Phytochemical Composition and Antioxidant and Anti-Inflammatory Activities of Humboldtia sanjappae Sasidh. & Sujanapal, an Endemic Medicinal Plant to the Western Ghats.

Ethnomedicinal plants are important sources of drug candidates, and many of these plants, especially in the Western Ghats, are underexplored. Humboldtia, a genus within the Fabaceae family, thrives in the biodiversity of the Western Ghats, Kerala, India, and holds significant ethnobotanical importance. However, many Humboldtia species remain understudied in terms of their biological efficacy, while some lack scientific validation for their traditional uses. However, Humboldtia sanjappae, an underexplored plant, was investigated for the phytochemical composition of the plant, and its antioxidant, enzyme-inhibitory, anti-inflammatory, and antibacterial activities were assessed. The LC-MS analysis indicated the presence of several bioactive substances, such as Naringenin, Luteolin, and Pomiferin. The results revealed that the ethanol extract of H. sanjappae exhibited significant in vitro DPPH scavenging activity (6.53 ± 1.49 µg/mL). Additionally, it demonstrated noteworthy FRAP (Ferric Reducing Antioxidant Power) activity (8.46 ± 1.38 µg/mL). Moreover, the ethanol extract of H. sanjappae exhibited notable efficacy in inhibiting the activities of α-amylase (47.60 ± 0.19µg/mL) and ß-glucosidase (32.09 ± 0.54 µg/mL). The pre-treatment with the extract decreased the LPS-stimulated release of cytokines in the Raw 264.7 macrophages, demonstrating the anti-inflammatory potential. Further, the antibacterial properties were also evident in both Gram-positive and Gram-negative bacteria. The observed high zone of inhibition in the disc diffusion assay and MIC values were also promising. H. sanjappae displays significant anti-inflammatory, antioxidant, antidiabetic, and antibacterial properties, likely attributable to its rich composition of various biological compounds such as Naringenin, Luteolin, Epicatechin, Maritemin, and Pomiferin. Serving as a promising reservoir of these beneficial molecules, the potential of H. sanjappae as a valuable source for bioactive ingredients within the realms of nutraceutical and pharmaceutical industries is underscored, showcasing its potential for diverse applications.

Potential use of bio functionalized nanoparticles to attenuate triple negative breast cancer (MDA-MB-231 cells).

This study showed that bio-functional silver nanoparticles (AgNPs) and zinc oxide nanoparticles (ZnONPs) were synthesized in aqueous extracts of Gymnema sylvestre leaves and tested for toxicity assessment against triple-negative breast cancer cells (TNBC). Biofunctional nanoparticle (NPs) samples were characterized using UV-Vis spectroscopy, FT-IR, XRD, SEM, and TEM. The results showed that the phytofabrication of AgNPs resulted in a dark brown, UV-vis maximum absorbance peak at 413 nm. The AgNPs were crystalline and spherical, with sizes ranging from 20 to 60 nm, as confirmed by the XRD pattern and TEM images. Another phytofabrication of ZnONPs exhibited a white precipitate corresponding to a UV-Vis maximum absorption peak at 377 nm and a fine micro flower morphology with a particle-sized tribution between 100 and 200 nm. In addition, FT-IR spectra showed that bioorganic compounds are associated with NPs that respond to reduced Ag+ ions and AgNPs tabilizers. Invitro cytotoxicity studies revealed the potent anti-cancer effects of phytofabricated AgNPs and ZnONPs on TNBC cells. Furthermore, the AO/EB double staining assay results proved that apoptotic cells are distinguished by greenish-yellow fluorescence of the cell nuclei with IC50 concentrations of 44 ± 0.8 µg/mL for AgNPs and 26.2 ± 0.5 µg/mL for ZnONPs, respectively. Based on our results, we expect that the anticancer function of the biofunctional NPs is due to the apoptotic activation of TNBC cells by increased ROS. Therefore, the presented study demonstrated that biofunctional AgNPs and ZnONPs have excellent prospects for the anti-cancer activity that can be used in pharmaceutical and medical fields.

