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Habenaria aitchisonii Reichb was analyzed in this research, including its chemical composition and its in vitro antioxidant, anti-inflammatory, acute oral toxicity, and antinociceptive activity. The chloroform and ethyl acetate fractions were found to be the most powerful based on in vitro antioxidant, anti-inflammatory, and analgesic assays. The acute oral toxicity of the crude methanolic extract was determined before in vivo studies. The acetic acid and formalin tests were used to measure the antinociceptive effect, and the potential mechanisms involved in antinociception were explored. The carrageenan-induced paw edema test was used to examine the immediate anti-inflammatory effect, and many phlogistic agents were used to determine the specific mechanism. Furthermore, for ex vivo activities, the mice were sacrificed, the forebrain was isolated, and the antioxidant levels of glutathione (GSH), superoxide dismutase (SOD), thiobarbituric acid reactive substances (TBARS) and catalase (CAT) were estimated using a UV spectrophotometer. No toxicity was seen at oral dosages up to 3,000 mg/kg. The antinociceptive impact was much higher than the standard drug. Both the inflammatory and neurogenic phases of the formalin experiment revealed an analgesic effect in the chloroform and ethyl acetate fractions. In carrageenan anti-inflammatory assays, the chloroform fraction (Ha.Chf) was the most potent fraction. We further studied the GC-MS of crude plant extract and found a total of 18 compounds. In the anti-inflammatory mechanism, it was observed that the Ha.Chf inhibits the COX-2 as well as 5-LOX pathways. The results exhibited that this species is a good source of phytocomponents like germacrone, which can be employed as a sustainable and natural therapeutic agent, supporting its traditional use in folk medicine for inflammatory conditions and pain.

The strong ethnopharmacological utilization of Isodon rugosus Wall. Ex. Benth is evident in the treatment of several types of pain and inflammation, including toothache, earache, abdominal pain, gastric pain, and generalized body pain and inflammation. Based on this background, the antinociceptive effects of the crude extract, various fractions, and essential oil have been reported previously. In this research work, we isolate and characterize pure bioactive compounds from I. rugosus and evaluate possible mechanisms using various in vivo and in vitro models. The pure compounds were analyzed for analgesic and anti-inflammatory activities through various assays. The column chromatography of the chloroform fraction of I. rugosus led to the identification of two pure compounds, i.e., 1 and 2. Compound 1 demonstrated notable inhibition (62% writhing inhibition, 72.77% COX-2 inhibition, and 76.97% 5-LOX inhibition) and anti-inflammatory potential (>50% paw edema inhibition at various intervals). The possible mechanism involved in antinociception was considered primarily, a concept that has already been elucidated through the application of naloxone (an antagonist of opioid receptors). The involvement of adrenergic receptors was investigated using a hot plate model (an adrenergic receptor antagonist). The strong ethnomedicinal analgesic background of I. rugosus, supported by previous reports and current observations, leads to the conclusion that I. rugosus is a potential source of antinociceptive and anti-inflammatory bioactive compounds. It may be concluded from the results that the isolated analgesic compounds of I. rugosus may be a possible alternative remedy for pain and inflammation management with admirable efficacy and safety profiles.

Brain tumor has become one of the fatal causes of death worldwide in recent years, affecting many individuals annually and resulting in loss of lives. Brain tumors are characterized by the abnormal or irregular growth of brain tissues that can spread to nearby tissues and eventually throughout the brain. Although several traditional machine learning and deep learning techniques have been developed for detecting and classifying brain tumors, they do not always provide an accurate and timely diagnosis. This study proposes a conditional generative adversarial network (CGAN) that leverages the fine-tuning of a convolutional neural network (CNN) to achieve more precise detection of brain tumors. The CGAN comprises two parts, a generator and a discriminator, whose outputs are used as inputs for fine-tuning the CNN model. The publicly available dataset of brain tumor MRI images on Kaggle was used to conduct experiments for Datasets 1 and 2. Statistical values such as precision, specificity, sensitivity, F1-score, and accuracy were used to evaluate the results. Compared to existing techniques, our proposed CGAN model achieved an accuracy value of 0.93 for Dataset 1 and 0.97 for Dataset 2.

