Significant Activity Research Articles

Synthesis, Aromatase Inhibition, Cytotoxicity and Molecular Docking Studies of New Fluorinated and Non-fluorinated Thiourea Derivatives of Desloratadine.

Aromatase inhibitors are among the most effective treatment of the breast cancer. Aromatase catalyzes estrogen biosynthesis, which is a long-term cause of breast cancer. Current study describes the synthesis, purification of 26 new fluorinated and non-fluorinated thiourea derivatives of desloratadine (5), and their aromatase inhibition activity, cytotoxicity against cancer cell line (MDA-MB-231). Compounds 7v and 7l exhibited a significant anti-aromatase activity, while compounds 7a, 7g-h, 7m and 7u were also significant active against MDA-MB-231 cell line. Furthermore, the molecular docking studies revealed that active compounds form key interactions with the crucial amino acid of aromatase active site including TRP224, LEU477, CYS437, ALA438, MET374, ARG115, ILE305, and PHE221, which are responsible for the binding interaction of aromatase. All analogues were new, except 7b and 7k and also lacked cytotoxicity BJ human fibroblasts, with the exception of 5 and 7x. This selectivity makes this series particularly interesting for further studies.

Concrete Times

Our existence has become so entangled with concrete that it would be difficult to imagine life without it, though we probably should. Anthropologists recognize the part that concrete plays in mediating social relations and in shaping political subjectivities. Thinking about concrete anthropologically involves moving across multiple scales—from large infrastructure projects to modest housebuilding projects. This review asks what we might gain from a focus on this ubiquitous material. I propose that attending ethnographically to how concrete mediates social experiences across scales brings to the fore building as an activity of political, economic, social, and ecological significance. Concrete offers a lens through which to apprehend social formations and transformations as well as to examine how built forms mediate and leverage power, how space is used and claimed, and how futures are imagined and pasts remembered. I conclude with a critical reflection on the ecological implications of these concrete times.

Antifungal Activity of Some New Binuclear Complexes

Three complexes of copper(II) and iron(II) with mixed ligands acetylacetonebis(thio-semicarbazone)- ABTSH2 and benzaldazine- BA have been prepared and characterized using different physico-chemical techniques including the determination of metal contents, mole-cular weight, measurement of molar conductivity, magnetic moment, molar refraction, infrared and electronic spectra. Accordingly, octahedral complexes having general formulaes [Cu2(ABTSH2)2(BA)2Cl2]Cl2 and [M2(ABTSH2)2(BA)2(SO4)2] {M= Cu(II) or (Fe(II)} have been proposed. The resulted complexes screened for antifungal activity in vitro against the citrus pathogen Aspergillus niger and Fusarium sp. which caused root rot of sugar and the beans pathogen Alternaria sp. All the complexes exhibited significant antifungal activities against these pathogens. The antifungal activity of these complexes were comparable with the standard fungicides in ethanol. The complex [Cu2(ABTSH2)2(BA)2Cl2]Cl2 had the best antifungal activity against Alternaria sp.

Hybrid Analogues of Hydrazone and Phthalimide: Design, Synthesis, In vivo, In vitro, and In silico Evaluation as Analgesic Agents.

Based on the anti-inflammatory and analgesic activity of hydrazone and phthalimide, a new series of hybrid hydrazone and phthalimide pharmacophores was prepared and evaluated as analgesic agents. The designed ligands were synthesized by reaction of the appropriate aldehydes and 2- aminophthalimide. Analgesic, cyclooxygenase inhibitory, and cytostatic activity of prepared compounds were measured. All the tested ligands demonstrated significant analgesic activity. Moreover, compounds 3i and 3h were the most potent ligands in the formalin and writhing tests, respectively. Compounds 3g, 3j, and 3l were the most COX-2 selective ligands and ligand 3e was the most potent COX inhibitor with a 0.79 of COX-2 selectivity ratio. The presence of electron-withdrawing moieties with hydrogen bonding ability at the meta position was found to affect the selectivity efficiently, in which compounds 3g, 3l, and 3k showed high COX-2 selectivity, and compound 3k was the most potent one. The cytostatic activity of selected ligands demonstrated that compounds 3e, 3f, 3h, 3k, and 3m showed good analgesic and COX inhibitory activity and were less toxic than the reference drug. High therapeutic index of these ligands is one of the valuable advantages of these compounds.

