Bioactive Principles Research Articles

Principle active metabolites of Pinus morrisonicola Hayata synergistically inhibit cell proliferation and autophagy to elevate apoptosis in hepatocellular carcinoma cells.

Hepatocellular carcinoma (HCC), a common primary tumor of liver is a leading cause of cancer-associated deaths. Improving cellular apoptosis and enhancing autophagic clearance is been considered to improve treatment outcomes of HCC. Polyphenols from Pinus morrisonicola (Hayata) have shown various physiological and therapeutic benefits and the flavonoid chrysin is been known for their anticancer effects. However, the main bioactive principle and the mechanism underlying the antitumor activity of pine needle extract are not clear yet. In this study, the effects of ethanol extract from pine needle on HCC cells were determined. The results show that when compared with administration of chrysin alone, a fraction containing pinocembrin, chrysin, and tiliroside significantly reduced autophagy and increased apoptosis. The results also correlated with decrease in cell cycle regulators and the autophagic proteins like LC3-II. Collectively, the results imply the fraction containing pinocembrin, chrysin, and tiliroside as an ideal complementary medicine for an effective antitumor activity.

A comprehensive review on traditional therapeutic uses, bioactive principles and pharmacological activities of Kantakari (Solanum virginianum L.): An important Ayurvedic herb

Solanum virginianum L., a perennial wild plant, belongs to the 'Dashamoola' group in Ayurveda. 'Kantkari Ghrita' in Charaka Samhita is used for cough, cold, fever, asthma, and cardiac diseases. 'Dasmul Asava' and 'Dashmularishta' are tonics for lactating mothers. Inflammatory disorders, rheumatism, and diabetes are traditionally treated using leaf juice and fruits. Various plant parts contain bioactive compounds like solamargine, solasonine, campesterol, ?-sitosterol, cycloartenol, chlorogenic acid, vanillic acid, etc. Roots, flowers, stems, and fruits are used for their medicinal properties such as carminative, febrifuge, expectorant, diuretic, and bitter tonic effects. They are employed to treat cough, asthma, fever, toothache, tuberculosis, rheumatism, sore throat, kidney disorders, gonorrhea, vesicular eruptions, and burning sensation in the feet. Different extracts from various plant parts exhibit significant anti-inflammatory, nephroprotective, anti-asthmatic, hepatoprotective, immunomodulatory, antimicrobial, larvicidal, antinociceptive, antispermatogenic, antioxidant, and antidiabetic activities. This study reviews 37 relevant research articles to comprehensively explore the plant's traditional uses, bioactive compounds, and pharmacological properties in both in-vitro and in-vivo settings, along with their mechanisms of action.

Efficiency of Recovery of the Bioactive Principles of Plants by Comparison between Solid-Liquid Extraction in Mixture and Single-Vegetable Matrices via Maceration and RSLDE.

The term "officinal" derives from the Latin and includes all medicinal, aromatic and perfume plant species, which have long been a subject of interest for multiple purposes: health, food, pharmacological, cosmetic and so on. In this work, a study on six different species of medicinal plants, particularly characterized by digestive, choleretic and diuretic properties, was carried out: rosemary (Rosmarinus officinalis), sage (Salvia officinalis), laurel (Laurus nobilis), gentian (Gentiana lutea), dandelion (Taraxacum officinale) and rhubarb (Rheum palmatum). The roots and aerial parts of plants were separately extracted with two different techniques-maceration and rapid solid-liquid dynamic extraction (RSLDE)-and the quali/quantitative analysis of active ingredients have been determined by applying dry residue, Folin-Ciocalteu and DPPH assays. Data obtained have provided useful answers regarding the efficiency of the extraction carried out on a mixture or on single plants, allowing us to evaluate the best choice according to the cases and the final uses.

Efficacy and Safety of Neem Oil for the Topical Treatment of Bloodsucking Lice Linognathus stenopsis in Goats under Field Conditions.