Bixa orellana (B. Orellana) is a frequently utilized plant that has grown in significance in pharmaceutical applications. The leaves extract of B. orellana was used in the current study for preliminary phytochemical analysis in terms of both quantitative and qualitative, which indicates the presence of phenols, alkaloids, and flavonoids. Furthermore, the extract demonstrated antifungal activity at 30 mm zone of clearance against Candida albicans and antibacterial activity at 16 mm zone of clearance against Bacillus nakamuria by well diffusion method against different strains. The plant extract showed a MIC of 20 µg/mL and MBC of 157.11 µg/mL against E. coli by ELISA and broth dilution method, respectively. To evaluate the phytochemicals in the extract, further purification of the extract by TLC, column chromatography, and component analysis by GC–MS, which reported 18 components, and UV spectrum were performed. A number of therapeutic applications for the extract were observed, including antidiabetic activity (anti-glucosidase) of 98.34% inhibition at 100 µg/mL, anti-lipase of 100% inhibition at 100 µg/mL, and anti-amylase activity of 100% inhibition at 100 µg/mL, antioxidant activity (anti-DPPH activity) of 59.74% inhibition at 100 µg/mL, anthelmintic at 1 min by 1000 µg/mL, antifibrinolytic at 20 secs by 1000 µg/mL and cytotoxic activity against A549 lung cell lines, wherein, the cell viability was below 40 % at the highest dose (100 µg/mL), with an IC50 value of 39.9 µg/mL.

Objective: The Illicium verum is an evergreen Chinese plant, from which a culinary spice named star anise is obtained and is predominantly used in Asian countries. Besides its flavor, it possess high medicinal value. Illicium verum possesses good antimicrobial properties and in the past utilized to treat versatile ailments of microbial origin. Illicium verum is commonly known as star anise. Methods: This study is an attempt to resurrect the ancient forgotten traditional spice Illicium verum by analyzing its essential oils (EOs) for the phyto-biochemical properties using GC–MS, IR studies and various standard biochemical tests to record the presence of the chemical compounds based on its test reactions and also to measure its anti-microbial vulnerability testing towards the MRSA clinical isolates, by deploying the standard anti-microbial assay in the aseptic microbiological laboratory conditions. Results: The data procured from the standard antimicrobial assay of Illicium verum essential oil were compared with that of the standard antibiotic e-strips towards the same set of MRSA clinical isolates. The antimicrobial assay test results of Illicium verum essential oil against the clinical isolates of the MRSA showed promising results when compared to that of standard antibiotic e-strips. The results showed that all the MRSA clinical isolates were susceptible to the tested drug with inhibition zone diameter ranging from 18 mm to 28 mm (Mean 24.05 mm). The MBC and MIC results confirmed that the tested extract was potent against the highly virulent Methicillin-Resistant Staphylococcus aureus (MRSA) clinical isolates with MBC and MIC of 0.97 µg/mL and 0.70 µg/mL, which was lower compared to MBC and MIC values of the standard antibiotics. Conclusion: The results obtained from this study is a motivation to rediscover the ancient phytochemical compounds as an added asset to the standard available drugs in dealing with the upcoming hazardous diseases and pandemics. Thus, it relishes us to perform more of such studies to enhance the phyto-pharmacological industry.