A Novel Phytocolorant, Neoxanthin, as a Potent Chemopreventive: Current Progress and Future Prospects.

Cancer is a general term for a group of similar diseases. It is a combined process that results from an accumulation of abnormalities at different biological levels, which involves changes at both genetic and biochemical levels in the cells. Several modifiable risk factors for each type of cancer include heredity, age, and institutional screening guidelines, including colonoscopy, mammograms, prostate-specific antigen testing, etc., which an individual cannot modify. Although a wide range of resources is available for cancer drugs and developmental studies, the cases are supposed to increase by about 70% in the next two decades due to environmental factors commonly driven by the way of living. The drugs used in cancer prevention are not entirely safe, have potential side effects and are generally unsuitable owing to substantial monetary costs. Interventions during the initiation and progression of cancer can prevent, diminish, or stop the transformation of healthy cells on the way to malignancy. Diet modifications are one of the most promising lifestyle changes that can decrease the threat of cancer development by nearly 40%. Neoxanthin is a xanthophyll pigment found in many microalgae and macroalgae, having significant anti-cancer, antioxidant and chemo-preventive activity. In this review, we have focused on the anti-cancer activity of neoxanthin on different cell lines and its cancer-preventive activity concerning obesity and oxidative stress. In addition to this, the preclinical studies and future perspectives are also discussed in this review.

Two-dimensional MXene Nanosheets and their Composites for Antibacterial Textiles: Current Trends and Future Prospects

Abstract: As a novel two-dimensional (2D) nanosheet (NS), MXene has attracted attention in antibacterial applications due to its excellent high surface area, remarkable hydrophilicity, strong flexibility, and excellent antibacterial properties. This review intends to provide valuable insight into the further development of antibacterial MXenes and their composite materials. In this paper, we review the antibacterial mechanisms of MXenes and their composite materials and summarize the research progress of antibacterial finishing fabrics, fibers and dressings based on MXene NSs. Due to the rich oxygen-containing groups, 2D MXene NSs and its composites exhibited significant antibacterial activity against Escherichia coli, Staphylococcus aureus, and Bacillus subtilis so they have been widely used in antibacterial textiles including finishing fabrics, fibers, and dressings. 2D MXene NSs have showed some antibacterial properties based on cell experiments or blood tests. The antibacterial mechanisms mainly include physical sterilization and chemical oxidative stress sterilization. The future direction of antibacterial textiles based on MXenes was proposed.

Investigation of The Effect of Metal-based Medicine Arsenicum album on Humoral Immune Response in SRBC-immunized Mice.

In complementary and alternative medicinal systems, the Arsenicum album in ultra-high dilution was used in various therapeutic conditions, considering its effects on the body's immune system, including the COVID-19 pandemic. However, scientific evidence regarding its immunomodulatory effects is insufficient. The current study aimed to investigate the immunomodulatory effects of Arsenicum album in an experimental mouse model. Immunomodulatory activity of potentized dilutions of Arsenicum album i.e., 6C, 30C, 200C in BALB/c mice was evaluated by humoral antibody titer and delayedtype hypersensitivity assays wherein a fixed concentration (0.5 ml of 1× 109 cells/ml) of freshly prepared sheep RBC was administered as a foreign antigen to generate primary and secondary antibodies. Arsenicum album showed significant immunomodulatory activity by increasing primary antibody titer evaluated on day 21 of the treatment in all the dilutions as compared to SRBC and vehicle control group in humoral immune response assay without showing any effect on delayed-type hypersensitivity. The results of this preliminary study indicate that oral administration of Arsenicum album has the potential to augment primary humoral response at all dilutions. Hence, the possibility of using the Arsenicum album could be explored to treat immunological conditions, infections, etc., as an alternative therapy alongwith modern medicines.