Antioxidant, Antimicrobial, Cytotoxicity, and Larvicidal Activities of Selected Synthetic Bis-Chalcones.

Plants are known to have numerous phytochemicals and other secondary metabolites with numerous pharmacological and biological properties. Among the various compounds, polyphenols, flavonoids, anthocyanins, alkaloids, and terpenoids are the predominant ones that have been explored for their biological potential. Among these, chalcones and bis-chalcones are less explored for their biological potential under in vitro experiments, cell culture models, and animal studies. In the present study, we evaluated six synthetic bis-chalcones that were different in terms of their aromatic cores, functional group substitution, and position of substitutions. The results indicated a strong antioxidant property in terms of DPPH and ABTS radical-scavenging potentials and ferric-reducing properties. In addition, compounds 1, 2, and 4 exhibited strong antibacterial activities against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Salmonella enteritidis. The disc diffusion assay values were indicative of the antibacterial properties of these compounds. Overall, the study indicated the antioxidant and antimicrobial properties of the compounds. Our preliminary studies point to the potential of this class of compounds for further in vivo investigation.

Solanum pubescens Wild Fruits Essential Oil - A Golden Casket for its Antimicrobial and Anti-inflammatory Mediated Wound Healing Efficacy in Vertebrate Model Mus musculus.

BACKGROUND: Solanum pubescens Willd, growing wild in the hills of Rayadurg jurisdiction of Southwestern Andhra Pradesh, has gained significant attention among researchers for its diverse folkloric applications, existence of novel phytochemicals and leaf extracts which hold great medicinal promises. To date, the S. pubescens fruit's essential oil (SPO) has never been investigated. METHODS: The current research has been focused to evaluate the chemical composition of S. pubescens fruit essential oil through Gas Chromatography-Mass Spectrometry (GC-MS), followed by the investigation of antibacterial, antifungal, anti-inflammatory, analgesic and wound healing activities in appropriate models to uncover its biological potentials. Extraction of (Solanopuboil/SPO) from the fresh unripe fruits of Solanum pubescens was carried out in Buchner funnel and Whatman no.10 filter paper and concentrated at 40°C using a rotary evaporator. The metabolic profiling of SPO was analysed by GC-MS technique. The MIC, MBC, activity index, and total antimicrobial activity of SPO were evaluated using standard procedures. Anti-inflammatory activity of SPO was screened using Carrageenan induced paw oedema and Cotton pellet-induced granuloma. Tail immersion test, Acetic acid writhing response and Formalin paw lick test was performed in rats in order to examine the analgesic activity of SPO. Wound healing activity of SPO was investigated by performing the incision wound model, Excision wound model and Dead space wound model in rats. RESULTS: The SPO displayed a constant degree of antimicrobial activity against B. cereus, B. subtilis, E. coli, A. niger, A. fumigatus and C. albicans with significant anti-inflammatory and analgesic activities. Also, a prominent wound healing potential of it was observed in excision, incision and dead space wound models with considerable elevation in granulation tissue hydroxyproline, hexuronic acid and hexosamine content in association with remarkable regulation of anti-inflammatory and antioxidant markers i.e., Lipid peroxidase (LPO), Nitric Oxide (NO), Superoxide dismutase (SOD), Glutathione (GSH), Catalase (CAT), Glutathione Peroxidase (GPx). CONCLUSION: These findings strongly validate the therapeutic potential of S. pubescens fruit essential oil in antimicrobial and anti-inflammatory mediated wound healing and suggests its promising application as valuable and novel indigenous leads in the food and pharmaceutical industries. To the best of our knowledge, this is the first-ever investigatory report on the systematic phytochemical and therapeutic examination of S. pubescens fruit essential oil.

Protective Effect of Borassus flabellifer Haustorium Extract against Alkoxyl Radical-Induced Cytotoxicity by Improving Glutathione Metabolism by Modulating Nrf2/Haeme Oxygenase-1 Expression.