The convenient and highly compliant route for the delivery of active pharmaceutical ingredients is the tablet. A versatile platform of tablets is available for the delivery of therapeutic agents to the gastrointestinal tract. This study aimed to prepare gastro retentive drug delivery floating tablets of silymarin to improve its oral bioavailability and solubility. Hydroxypropyl methylcellulose (HPMCK4M and HPMCK15), Carbopol 934p and sodium bicarbonate were used as a matrix, floating enhancer and gas generating agent, respectively. The prepared tablets were evaluated for physicochemical parameters such as hardness, weight variation, friability, floating properties (floating lag time, total floating time), drug content, stability study, in vitro drug release, in vivo floating behavior and in vivo pharmacokinetics. The drug–polymer interaction was studied by Differential Scanning Calorimetry (DSC) thermal analysis and Fourier transform infrared (FTIR). The floating lag time of the formulation was within the prescribed limit (12 h. The dissolution can be described by zero-order kinetics (r2 = 0.979), with anomalous diffusion as the release mechanism (n = 0.65). An in vivo pharmacokinetic study showed that Cmax and AUC were increased by up to two times in comparison with the conventional dosage form. An in vivo imaging study showed that the tablet was present in the stomach for 12 h. It can be concluded from this study that the combined matrix system containing hydrophobic and hydrophilic polymers min imized the burst release of the drug from the tablet and achieved a drug release by zero-order kinetics, which is practically difficult with only a hydrophilic matrix. An in vivo pharmacokinetic study elaborated that the bioavailability and solubility of silymarin were improved with an increased mean residence time.

Plants’ bioactives are well-known safe drugs for vital diseases. Flavones and Flavonoid-rich dietary supplements are known to exhibit neuroprotective potential. In this study, we isolated a flavone 2-(3,4-dimethoxyphenyl)-3,7-dihydroxy-4H-chromen-4-one from Notholirion thomsonianum and it was evaluated against various targets of the oxidative stress-related neurological disorders. The compound showed excellent acetyl and butyrylcholinesterase inhibitions in its profile, giving IC50 values of 1.37 and 0.95 μM, respectively. Similarly, in in-vitro MAO-B assay, our flavone exhibited an IC50 value of 0.14 μM in comparison to the standard safinamide (IC50 0.025 μM). In in-vitro anti-inflammatory assay, our isolated compound exhibited IC50 values of 7.09, 0.38 and 0.84 μM against COX-1, COX-2 and 5-LOX, respectively. The COX-2 selectivity (SI) of the compound was 18.70. The compound was found safe in animals and was very effective in carrageenan-induced inflammation. Due to the polar groups in the structure, a very excellent antioxidant profile was observed in both in-vitro and in-vivo models. The compound was docked into the target proteins of the respective activities and the binding energies confirmed the potency of our compound. Furthermore, absorption, distribution, metabolism, excretion, and toxicity (ADMET) results showed that the isolated flavone has a good GIT absorption ability and comes with no hepatic and cardiotoxicity. In addition, the skin sensitization test, in-vitro human cell line activation test (h-CLAT) and KeratinoSens have revealed that isolated flavone is not skin sensitive with a confidence score of 59.6% and 91.6%. Herein, we have isolated a natural flavone with an effective profile against Alzheimer’s, inflammation and oxidative stress. The exploration of this natural flavone will provide a baseline for future research in the field of drug development.

Based on the pharmacological importance of different species of fragaria, this research was carried out for the isolation of bioactive compounds from Fragaria × ananassa. Using the conventional gravity column chromatography followed by small analytical column purification, two major components were isolated from the plant materials. The structures of both compounds (1 and 2) were accurately confirmed with GC-MS analysis by comparison of the fragmentation pattern within the library of the instrument. Further, the NMR analysis was also used to supplement the structural evidence. Compound 1 was observed to be 4,22-cholestadien-3-one, while compound 2 was identified as stigmast-4-en-3-one. Both compounds were evaluated for anticholinesterase, COX/LOX inhibitions and antioxidant assays. Compound 1 exhibited the IC50 values of 20.29, 27.35, 10.70, 80.10 and 7.40 μg/mL against acetylcholinesterase, butyrylcholinesterase, COX-2, COX-1 and 5-LOX, respectively. Similarly, the IC50 values of compound 2 against the same targets were 14.51, 10.65, 8.45, 109.40 and 8.71 μg/mL. Similarly, both compounds were less potent in ABTS and DPPH targets with IC50 values in the range of 185.83–369.86 μg/mL. Despite the low potencies of these compounds in antioxidant targets, they can be considered as supplementary targets in Alzheimer and inflammation. The molecular docking studies for the in vitro anti-Alzheimer and anti-inflammatory targets were also performed, which showed excellent binding interactions with the respective target proteins. In conclusion, the isolated phytosteroids from Fragaria × ananassa were evaluated scientifically for anti-Alzheimer and anti-inflammatory activities using in vitro and molecular docking approaches.