Using Integrin αvβ6–Targeted Positron Emission Tomography Imaging to Longitudinally Monitor Radiation-Induced Pulmonary Fibrosis In Vivo

PurposeRadiation-induced pulmonary fibrosis (RIPF) is a potentially serious and disabling late complication of radiation therapy. Monitoring RIPF progression is challenging due to the absence of early detection tools and the difficulty in distinguishing RIPF from other lung diseases using standard imaging methods. In the lungs, integrin αvβ6 is crucial in the development of RIPF, acting as a significant activator of TGF-β after radiation injury. This study aims to investigate integrin αvβ6-targeted PET imaging ([64Cu]Cu-αvβ6-BP) to study RIPF development in vivo. Methods and MaterialsWe used a focal RIPF model (70 Gy delivered focally to a 3 mm spot in the lung) and a whole lung RIPF model (14 Gy delivered to the whole lung) in adult C57BL/6J mice. Small animal PET/CT images were acquired 1h post-injection of 11.1 MBq of [64Cu]Cu-αvβ6-BP. Animals were imaged for eight weeks in the focal RIPF model and six months for the whole lung RIPF model. Immunohistochemistry for integrin αvβ6 and trichrome staining were performed. ResultsIn the focal RIPF model, there was focal uptake of [64Cu]Cu-αvβ6-BP in the irradiated region at week four that progressively increased at week 6 and 8. In the whole lung RIPF model, minimal uptake of the probe was observed at four months post-RT, which significantly increased at months five and six. Expression of integrin αvβ6 was validated histologically by immunohistochemistry in both models. ConclusionsIntegrin αvβ6-targeted PET imaging using [64Cu]Cu-αvβ6-BP can serve as a useful tool to identify radiation-induced pulmonary fibrosis in vivo.

Depression-reminiscent Behavior Induced by Chronic Unpredictable Mild Stress Paradigm in Mice Substantially Abrogated by Diosmin

Background: Diosmin has already been described and documented to be neuroprotective, antioxidant and anti-inflammatory. It may possess or hold depressionalleviating activity. Therefore, the purpose of the current research protocol is to investigate the depression-relieving proficiency of diosmin in stressed and unstressed mice. Methods: Male mice (Swiss albino) were imperiled to an unpredictable chronic stress paradigm every day for three sequential weeks, and depression-resembling behavioral despair was induced. Imipramine 15 mg/kg and diosmin (25, 50 and 100 mg/kg) were dispensed for 21 successive days to discrete groups of stressed and unstressed mice. Results: Both diosmin (100 mg/kg) and 15 mg/kg imipramine administration for 3 consecutive weeks substantially or significantly diminished the immobility period of mice imperiled to stress in comparison to stressed mice gauzed with the vehicle. Diosmin (25, 50 and 100 mg/kg) and imipramine considerably reinstated the diminished sucrose proclivity (sucrose preference percentage; %) in stressed mice, demonstrating their considerable or substantial depression-relieving effects. The locomotor activities of mice were not considerably altered by these drugs. Antidepressant-like activity of diosmin for immobility periods and preference for sucrose was observed to be analogous to imipramine. Diosmin (100 mg/kg) and imipramine substantially quashed CUMS- persuaded escalation of plasma corticosterone and nitrite levels, malondialdehyde levels and MAO-A activity in the brain of stressed mice. Both drugs also substantially reversed CUMS-prompted reduction in catalase activity and brain glutathione levels. Conclusion: Accordingly, diosmin revealed significant anti-depressive activity in mice imperiled to chronic mild unpredictable stress paradigm conceivably via mitigation of nitrosative and oxidative stress, reticence of brain MAO-A action, and sink drop of plasma corticosterone degrees.

READRetro: natural product biosynthesis predicting with retrieval-augmented dual-view retrosynthesis.

Plants, as a sessile organism, produce various secondary metabolites to interact with the environment. These chemicals have fascinated the plant science community because of their ecological significance and notable biological activity. However, predicting the complete biosynthetic pathways from target molecules to metabolic building blocks remains a challenge. Here, we propose retrieval-augmented dual-view retrosynthesis (READRetro) as a practical bio-retrosynthesis tool to predict the biosynthetic pathways of plant natural products. Conventional bio-retrosynthesis models have been limited in their ability to predict biosynthetic pathways for natural products. READRetro was optimized for the prediction of complex metabolic pathways by incorporating cutting-edge deep learning architectures, an ensemble approach, and two retrievers. Evaluation of single- and multi-step retrosynthesis showed that each component of READRetro significantly improved its ability to predict biosynthetic pathways. READRetro was also able to propose the known pathways of secondary metabolites such as monoterpene indole alkaloids and the unknown pathway of menisdaurilide, demonstrating its applicability to real-world bio-retrosynthesis of plant natural products. For researchers interested in the biosynthesis and production of secondary metabolites, a user-friendly website (https://readretro.net) and the open-source code of READRetro have been made available.