AIM: The study was aimed to assess the ability of Borassus flabellifer haustorium methanolic extract (BHE) on de novo glutathione biosynthesis in normal and pro-oxidant exposed cells via Nuclear factor erythroid 2-related factor 2 (Nrf2) and haeme oxygenase-1 (HO1) signaling in 2,2'-Azobis(2-methylpropionamidine) di-hydrochloride (AAPH) induced cytotoxicity in normal intestinal epithelial cells (IEC-6 cells). METHODS: The in vitro antioxidant activity was determined in terms of radical scavenging and ex vivo hemolysis. The cytoprotective effect was studied using AAP H as the alkoxyl radical inducer in IEC-6 cell model. The mechanistic basis of protection is determined by Nrf2/HO1 expression using qPCR. RESULTS: In vitro screening observed DPPH, hydrogen peroxide and ABTS radical scavenging activity for the BHE; further, BHE also protected the oxidative hemolysis in the erythrocytes induced by AAPH. In IEC-6 cells, AAPH treatment significantly reduced the cell viability (p < 0.001) by inducing lipid peroxidation. Further, there observed a significant reduction in the activities of enzymes involved in the de novo glutathione biosynthesis (p < 0.01) and glutathione reductase in these cells. However, pretreatment with BHE (10, 25 and 50 µg/mL) dose-dependently protected from the cytotoxicity of AAPH-derived alkoxyl radicals (p < 0.05); besides, the de novo glutathione biosynthesis and regeneration of GSH from oxidized form was also increased in these cells. In corroboration with the biochemical parameters, the Nrf2/HO1 expression was upregulated by the BHE pretreatment concomitantly reducing the cellular lipid peroxidation products. The improvement glutathione biosynthesis was also observed in BHE alone treated cells. CONCLUSION: The study indicated the potential of methanolic extract of Borassus flabellifer haustorium in enhancing the de novo glutathione biosynthesis in normal and pro-oxidant exposed cells by Nrf2/HO1 dependent manner, concomitantly mitigating the toxicity of AAPH-derived alkoxyl radicals in intestinal epithelial cells.

Analysis of the chemical composition of root essential oil from Indian sarsaparilla (Hemidesmus indicus) and its application as an ecofriendly insecticide and pharmacological agent.

The Indian sarsaparilla (Hemidesmus indicus) is a commonly used plant in Indian traditional medicine of Ayurveda for the preparation of various non-alcoholic beverages. However, limited studies are available on the essential oil of H. indicus roots (HRO); therefore, the study evaluated the antioxidant, anti-inflammatory and antidiabetic activities of H. indicus root essential oil as well as insecticide potential against the common pests of stored food materials (Sitophilus oryzae, Callosobruchus maculatus and Tribolium castaneum). The repellant efficacy of HRO was found to be high against S. oryzae (8.21 ± 0.55 µg/mL). Likewise, the fumigant potential was also observed for HRO against these pests; the higher activities were observed against S. oryzae and C. maculatus (32.46 ± 1.42 and 35.18 ± 1.62 µg/L). Besides, the essential oil was also found to be active as a contact poison, however, against all the three pests, the toxicity was above 100 µg/mm3, being the highest against C. maculatus (122.8 ± 3.57 µg/mm3). To analyze the possible effect of the essential oil on grains, the different grains were allowed to germinate and compared to that of normal; thus, the non-toxic nature of HRO against the stored products is also confirmed. The essential oil shown to have DPPH hydrogen peroxide and ABTS radical scavenging, nitric oxide scavenging potential, and inhibition of lipoxgenase, alpha-amylase and alpha-glucosidase. Overall, the present study concludes that the H. indicus may be a suitable repellant and fumigant agent against different pests of stored products and a possible antioxidant, anti-inflammatory, and anti-diabetic agent.

Antimicrobial and anti-biofilm activities of polyphenols extracted from different Saudi Arabian date cultivars against human pathogens.