The aim of the present study was to evaluate the efficacy and safety of neem oil on caprine pediculosis and on kids' growth performances. The neem (Azadirachta indica) belongs to the Meliaceae family, and in Eastern countries it is mainly considered for the insecticidal activities of the kernel oil. The neem seeds contain bioactive principles, such as azadirachtin A, salannin, nimbin, and nimbolide. The trial was carried out on 24 kids, 120 days old, maintained in open yards. Animals were divided in 4 homogeneous groups (n = 6 animals/group) based on age, louse count, body condition score (BCS) and live body weight: Control Group (C, saline NaCl, 0.9%), Neem Group 1 (NO-100, 100 mL of neem oil per 10 kg), Neem Group 2 (NO-200, 200 mL/10 kg), Neem Group 3 (NO-300, 300 mL/10 kg). The treatments were performed by spraying the insecticide on the goat's body. The study lasted 56 days, and weekly, the kids underwent louse count, BCS and body weight determination, and FAMACHA score. Data were analyzed by ANOVA for repeated measures. The species of lice identified was Linognathus stenopsis. Kids belonging to NO-200 and NO-300 showed a stronger reduction of louse count throughout the study (>95%). The daily weight gain recorded was significantly higher (p < 0.05) in NO-300 than C. No differences were found for BCS and FAMACHA scores. The results of this trial showed that the administration of neem oil to control caprine pediculosis caused by sucking lice represents an alternative to synthetic compounds.

Therapeutic Role of Alkaloids and Alkaloid Derivatives in Cancer Management.

Cancer is a neoplastic disease that remains a global challenge with a reported prevalence that is increasing annually. Though existing drugs can be applied as single or combined therapies for managing this pathology, their concomitant adverse effects in human applications have led to the need to continually screen natural products for effective and alternative anticancer bioactive principles. Alkaloids are chemical molecules that, due to their structural diversity, constitute a reserve for the discovery of lead compounds with interesting pharmacological activities. Several in vitro studies and a few in vivo findings have documented various cytotoxic and antiproliferative properties of alkaloids. This review describes chaetocochin J, neopapillarine, coclaurine, reflexin A, 3,10-dibromofascaplysin and neferine, which belong to different alkaloid classes with antineoplastic properties and have been identified recently from plants. Despite their low solubility and bioavailability, plant-derived alkaloids have viable prospects as sources of viable lead antitumor agents. This potential can be achieved if more research on these chemical compounds is directed toward investigating ways of improving their delivery in an active form close to target cells, preferably with no effect on neighboring normal tissues.

Antineoplastic effects of cassava-cyanide extract on human glioblastoma (LN229) cells

Several natural compounds reduce tumour cell growth and metastasis by inducing programmed cell death. Cassava (Manihot esculenta Crantz) contains cyanogenic glycosides such as, linamarin and lotaustralin, can be enzymatically cleaved by linamarase to release hydrogen cyanide (HCN), which can have therapeutic benefits against hypertension, asthma, and cancer. We have developed a technology for isolating bio-active principles from cassava leaves.The present study is designed to analyze the cytotoxic effect of cassava cyanide extract (CCE) against human glioblastoma cells (LN229). The treatment of CCE demonstrated a dose dependent toxicity on glioblastoma cells. At higher concentration tested, the CCE (400 μg/mL) was found to be cytotoxic, reducing the cell viability to 14.07 ± 2.15% by negatively influencing the mitochondrial activity, and lysosomal and cytoskeletal integrity. Coomassie's brilliant blue staining confirmed cells' morphological aberration after 24 h of treatment with CCE. Moreover, DCFH-DA assay and Griess reagent showed an increase in ROS but a decrease in RNS production at a concentration of CCE. Flow cytometry analysis revealed that CCE interfered with G0/G1, S, and G2/M stages of the cell cycle of glioblastoma, and Annexin/PI staining indicated a dose-dependent increase in cell death, confirming the toxic nature of CCE on LN229 cells. These findings suggest that cassava cyanide extract has potential as an antineoplastic agent against glioblastoma cells, which is an aggressive and difficult-to-treat type of brain cancer. However, it is important to note that the study was conducted in vitro, and further research is necessary to assess the safety and efficacy of CCE in vivo. Additionally, it is essential to establish the optimal dose and potential side effects before considering its use as a therapeutic agent.

GC-MS profile and antimicrobial activities of extracts from root of Senna occidentalis Linn.