Mechanism analysis of essential oil from Radix Bupleuri for the treatment of asthma through regulation of ectopic olfactory receptor

Ethnopharmacological relevanceRadix Bupleuri is the root of Bupleurum chinense DC. (BC) and a classic aromatic traditional Chinese medicine. The traditional pharmacological effects of Radix Bupleuri are alleviating bronchial spasms, dilating airways, and promoting the resolution of respiratory inflammation, thereby reducing asthma symptoms. Aim of the studyStudies have demonstrated the efficacy of water extracts from BC in asthma treatment. However, the potential role of volatile oil, another active constituent in BC, remains unexplored with asthma. Notably, volatile oil is renowned for its ease of absorption and direct targeting of affected areas, offering distinct advantages in alleviating airway inflammation. This study aims to explain the anti-asthmatic mechanism of BC-oil through in vivo and in vitro pharmacological experiments. Materials and methodsFirstly, the OVA-induced SD rat asthma model was utilized to evaluate the pharmacological effect of BC-oil by lung function monitoring, HE staining, flow cytometry, ELISA, and RT-qPCR. The anti-asthmatic mechanism was further analyzed by combining transcriptomic analysis of lung tissue from rat model and airway smooth muscle tissue from public database. Initially, GC-MS was used to analyze the components of BC-oil. The anti-asthmatic activity was evaluated in 16-HBE, RBL-2H3, and ASMC cells using CAMKII inhibitors to explore of the critical signal transduction regulated by BC-oil. Furthermore, molecular docking and calcium flow assay were utilized to screen and identify the active components from BC-oil. ResultsOral administration of BC-oil significantly enhanced pulmonary function in asthmatic SD rats by reducing airway resistance and elastic resistance. Additionally, BC-oil inhibited inflammatory cytokines, including serum IL-2, pulmonary Il1b, Tnf, and Cxcl13, demonstrating potent anti-inflammatory and immunomodulatory effects. In this study, we analyzed the significant role of OR2W3 in asthma using public transcriptomic data. Furthermore, we indicated that BC-oil regulated the expression of Olr1433 and GNAL in rat lung tissue. BC-oil reduced degranulation and inhibited gene expression of Il3 and Tnf in RBL-2H3 cells and suppressed gene expression of IL8 and TNF in 16-HBE cells. BC-oil also attenuated airway smooth muscle cell proliferation and expression of Acta2 and Ccnd1. Furthermore, BC-oil regulates asthma-related cellular processes by activating CAMKII. GC-MS analysis identified 11 components of BC-oil, and n-hexadecanoic acid, linoleic acid and oleic acid from BC-oil were identified to interact with OR2W3 by molecular docking. The calcium flow assay revealed linoleic acid as a significant activator of OR2W3 and indicated that BC-oil alleviated asthma through the ectopic olfactory signaling pathway. ConclusionsThe mechanism of BC-oil in treating asthma through signal transduction of OR2W3 is revealed at the molecular and cellular levels.

Rape, law and stories of trauma: representations of sexual violence in The Australian Women’s Weekly, 1970–82

The 1970s ushered in a period of significant feminist activism, public debate and judicial reform on issues of rape and child sexual abuse. In this article, I examine how The Australian Women’s Weekly raised and navigated the issue of rape from its commercial position as a conservative-leaning publication between 1970 and 1982. It seeks to understand mainstream Australian women’s attitudes towards sexual assault and how they evolved under emerging feminist critique.

Biochemical and nutritional analysis of seaweed (Iyengaria stellata) and its therapeutic significance, using antioxidant, antimicrobial, and hypoglycemic activities