Cardiac and hepatotoxicities are major concerns in the development of new drugs. Better alternatives to other treatments are being sought to protect these vital organs from the toxicities of these pharmaceuticals. In this regard, a preclinical study is designed to investigate the histopathological effects of a new succinimide derivative (Comp-1) on myocardial and liver tissues, and the biochemical effects on selected cardiac biomarkers, hepatic enzymes, and lipid profiles. For this, an initially lethal/toxic dose was determined, followed by a grouping of selected albino rats into five groups (each group had n = 6). The control group received daily oral saline for 8 days. The 5-FU (5-Fluorouracil) group received oral saline daily for 8 days, added with the administration of a single dose of 5-FU (150 mg/kg I.P.) on day 5 of the study. The atenolol group received oral atenolol (20 mg/kg) for 8 days and 5-FU (150 mg/kg I.P.) on day 5 of the protocol. Similarly, two groups of rats treated with test compound (Comp-1) were administered with 5 mg/kg I.P. and 10 mg/kg I.P. for 8 days, followed by 5-FU (150 mg/kg I.P.) on day 5. Toxicity induced by 5-FU was manifested by increases in the serum creatinine kinase myocardial band (CK-MB), troponin I (cTnI) and lactate dehydrogenase (LDH), lipid profile, and selected liver enzymes, including ALP (alkaline phosphatase), ALT (alanine transaminase), AST (aspartate aminotransferase), BT (bilirubin total), and BD (direct bilirubin). These biomarkers were highly significantly decreased after the administration of the mentioned doses of the test compound (5 mg/kg and 10 mg/kg). Similarly, histological examination revealed cardiac and hepatic tissue toxicity by 5-FU. However, those toxic effects were also significantly recovered/improved after the administration of Comp-1 at the said doses. This derivative showed dose-dependent effects and was most effective at a dose of 10 mg/kg body weight. Binding energy data computed via docking simulations revealed that our compound interacts toward the human beta2-adrenergic G protein-coupled receptor (S = −7.89 kcal/mol) with a slight stronger affinity than the calcium channel T-type (S = −7.07 kcal/mol). In conclusion, the histological and biochemical results showed that the test compound (Comp-1) had prominent cardioprotective, hepatoprotective, and lipolytic effects against 5-FU-induced toxicity in the subjected animal model.

Background Type 2 diabetes mellitus (T2DM) is a multifactorial disorder that leads to alterations in gene regulation. Long non-coding RNAs (lncRNAs) have become a major research topic as they are involved in metabolic disorders.Methods This study included a total of 400 study subjects; 200 were subjects with T2DM and 200 were healthy subjects. Extracted RNA was used to synthesize cDNA by quantitative real time. Serum analysis was carried out to determine differences in biochemical parameters. Recorded data were used to evaluate associations with expression of lncRNAs NF-kappaB interacting lncRNA (NKILA), nuclear enriched abundant transcript 1 (NEAT1), metastasis-associated lung adenocarcinoma transcript 1 (MALAT1), and myocardial infarction-associated transcript (MIAT) in T2DM cases.Results Compared with healthy controls, patients with T2DM showed an overall increase in expression of lncRNAs NKILA, NEAT, MALAT1, and MIAT by 3.94-fold, 5.28-fold, 4.46-fold, and 6.35-fold, respectively. Among patients with T2DM, higher expression of lncRNA NKILA was associated with hypertension (p=0.001), smoking (p