BACKGROUND: Microbial diseases have emerged as a serious threat to the healthcare system globally and also in Saudi Arabia; various diseases are associated with higher mortality and increased spreading rates. Dietary sources are often entertained to improve the immune system of the body to fight against these infections. The date fruit (Phoenix dactylifera L) is one such functional food that is less explored for its actual potentials. METHODS: The polyphenols isolated from the different cultivars of dates in Saudi Arabia (Ajwa, Safawi, Khalas, and Sukkary) was evaluated for their antibacterial, anti-fungal and anti-biofilm forming abilities. The anti-radical properties of the phenolic extract were conducted in terms of the scavenging of diphenyl-1-picrylhydrazyl radical, hydrogen peroxide radicals and ABTS radicals. The anti-inflammatory potential was analyzed in terms of lipoxygenase activity inhibition. RESULTS: The phenolic compounds of different dates were spectrophotometrically estimated and cultivars such as Ajwa and Sukkary had the highest polyphenol content. It was also noteworthy that they exerted potent antibacterial activities against Staphylococcus aureus, Streptococcus pyogenes, and Pseudomonas aeruginosa as estimated by the least minimal inhibitory concentration (MIC) or minimal bactericidal concentration (MBC) values. Besides, these polyphenols reduced the biofilm formation by these bacterial pathogens; it is thus possible that the polyphenols from dates can be a promising antimicrobial agent against various pathogenic strains. Corroborating with these, the polyphenol extracts from different Saudi Arabian dates were found to inhibit the growth of mycelium in strains of Candida albicans and Aspergillus niger. Apart from these, the polyphenol isolates also exhibited significant anti-radical properties against different reactive radical systems. CONCLUSION: Overall, the efficacy of phenolic compounds extracted from the dried date fruits are not only restricted to the functional food features; instead, these molecules are capable of preventing the growth of microbial pathogens of humans. Hence, it may emerge as potent antibacterial, anti-fungal and anti-biofilm forming candidates.

Phytochemical profiling of Azima tetracantha Lam. leaf methanol extract and elucidation of its potential as a chain-breaking antioxidant, anti-inflammatory and anti-proliferative agent.

Azima tetracantha, a traditional medicinal plant included in the order Brassicales and family Salvadoraceae, is widely used as a dietary supplement in folklore medicines. The plant is also used for the treatment of rheumatism, diarrhea and other inflammatory disorders. The present investigation focused on the phytochemical composition, radical scavenging, reducing potential and anti-proliferative activities of the A. tetracantha leaves. Quantitative estimation of the polyphenols and flavonoids revealed significantly elevated levels in the methanol extract. Corroborating with this, methanol extract exhibited higher in vitro anti-radical scavenging effect against 2,2-diphenyl-1- picrylhydrazyl (34.14 ± 2.19 µg/mL), and hydrogen peroxide (44.96 ± 1.77 µg/mL), as well as ferric reducing properties (58.24 ± 6.98 µg/mL). The methanolic extract also showed strong lipoxygenase (71.42 ± 6.36 µg/mL) and nitric oxide inhibitory activities (94.23 ± 8.11 µg/mL). Cytotoxic activity against MCF7 cells was found to be higher (IC50= 37.62 ± 2.94 µg/mL), than that of MDAMB231 cells (IC50= 69.11 ± 5.02 µg/mL). The qPCR-based analysis indicated dose-dependent increase in the expression of the pro-apoptotic genes such as executioner caspases and apoptotic protease activating factor-1. Overall, the results indicated the possible use of methanol extract of A. tetracantha leaves as a chain-breaking antioxidant molecule and are capable of inhibiting inflammatory enzymes and the proliferative potential of breast cancer cells.

Chemical Composition, Insecticidal and Mosquito Larvicidal Activities of Allspice (Pimenta dioica) Essential Oil.