Seaweeds have gained significant attention for their bioactive compounds and extensive use in pharmaceuticals, nutraceuticals and cosmeceuticals. Therefore, comprehensive analysis was conducted to investigate the nutritional composition, identify and quantify the Phyco-chemicals and to evaluate the pharmacological potential using hypoglycemic, antimicrobial and antioxidant activities of Iyengaria stellata extract. The results of nutritional analysis revealed 39.72±2.60 % total ash, 14.54±0.44 % crude fat, 9.61±0.60 % proteins, 5.29±0.52 % crude fibers, 10.49±1.00 % moisture content, and total energy was 108.26±2.01 Kcal 100 g−1 of dry powder. Approximately, 15 compounds were tentatively detected in ethyl acetate extract with major compounds being Pentadecanoic acid, 14-methyl-, easter (31.62 %), (Z) -9- stearic acid, methyl easter (13.36 %), Elaidic acid, methyl easter (11.46 %), Phytol (6.31 %), n-Hexadecanoic acid (7.47 %), Linolelaidic acid, methyl ester (5.64 %) and 1-octadecyne (5.34 %). Similarly, n-butanol extract contained 16 compounds with primary compounds being Hexadecanoic acid, methyl ester (25.96 %), Elaidic acid methyl ester (21.39 %), Linolelaidic acid methyl ester (11.53 %), Octadecanoic acid, methyl ester (5.89 %), and Hexanedioic acid, dioctyl ester (5.26 %). FT-IR analysis revealed the presence of similar groups of compounds i.e. alcohols, phenols, lipids, carboxylic acids, amines, aromatics, ketones and halogens. Total phenolic contents (TPC) in ethyl acetate and n-butanol extract were measured as 2.982±0.876 mg GAEg−1 and 1.538±0.711 mg GAE g−1, whereas Total Flavonoids contents (TFC) were 2.058 ± 0.121 mg QE g−1 and 1.614 ± 0.643 mg QE g−1, respectively. Ethyl acetate extract exhibited more antioxidant potential with an IC50 (2.59±1.34) compared to n-butanol extract (2.75±1.60). Moreover, n-butanol extract exhibited strong antimicrobial activity. The most susceptible strains were E. coli, S. aureus and P. aeruginosa. In terms of in-vivo hypoglycemic activity, the n-butanol extract proved to be more effective which significantly reduced the blood glucose level up to 226.17±3.43, 201.33±4.63 and 265.17±3.92 at 300, 200 and 100 mg kg−1 doses respectively after 24 h. In conclusion, the seaweed I. stellata exhibited significant potential in terms of its antioxidant, antimicrobial, and hypoglycemic properties.

Diversity and Isolation of Endophytic Fungi in Panax japonicus and Biotransformation Activity on Saponins.

This study reports the diversity and community structure differences of the endophytic fungi of Panax japonicus of different ages to obtain novel endophytic fungi with glycoside hydrolytic activity for rare saponins production. This study used the high-throughput sequencing method to analyze the diversity and community structure of endophytic fungi of P. japonicus. The endophytic fungi were processed by traditional isolation, culture, conservation, and ITS rDNA sequence analyses. Then the total saponins of P. japonicus were used as the substrate to evaluate the glycoside hydrolytic activity. The composition analysis of the community structure showed that the abundance, evenness, and diversity of endophytic fungi of nine-year-old P. japonicus were the best among all samples. A total of 210 endophytic fungi were isolated from P. japonicus samples and further annotated by sequencing the internal transcribed spacer. Then the biotransformation activity of obtained strains was further examined on total saponins of P. japonicus (TSPJ), with a strain identified as Fusarium equiseti (No.30) from 7-year-old P. japonicus showing significant glycoside hydrolytic activity on TSPJ, including ginsenoside Ro→zinglbroside R1, pseudoginsenoside RT1→pseudoginsenoside RP1, chikusetsusaponin IV→tarasaponin VI and chikusetsusaponin IVa →calenduloside E. These results reveal the diversity and community structure differences of the endophytic fungi of P. japonicus with different ages and establish a resource library of endophytic fungi of P. japonicus. More importantly, we identified a valuable endophytic fungus with glycoside hydrolytic activity and provided a promising convenient microbial transformation approach to produce minor deglycosylated ginsenosides.

New findings on post-mortem chicken quality changes: The ROS-influenced MAPK-JNK signaling pathway affects chicken quality by regulating muscle cell apoptosis

Research conducted previously has demonstrated that apoptosis significantly influences the chicken quality. While ROS are acknowledged as significant activators of apoptosis, the precise mechanism by which they influence muscle cell apoptosis in the post-mortem remains unclear. In this study, chicken samples were treated with rosemarinic acid and H2O2 to induce varying ROS levels, and the ROS-triggered apoptosis mechanism in chicken muscle cells in post-mortem was analyzed. The TUNEL results revealed that elevated ROS levels in chicken were associated with a greater degree of muscle cell apoptosis. Western-blot results suggested that sarcoplasmic ROS could initiate apoptosis through the mitochondrial pathway by activating the MAPK-JNK signaling pathway. Moreover, TEM and shear force results demonstrated that muscle cell apoptosis initiates myofiber fragmentation and structural damage to sarcomeres, ultimately reducing chicken tenderness. This study enhances our understanding of post-mortem muscle cell apoptosis, providing valuable insights for regulating chicken quality.

