Publications

Abstract

Quercetin, a major representative of the favonol subclass found abundantly in almost all edible vegetables and fruits, showed re-markable therapeutic properties and was benefcial in numerous degenerative diseases by preventing lipid peroxidation. Quercetin is benefcial in diferent diseases, such as atherosclerosis and chronic infammation. Tis study aims to fnd out the anticancer activities of quercetin and to determine diferent mechanisms and pathways which are responsible for the anticancer efect. It also revealed the biopharmaceutical, toxicological characteristics, and clinical utilization of quercetin to evaluate its suitability for further investigations as a reliable anticancer drug. All of the relevant data concerning this compound with cancer was collected using diferent scientifc search engines, including PubMed, Springer Link, Wiley Online, Web of Science, SciFinder, ScienceDirect, and Google Scholar. This review demonstrated that quercetin showed strong anticancer properties, including apoptosis, inhibition of cell proliferation,autophagy, cell cycle arrest, inhibition of angiogenesis, and inhibition of invasion and migration against various types of cancer. Findings also revealed that quercetin could signifcantly moderate and regulate diferent pathways, including PI3K/AKT-mTORC1 pathway, JAK/STAT signaling system, MAPK signaling pathway, MMP signaling pathway, NF-κB pathway, and p-Camk2/p-DRP1 pathway. However, this study found that quercetin showed poor oral bioavailability due to reduced absorption; this limitation is overcome by applying nanotechnology (nanoformulation of quercetin). Moreover, diferent investigations revealed that quercetin expressed no toxic efect in the investigated subjects. Based on the view of these fndings, it is demonstrated that quercetin might be considered a reliable chemotherapeutic drug candidate in the treatment of diferent cancers. However, more clinical studies are suggested to establish the proper therapeutic efcacy, safety, and human dose

Abstract

Dihydrocoumarin (DCN) is a natural compound widely used in the flavor industry and has antioxidant and anti-inflammatory properties. However, its potential antiemetic effects on gastrointestinal disturbances remain untested. This study emphasizes assessing the antiemetic properties of the natural aromatic compound DCN using copper sulfate (CuSO4.5H2O)-induced emetic model on chicks, and an in silico approach was also adopted to estimate the possible underlying mechanisms. Two doses (25 and 50 mg/kg b.w.) of DCN and several referral drugs considered positive controls (PCs), including domperidone (6 mg/kg), hyoscine (21 mg/kg), aprepitant (16 mg/kg), diphenhydramine (10 mg/kg), and ondansetron (5 mg/kg), were orally administered to chicks. The vehicle was provided as the control group. Co-treatments of DCN with referral drugs were also provided to chicks to evaluate the modulatory action of the test compound. According to the results, DCN delayed the emetic onset and decreased the frequency of retches in a dose-dependent manner compared to the vehicle group. DCN (50 mg/kg) represented a notable delayed latency period (61.17 ± 4.12 s) and a diminished number of retchings (17.67 ± 1.82 times) compared to the control group. Further, in the co-treatments, DCN increased the latency period and reduced the number of retches, except for domperidone. In the in silico investigation, DCN showed notable binding affinity toward the D2 (−7 kcal/mol), H1 (−7.5 kcal/mol), and M5 (−7 kcal/mol) receptors in the same binding site as the referral ligand. Our research indicates that DCN has mild antiemetic properties by interacting with the D2, H1, and M5 receptors. Therefore, several pre-clinical and clinical studies are necessary to assess the effectiveness and safety profile of this food ingredient. 

Abstract

Background Lonicerin (LON) has been identified to have different biological properties, such as anticancer, anti‐inflammatory, immunomodulatory, antibacterial, antimicrobial, and neuroprotective. This study aims to assess the sedative effect of LON in Swiss albino mice, which is yet to be discovered. Materials and Methods Mice were treated with two different doses of LON (5 and 10 mg/kg) and 2 mg/kg of diazepam (DZP), which is the referral GABAergic medication, and the latency time and sleeping duration of animals were observed. A computational study was also conducted to evaluate the docking scores and display the binding sites of LON and receptor (GABAA α1 and β2 subunits). The study also investigated the pharmacokinetics and drug‐likeness properties of LON along with toxicological analysis by using SwissADME and Protox‐3 software, respectively. Results Findings revealed that the higher concentration of LON reduced the latency (9.86 ± 1.44 min) and increased the sleep duration (191.29 ± 7.43 min) compared to the lower concentration. Besides, the combination group of LON and DZP showed the lowest latency (6.17 ± 0.82 min) and highest sleeping time (219.00 ± 6.39 min). In the in silico study, LON exhibited a strong docking score (−8.1 kcal/mol) with the macromolecules, which is closer to the binding affinity of DZP (–8.3 kcal/mol), indicating that LON could show strong sedative activity by binding with the GABAA receptor. Computational toxicity analysis revealed that LON is non‐hepatotoxic, non‐neurotoxic, noncarcinogenic, noncytotoxic, non‐ecotoxic, and non‐mutagenic. Conclusion Therefore, LON may be effective for the treatment of insomnia in the near future. 