Abstract We considered the extraction of plant materials from Senna occidentalis root, and its fractionation monitored by bioassay towards isolating its bioactive principles. Pulverized root sample of Senna occidentalis (fam. leguminaceae) was extracted with methanol using a maceration method. The crude methanol extract (MSo) 6.06 g was partitioned into petroleum ether and ethyl acetate to yield their respective fractions viz: petroleum ether fraction (1.20 g), ethyl acetate fraction (1.86 g) and methanol fraction (2.92 g). The crude methanol extract was analyzed using phytochemical screening, infrared spectroscopy, and gas chromatography/mass spectrometry while the fractions were examined for antimicrobial properties. Phytochemical screening indicated the presence of tannins, phenolics, alkaloids, flavonoids, saponins, cardiac glycosides, phlobatannin, and absence of steroids. The infrared spectrum revealed a broad absorption band at 3437.26 cm-1 due to O-H symmetric stretch in polymeric alcohols, and absorption frequency of 1640.51cm-1 of moderate intensity due to C=O stretch. Enols are easily identified by the broad H-bonded O-H stretch absorption and low C=O stretch frequency as in β-keto enolic esters and phenol acetates, -CO-O-C=C-, (1690-1650 cm-1). Gas chromatography/mass spectrometry identified the presence of ten compounds including n-hexadecanoic acid (23.76%), linoleic acid (1.64%), E-9-tetradecenoic acid (4.88%), octadecanoic acid, 2-(2 hydroxyethoxy) ethyl ester (6.24%) and E-2-octadecadecen-1-ol (13.74%). Similar broad spectrum antimicrobial activities were manifested by methanol and ethyl acetate fractions. Escherichia coli and Bacillus cereus were the most susceptible with the highest zone of inhibition of 30 mm and 28 mm respectively at minimum inhibition concentration of 1.35 x103 μg/ml. The methanol fraction has the highest potency against the tested pathogens whereas the petroleum ether fraction exhibited activity only on gram negative pathogens. The antimicrobial activities observed in these fractions suggest the presence of active chemical components in the crude methanol root extract of Senna occidentalis thus provides a potential source of novel antimicrobial agents. Further work is however, required to isolate and characterize these bioactive principles.

Physicochemical Aspects, Bioactive Compounds, Phenolic Profile and In Vitro Antioxidant Activity of Tropical Red Fruits and Their Blend.

The combination of fruit pulps from different species, in addition to multiplying the offer of flavors, aromas and textures, favors the nutritional spectrum and the diversity of bioactive principles. The objective was to evaluate and compare the physicochemical characteristics, bioactive compounds, profile of phenolic compounds and in vitro antioxidant activity of pulps of three species of tropical red fruits (acerola, guava and pitanga) and of the blend produced from the combination. The pulps showed significant values of bioactive compounds, with emphasis on acerola, which had the highest levels in all parameters, except for lycopene, with the highest content in pitanga pulp. Nineteen phenolic compounds were identified, being phenolic acids, flavanols, anthocyanin and stilbene; of these, eighteen were quantified in acerola, nine in guava, twelve in pitanga and fourteen in the blend. The blend combined positive characteristics conferred by the individual pulps, with low pH favorable for conservation, high levels of total soluble solids and sugars, greater diversity of phenolic compounds and antioxidant activity close to that of acerola pulp. Pearson's correlation between antioxidant activity and ascorbic acid content, total phenolic compounds, flavonoids, anthocyanins and carotenoids for the samples were positive, indicating their use as a source of bioactive compounds.

Clematis Species: Phytochemicals and Pharmacological Effects- A Report

The genus Clematis has been a source of various traditionally useful and pharmacologically active species. Many plants of this genus are prominently climbers and woody vines. The species are mosly wild however; few are grown as ornamental plants. The species Clematis apifolia, Clematis ganpiniana, Clematis graveolens, and Clematis terniflora were selected to study on their traditional use, chemical composition and pharmacological effects reported in literature. In folklore these species are used as antispasmodic, carminative, diuretic, anodyne, antidote, diuretic and sedative agents. The triterpenoid saponins are the dominant compounds of these species flavonoids, alkaloids, lignans, coumarins, steroids and volatile oils have also been reported. The pharmacological effects evaluated are antioxidant, cytotoxic, antimicrobial, antidiabetic, hepatoprotectve, and anti-inflammatory activities. As such these species has emerged as good source of traditional medicines. The chemical compounds isolated from these species have been reported for their pharmacological effects. Although, few experimental studies validated their traditional claim, but uncharacterized crude extracts were employed in most of the activities. Such species need to be explored properly for their bioactive principle and exploited as potential drug. The review will help the researchers to select medicinally potential species of Clematis for future research.