Recent Advances in Biomedical Nanotechnology Related to Natural Products.

Natural product processing via nanotechnology has opened the door to innovative and significant applications in medical fields. On one hand, plants-derived bioactive ingredients such as phenols, pentacyclic triterpenes and flavonoids exhibit significant pharmacological activities, on another hand, most of them are hydrophobic in nature, posing challenges to their use. To overcome this issue, nanoencapsulation technology is employed to encapsulate these lipophilic compounds and enhance their bioavailability. In this regard, various nano-sized vehicles, including degradable functional polymer organic compounds, mesoporous silicon or carbon materials, offer superior stability and retention for bioactive ingredients against decomposition and loss during delivery as well as sustained release. On the other hand, some naturally occurring polymers, lipids and even microorganisms, which constitute a significant portion of Earth's biomass, show promising potential for biomedical applications as well. Through nano-processing, these natural products can be developed into nano-delivery systems with desirable characteristics for encapsulation a wide range of bioactive components and therapeutic agents, facilitating in vivo drug transport. Beyond the presentation of the most recent nanoencapsulation and nano-processing advancements with formulations mainly based on natural products, this review emphasizes the importance of their physicochemical properties at the nanoscale and their potential in disease therapy.

A Comprehensive Review of the Benzimidazole Scaffold as a Potential Nucleus for Anti-Ulcer Activity

Abstract: The benzimidazole scaffold is a promising nucleus for developing novel therapeutic agents for ulcer treatment. Its unique chemical structure provides desirable pharmacological properties, such as excellent bioavailability, metabolic stability, and low toxicity, making it an attractive candidate for ulcer treatment. Several benzimidazole derivatives have shown significant anti-ulcer activity in preclinical and clinical studies, acting through multiple pathways, including inhibition of gastric acid secretion, suppression of gastric inflammation, and promotion of mucosal protection. Some benzimidazole derivatives have also demonstrated anti-Helicobacter pylori activity, suggesting their potential for eradicating bacteria associated with ulcer formation. However, challenges such as poor solubility and limited selectivity remain. Various approaches, such as prodrug design and formulation optimization, have been explored to overcome these issues and improve the therapeutic profile of benzimidazole derivatives. Overall, the benzimidazole scaffold holds great promise as a nucleus for developing novel anti-ulcer agents. Further research and optimization efforts are needed to harness its full potential and translate it into effective treatments for ulcers. With continued advancements in medicinal chemistry and drug design, benzimidazole-based compounds may offer new therapeutic options for patients suffering from ulcers and related gastrointestinal disorders. Hence, this review highlights the knowledge about benzimidazole scaffold, the mechanism of ulcer formation, and various benzimidazole derivatives with anti-ulcer activity, which can be further studied in pre-clinical and clinical trials.

In-vitro Antioxidant, In-vitro and In-silico Ovarian Anticancer Activity (Ovarian Cancer Cells-PA1) and Phytochemical Analysis of Cissus quadrangularis L. Ethanolic Extract.