Abstract

Introduction: Decursin is a pyranocoumarin natural phytochemical found in the Angelica gigas Nakai herb, which shows various therapeutic properties and beneficial effects against various diseases. Objective: The aim of this study was to find the anticancer potential of decursin and its molecular mechanisms involved with different anticancer effects. Methodology: All of the relevant data concerning this compound and cancer were collected using different scientific search engines, including PubMed, Scopus, Springer Link, Wiley Online, Web of Science, Scifinder, ScienceDirect, and Google Scholar. Results: This study found that decursin shows anticancer properties through various mechanisms, such as apoptosis, cell cycle arrest, inhibition of cell proliferation, autophagy, inhibition of angiogenesis, cytotoxicity, and the inhibition of invasion and migration against a number of cancers, including breast, bladder, lung, colon, skin, ovarian, prostate, pancreatic, and bone cancers. This study also discovered that decursin has the ability to affect several signaling pathways in the molecular anticancer mechanisms, such as the PI3K/AKT/mTOR, JAK/STAT, and MAPK signaling pathways. Findings also revealed that decursin expresses poor oral bioavailability. Conclusions: Based on the data analysis from this literature-based study, decursin has properties to be considered as a potential candidate in the treatment of cancer. However, more clinical research is suggested to establish proper efficacy, safety, and human dosage. 

Abstract

Background Numerous studies suggest that morellic acid (MOR), highly available in Garcinia plants, has different physiological activities, including anti‐cancer, anti‐oxidant, and anti‐microbial activity. Aim In this investigation, we aimed to demonstrate the anxiolytic activity, along with the mechanism behind this activity of MOR, using in vivo and in silico studies. Methods For this, we used different doses of MOR (5 and 10 mg/kg) and administered this drug intraperitoneally to Swiss albino mice (male and female). Diazepam (DZP), a positive allosteric modulator of the GABAA receptor, was used as a positive control at a dose of 2 mg/kg (i.p), and vehicle was used as a control group. In this test, various test protocols are used to assess the behavioral patterns of mice, including swing, hole cross, light–dark testing, and open field testing. Results This investigation revealed that MOR remarkably reduced the locomotor activity of mice in a dose‐dependent manner and produced calming behaviors like DZP. However, the findings showed that the combination of MOR and DZP synergistically reduced the locomotion of mice compared to the single therapy. On the other hand, from the computational study, the result demonstrated that MOR exhibited the highest binding scores (−9.2 kcal/mol) towards the GABAA receptor α3 subunit and −7.6 kcal/mol towards the GABAA α2 receptor. Whereas, DZP showed −6.6 and −7.3 kcal/mol docking affinity and FLU exerted −6.2 and −6.3 kcal/mol docking scores towards the GABAA receptor α2 and α3 subunits, respectively. The ligand interacted with the receptor by forming different hydrogen and hydrophobic bonds. Conclusion However, it is recommended that more precise and comprehensive preclinical investigations be required to demonstrate the exact mechanism behind the anxiolytic effects and conduct clinical trials to determine efficacy and safety. 

Abstract

Sesamol (SES) and linalool (LIN) are aromatic compounds that have neuroprotective effects. The main purpose of this study is to evaluate the anxiolytic activity of LIN and SES co‐treatment on Swiss albino mice and analyze its possible mechanism through in silico study. In this sense, the mice were given the gamma‐aminobutyric acid type A receptors (GABAA) agonist diazepam (DZP; 3 mg/kg, p.o.) as a positive control. A vehicle (10 mL/kg) was served as control. The tested chemicals, single‐dose LIN (50 mg/kg) and SES (50 mg/kg), as well as a combination (LIN + SES) and (DZP + LIN + SES), were administered orally in order to conduct several behavioral tests, including open‐field, swings box, hole‐crossing, and dark‐resident time tests. Further, molecular docking studies of LIN, SES, and DZP were carried out through different software. The results showed that LIN and SES individually have significant anxiolytic‐like activity in mice. Further, when LIN was combined with SES and with (SES + DZP), it exhibited a relatively lower locomotor activity in mice compared to individual treatment groups, indicating a synergistic action. In addition, the molecular docking analysis revealed that LIN and SES have a moderate binding affinity (−5.0 and −5.1 kcal/mol) toward the GABAA receptor α3 subunit. In conclusion, our findings suggest that LIN and SES exerted synergistic anxiolytic activity on Swiss albino mice, possibly through the GABAergic interaction pathways. 

Abstract

Mefloquine (MFQ) is an effective medication for the prevention and treatment of malaria. However, it has anticancer effects found in the literature. The main focus of this study is to review the anticancer activity of MFQ and also find the macromolecules or receptors that are mainly responsible for anticancer activity. For this reason, data was gathered (as of June 30, 2024) by utilizing a variety of reliable and well-known search engines. The molecular docking of MFQ with the selected macromolecules was performed. Our study findings showed that MFQ strongly showed anticancer activity by inhibiting proliferation, tumor growth, mitochondrial respiration, PI3K, MMP, IKK activation, Bcl-2, MCl-1, XIAP, and induced cell death, apoptosis, ROS, and PARP. In addition, an in silico study demonstrated that MFQ showed the highest binding affinity (-8.7 kcal/mol) against PI3K, whereas co-crystal ligand exhibited-8.6 kcal/mol binding affinity. The study also predicted that MFQ has better pharmacokinetics and toxicity parameters. However, we recommend additional evaluation and clinical research to further explore MFQ as a reliable PI3K inhibitor and an anticancer agent.