Essential oils are biologically and environmentally safe pesticidal compounds yielded from aromatic plants. Spices are important sources of essential oils, and they are widely used in the medicine, food, and various other industries. Among the different spices, Allspice (Pimenta dioica) is underexplored in terms of its biological efficacy and a limited number of studies are available on the chemical composition of Allspice essential oil (AEO); thus, the present study evaluated the larvicidal property, the repellency, and the fumigant toxicity against common pests of stored products of AEO. AEO was found to inhibit the survival of larvae of such vectors as Aedis, Culex, and Armigeres species. Further, AEO was found to exert repellant effects against the pests of such stored products as Sitophilus, Callosobruchus, and Tribolium. Similarly, the fumigant toxicity was found to be high for AEO against these species. The contact toxicity of AEO was high against Sitophilus and Callosobruchus. Apart from that, the essential oil was found to be safe against a non-target organism (guppy fishes) and was found to be non-genotoxic in an Allium cepa model. Overall, the results of the present study indicate that the essential oil from Allspice could be used as an environmentally safe larvicidal and biopesticidal compound.

Partially purified lead molecules from Dodonaea viscosa and their antimicrobial efficacy against infectious human pathogens.

BACKGROUND: The utilization of medicinal plants and their drugs have the advantage of reducing side effects compared with manufactured antimicrobials. Artificial drugs have unpleasant side effects, further, the number of drug resistant pathogens is increasing, thus huge challenge for control of resistant pathogens. Therefore, the current research explores the potential of partially purified bioactive compounds from Dodonaea viscosa against certain human pathogens. METHODS: Healthy leaves of D. viscosa (L.) were collected, extracted and optimized with different solvents. Preliminary phytochemical screening of the extracts was done and antibacterial activities were tested against human pathogens. The active crude extract was further purified by column chromatography and the homogeneity was confirmed by thin layer chromatography (TLC). The partially purified compounds were screened further for antibacterial, antibiofilm and anticancer activities. RESULTS: The crude ethanol extract of D. viscosa leaves showed the presence of phytochemical like tannins, alkaloids, flavanoids, terpenoids, glycosides, steroids and phenols. Ethanol extract exhibited the maximum zone of inhibition (11 mm) against S. agalactiae, B. cereus, S. typhi and E. coli at 15 mg when compared with other bacteria. Column chromatography fractions Dv12 and Dv20 exhibited the maximum zone of inhibition against B. cereus. 1000 µg of Dv12 partially purified compound against streptococcus isolates in glass test tube showed biofilm inhibition range of 34.4%-63.1%. Whereas B. cereus, S. aureus, S. typhi, and K. pneumoniae showed 31.1%-53.6% biofilm inhibition compared to curcumin control. Active fractions of Dv12 and Dv20 increased concentration confirmed that the gradual decrease in cell density and possesses growth inhibition towards A 549 human lung adenocarcinoma cells. CONCLUSION: We have extracted the bioactive compounds from D. viscosa (L.) leaves and tested the activity of a partially purified compound against human pathogenic bacteria, biofilm formation and cytotoxicity against A 549 human lung adenocarcinoma cells. The purified bioactive compounds might be used as therapeutic agents against different microbial infections such as skin infection, throat infection and other infectious diseases.

Chemical Composition of Cinnamomum verum Leaf and Flower Essential Oils and Analysis of Their Antibacterial, Insecticidal, and Larvicidal Properties.

Cinnamomum verum is widely used in traditional medicines, and the different parts of the plant, such as bark, leaves, and flowers, are used for essential oil production. The present study compared the chemical composition of the essential oil of C. verum extracted from the leaves and flowers. In addition, efficacy of these essential oils against the two common pests Sitophilus oryzae and Callosobruchus maculatus was also evaluated. The results indicated the presence of cinnamaldehyde, eugenol, caryophyllene, and linalool in these essential oils, however, at different concentrations. The leaf essential oil was found to be 10-20% more effective as a fumigant against both the pests. Likewise, the leaf essential oil found to repel these pests even at lower concentrations than that of flower essential oil of C. verum. Besides, these essential oils were also effective in controlling the growth of various gram positive and gram negative microbial pathogens and possibly a safeguard for human health. On contrary, both the essential oils were found to be safe for the application on grains, as indicated by their germination potentials. It was also observed that these essential oils do not cause any significant toxicity to guppy fishes, thus confirming their ecological safety for use as a biopesticide.