Cissus quadrangularis is a valuable natural source of traditional medicines. An in vitro investigation was performed to determine whether the ethanolic extract from the whole portions of C. quadrangularis had anticancer and free radical scavenging activities against ovarian cancer cells-PA1. C. quadrangularis is a herb collected from rural areas in Andhra Pradesh, India. C. quadrangularis was air-dried and crushed, and the powder and ethanol (0.5 kg) were used in a Soxhlet device for continuous extraction. Phytochemical analysis of the extracts was performed using a standard procedure. The antioxidant activity of the ethanolic extract of C. quadrangularis was evaluated using DPPH. An in vitro anticancer study used an ethanolic extract against the PA1 cell line. Apoptosis of ovarian cancer cells was studied using DAPI and carboxy-H2DCFDA staining. From LC-MS analysis, quercetin-3-O-alpha-Lrhamnopyranoside and erucic acid were docked with the threonine tyrosine kinase (TTK) enzyme using auto docking. The ethanolic extract of C. quadrangularis demonstrated significant dose-dependent antioxidant activity compared to ascorbic acid. The ethanolic extract of C. quadrangularis was found to have high anticancer activity against ovarian cancer cell lines (PA1), with an IC50 value of 482.057 ± 113.857 μg/ml. DAPI and carboxy-H2DCFDA staining confirmed that C. quadrangularis ethanolic extract induced apoptosis in ovarian cancer cells (p < .001). Molecular docking studies helped identify the binding affinities between the protein and ligand complexes, such as Quercetin-3-O-alpha-Lrhamnopyranoside binding sites of target proteins 5N7V (MET602, GLN672) and erucic acid 5N7V (GLY354). Quercetin-3-O-alpha-L-rhamnopyranoside was reported to bind with 5N7V by hydrogen bonding at MET602 and GLN672 amino acids with 2.02, 2.99 Å bonding length distance and binding affinity of -7.9 kcal/mol. Erucic acid was reported to bind with 5N7V by hydrogen bonding at GLY354 amino acid with 3.18, 2.93 Å bonding length (Å) distance and binding affinity of -4.3 kcal/mol. The current analysis showed that the ethanolic extracts of C. quadrangularis L. exhibited antioxidant and anticancer properties against ovarian PA1 cells. The experimental results confirmed that C. quadrangularis L. is a promising, safe chemotherapeutic plant for ovarian cancer PA1 cells. The docking results demonstrated that Quercetin-3-O-alpha-L-rhamnopyranoside strongly binds threonine tyrosine kinase at the MET602 and GLN672 positions. This study showed that the C. quadrangularis ethanolic extract has Quercetin-3-O-alpha-L-rhamnopyranoside, which can be used as an anticancer agent.

Biological Potential of a Bibenzyl Compound ‘Gigantol’ for the Treatment of Human Disorders: Pharmacological Activities and Analytical Aspects of an Active Phytochemical Isolated from Orchid

Background: Dendrobium chrysotoxum Lindl. is an important medicinal plant of the genus Dendrobium from the Orchidaceae family. Gigantol is one of the key bioactive phytochemicals found in Dendrobium plants. Gigantol is reported to have diverse pharmacological activities Aims: This narrative review explores the analytical aspects along with pharmacological activities of gigantol as reported in different scientific publications. Methods: To find appropriate information related to Dendrobium plants and gigantol, extensive data extraction was done using ScienceDirect, Google, PubMed, and Scopus databases, and diverse facts were collected, arranged and analyzed to know the therapeutic potential of gigantol. Analytical aspects of gigantol were also discussed in the present work. Results: Gigantol has a wide distribution in the Dendrobium officinale, Dendrobium chrysanthum, Dendrobium crystallinum, Dendrobium aphyllum, and Dendrobium devonianum. Available data indicates diverse pharmacological activities of gigantol. Preclinical studies have shown its effectiveness in the treatment of cataractogenesis, liver injury, leishmaniasis, nephrotoxicity, spasm, and skin disorders. Gigantol has been found to control hepatocellular cancer, lung cancer, breast cancer, bladder cancer, and cervical cancer. The neuroprotective, antinociceptive, anti-inflammatory, antioxidant, vasorelaxant, immune modulatory effect, antimalarial, and anti-herpetic properties of gigantol have also been observed. Applications of different analytical techniques for the isolation and characterization of gigantol were also discussed in detail. Conclusion: Gigantol has significant and diverse pharmacological activities that must be explored in clinical setup to develop therapeutic leads for different diseases and health conditions.

Screening of essential oils against oxacillin-resistant Staphylococcus aureus strains isolated from bovine mastitis

Bovine mastitis is a disease with far-reaching consequences for the dairy industry. Staphylococcus aureus is a pathogen that is especially resistant to antibiotics. The objective of this study was to evaluate the antimicrobial activity of the essential oils Lippia citriodora (Lam.), Thymus vulgaris (L), and a mixture of the essential oils Lippia citriodora and Thymus vulgaris (50/50 v/v), against isolates of oxacillin-resistant Staphylococcus aureus (n=15) of positive cases of bovine mastitis. For the statistical analysis, the IBM SPSS statistical package was used. The mixture of essential oils (Lippia citriodora and Thymus vulgaris (50/50 v/v)) obtained the most significant antimicrobial activity in relation to pure essential oils. It is therefore concluded that the mixture of these oils boosts their antimicrobial activity (p&lt;0.05). The minimum inhibitory and bactericidal concentration of this mixture for the total isolations was 12 μL/L and 25 μL/mL, respectively.