverine, thus confirming the PDE inhibitory-like mechanism whereas its CCB-like effect of the extract was confirmed at 3 and 5 mg/mL by non-specific inhibition of CaCl2-mediated concentration response curves towards the right with suppression of the maximum peaks, similar to verapamil, used as standard CCB. Thus, this study characterized the chemical composition and provides mechanistic support for medicinal use of A. nilotica in diarrheal and hyperactive gut motility disorders.
MeSH term(s)	Acacia ; Animals ; Antidiarrheals/chemistry ; Diarrhea/drug therapy ; Gas Chromatography-Mass Spectrometry ; Gastrointestinal Agents/pharmacology ; Jejunum ; Methanol/pharmacology ; Mice ; Papaverine/pharmacology ; Parasympatholytics/chemistry ; Phosphoric Diester Hydrolases/pharmacology ; Plant Extracts/pharmacology ; Plant Extracts/therapeutic use ; Polyphenols/pharmacology ; Rats
Chemical Substances	Antidiarrheals ; Gastrointestinal Agents ; Parasympatholytics ; Plant Extracts ; Polyphenols ; Papaverine (DAA13NKG2Q) ; Phosphoric Diester Hydrolases (EC 3.1.4.-) ; Methanol (Y4S76JWI15)
Language	English
Publishing date	2022-03-24
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules27072107
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Article ; Online: In Silico and Ex Vivo Studies on the Spasmolytic Activities of Fenchone Using Isolated Guinea Pig Trachea.

Rehman, Najeeb Ur / Ansari, Mohd Nazam / Samad, Abdul / Ahmad, Wasim

Molecules (Basel, Switzerland)

2022 Volume 27, Issue 4

Abstract: Fenchone is a bicyclic monoterpene found in a variety of aromatic plants, ... ...

Abstract	Fenchone is a bicyclic monoterpene found in a variety of aromatic plants, including
MeSH term(s)	Animals ; Calcium Channel Blockers/chemistry ; Calcium Channel Blockers/pharmacology ; Camphanes/chemistry ; Camphanes/pharmacology ; Chemical Phenomena ; Dose-Response Relationship, Drug ; Guinea Pigs ; In Vitro Techniques ; Molecular Docking Simulation ; Molecular Dynamics Simulation ; Molecular Structure ; Norbornanes/chemistry ; Norbornanes/pharmacology ; Parasympatholytics/chemistry ; Parasympatholytics/pharmacology ; Phosphodiesterase Inhibitors/chemistry ; Phosphodiesterase Inhibitors/pharmacology ; Potassium Channels/agonists ; Potassium Channels/chemistry ; Structure-Activity Relationship ; Trachea/drug effects
Chemical Substances	Calcium Channel Blockers ; Camphanes ; Norbornanes ; Parasympatholytics ; Phosphodiesterase Inhibitors ; Potassium Channels ; fenchone (1195-79-5)
Language	English
Publishing date	2022-02-17
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules27041360
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Article ; Online: Crisaborole Loaded Nanoemulsion Based Chitosan Gel: Formulation, Physicochemical Characterization and Wound Healing Studies.

Ansari, Mohd Nazam / Soliman, Gamal A / Rehman, Najeeb Ur / Anwer, Md Khalid

Gels (Basel, Switzerland)

2022 Volume 8, Issue 5

Abstract: The development of an effective gel capable of treating eczema remains a challenge in medicine. Because of its greater retention in the affected area, good absorption of wound exudates, and induction of cell growth, nanogel is widely investigated as a ... ...

Abstract	The development of an effective gel capable of treating eczema remains a challenge in medicine. Because of its greater retention in the affected area, good absorption of wound exudates, and induction of cell growth, nanogel is widely investigated as a topical preparation. Chitosan gel based on nanoemulsions has received much attention for its use in wound healing. In this study, four formulae (CRB-NE1-CRB-NE4) of crisaborole-loaded nanoemulsions (CRB-NEs) were developed using lauroglycol 90 as an oil, Tween-80 as a surfactant, and transcutol-HP (THP) as a co-surfactant. The prepared NEs (CRB-NE1-CRB-NE4) were evaluated for their physicochemical properties. Based on vesicle size (64.5 ± 5.3 nm), polydispersity index (PDI) (0.202 ± 0.06), zeta potential (ZP, -36.3 ± 4.16 mV), refractive index (RI, 1.332 ± 0.03), and percent transmittance (% T, 99.8 ± 0.12) was optimized and further incorporated into chitosan (2%,
Language	English
Publishing date	2022-05-19
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2813982-3
ISSN	2310-2861 ; 2310-2861
ISSN (online)	2310-2861
ISSN	2310-2861
DOI	10.3390/gels8050318
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Article: Dual Inhibition of Phosphodiesterase and Ca

Rehman, Najeeb Ur / Ansari, Mohd Nazam / Ahmad, Wasim / Ahamad, Syed Rizwan

Plants (Basel, Switzerland)

2022 Volume 11, Issue 9

Abstract: The present study attempted to evaluate and rationalize the medicinal use of the methanolic extract of the fruits ... ...

Abstract	The present study attempted to evaluate and rationalize the medicinal use of the methanolic extract of the fruits of
Language	English
Publishing date	2022-04-27
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2704341-1
ISSN	2223-7747
ISSN	2223-7747
DOI	10.3390/plants11091183
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