Toxic effects of fluoride in intestinal epithelial cells and the mitigating effect of methanol extract of coconut haustorium by enhancing de novo glutathione biosynthesis.

Fluoride ions are an important environmental contaminant and pollutant found in a wide variety of environmental conditions. The fluoride in drinking water is evident to induce toxic effects including neurodegeneration, skeletal and dental fluorosis as well as organ damage. Nutraceuticals and functional foods are emerging as possible preventive agents against fluoride toxicity. Hence, the possible use of an emerging functional food-the coconut haustorium is being evaluated against sodium fluoride-induced toxicity in intestinal cells (IEC-6). The cells exposed to fluoride showed significant cell death mediated through the increased lipid peroxidation and glutathione depletion. The glutathione biosynthetic enzymes were inhibited by the exposure to fluoride and the apoptotic genes (caspases 3/7 and apaf-1) were upregulated. The CHE pre-treatment improved the activity of enzymes involved in the de novo biosynthesis of glutathione and subsequently improved the intracellular GSH pool. The improved antioxidant defense was also evident from the reduced expression of apoptotic genes (p < 0.05). Overall, the study concludes that fluoride ions induce oxidative stress-mediated apoptosis in intestinal epithelial cells, via inhibiting glutathione biosynthesis. Methanol extract of coconut haustorium increased glutathione biosynthesis and subsequently prevented fluoride toxicity in IEC-6 cells by virtue of its antioxidant potentials.

Changes in chemical composition of Zilla spinosa Forssk. medicinal plants grown in Saudi Arabia in response to spatial and seasonal variations.

Extracts of different medicinal plants had been used to control several diseases in both traditional medicine and modern drugs. In the current study, we aimed to examine the changes in chemical composition of Zilla spinosa Forssk. plants collected from different habitats in Saudi Arabia in response to spatial and seasonal variations. Z. spinosa samples were collected from two different sites in Riyadh and Eastern regions in Saudi Arabia to examine the spatial variations effects on the studied parameters. Samples were collected from both sites at two different times (3:00 PM and 3:00 AM) to examine the effect of light on the chemical content and composition of these plants. Samples was, also, collected from the same sites at two different seasons (on start of January 2018 "winter season" and end of May 2018 "summer season") to examine the effect of temperature changes (seasonal variations) on the chemical content and composition of the different studied plants. In Z. spinosa plants collected from Riyadh region, squalene was found to be the major constitute of 3 samples; however, surprisingly, the sample collected in Winter at 3:00 AM showed the presence of mome inositol and (Z)-5-(formylmethylene)-4-methoxy-2(5 h)-furanone as the dominant components. Similarly, chemical compositions of essential oils extracted from Z. spinosa samples collected from Eastern region in the Summer season was dominated by squalene. Z. spinosa plants showed that all collected samples had high carbohydrate and protein contents with very low content of fats.

Tracking Five Millennia of Horse Management with Extensive Ancient Genome Time Series.

Horse domestication revolutionized warfare and accelerated travel, trade, and the geographic expansion of languages. Here, we present the largest DNA time series for a non-human organism to date, including genome-scale data from 149 ancient animals and 129 ancient genomes (≥1-fold coverage), 87 of which are new. This extensive dataset allows us to assess the modern legacy of past equestrian civilizations. We find that two extinct horse lineages existed during early domestication, one at the far western (Iberia) and the other at the far eastern range (Siberia) of Eurasia. None of these contributed significantly to modern diversity. We show that the influence of Persian-related horse lineages increased following the Islamic conquests in Europe and Asia. Multiple alleles associated with elite-racing, including at the MSTN "speed gene," only rose in popularity within the last millennium. Finally, the development of modern breeding impacted genetic diversity more dramatically than the previous millennia of human management.