Review on Butea monosperma Plant and Its Medicinal Use

Butea monosperma (Lam.) Kuntze (Syn. Butea frondosa; Family Fabaceae), This is a moderate sized deciduous tree which is widely distributed throughout India, Burma and Ceylon, popularly known as 'dhak' or 'palas', commonly known as ‘Flame of forest’. The family Fabaceae compromises of 630 genera and 18,000 species. The crude extracts of various parts and pure isolates of Butea monosperma was reported to possess antibacterial, antifungal, hypoglycemic, anti-inflammatory activities. Butea monosperma have been found to possess tonic, astringent, aphrodisiac and diuretics properties. The widespread uses of Butea monosperma in traditional systems of medicine have resulted in their extensive chemical analysis for their bio-active principles. This article briefly reviews the botany, chemistry and pharmacology of Butea monosperma (Lam) Kuntze. It is evident that without nature human being life is impossible. There are three basic necessity of humans is food, clothes and shelter and now the fourth one is good health, which provided by plant kingdom. Nature stands a golden mark and provided the storehouse of remedies to cure all ailments of mankind. Plant kingdom represents a rich house of organic compounds, many of which have been used for medicinal purposes and could serve as lead for the development of novel agents having good efficacy in various pathological disorders in the coming years. Herbs have always been the principal form of medicine in India and presently they are becoming popular throughout the world, as people strive to stay healthy in the face of chronic stress and pollution, and to treat illness with medicines that work in count with the body’s own defence.

Elettaria cardamomum leaves, an underutilized resource: chemical profile of its essential oil and insecticidal activity

ABSTRACT Elettaria cardamomum is known as the ‘Queen of spices’; its leaf essential oil (EO) is least investigated and barely utilized. Here we report the chemical composition of E. cardamomum leaf EOs collected from five locations in the southern Western Ghats in India. EOs of fresh and dry capsules were also analyzed for comparison of their chemical profiles. The major constituents in cardamom leaf EOs were β-pinene (35.6–51.9%) and coronarin E (17.7–34.2%). In fumigant toxicity assays against two stored product pests, lowest LC50 against Tribolium castaneum was recorded in EO of fresh capsules (124.05 µL/L), followed by dry capsules (LC50 128.21 µL/L) and leaves (LC50 148.00 µL/L); LC50s of fresh, dry capsule and leaf EOs against Sitophilus oryzae were 30.24, 35.33 and 89.42 µL/L, respectively. This study demonstrates cardamom leaves as a source of untapped bioactive principles which can be viably utilized for the production of botanical pesticides.

Detection and isolation of intestinal muscle relaxant substances from the root of Taverniera abyssinica A. Rich

Ethnopharmacological relevanceIn Ethiopian traditional medicine the root of Taverniera abyssinica A.Rich is known as a remedy for sudden gastrointestinal cramping and fever. In this study we have isolated and identified the bioactive principle of Taverniera abyssinica that exerts effects on isolated smooth muscle tissues of the rabbit duodenum and guinea-pig ileum. Aim of the studyTo isolate and purify the bioactive principle from the root of Taverniera abyssinica A.Rich by bioassay-guided fractionation, HPLC purification and masspectrometry, with further investigation of its bioactivity on isolated smooth muscle strips. Materials and methodsRoots of Taverniera abyssinica A.Rich extracted in 75% methanol/water were fractioned with a reverse phase column and then subjected to HPLC purification. Each fraction collected from the HPLC was tested for its bioactivity using electric field stimulation-evoked contractions of the rabbit duodenum and guinea-pig ileum. Finally, detailed structural analysis of the fraction displaying significant bioactivity was made by mass spectrometry. ResultsThrough bioassay-guided fractionation and HPLC purification the bioactive fractions were identified. These were tested for bioactivity on isolated smooth muscle strips which showed about 80% inhibition of contractions evoked by electric field stimulation. These compounds were identified as formononetin, afrormosin and tectorigenin by using masspectrometry applying relevant standards for detection. ConclusionThe traditionally claimed smooth muscle-relaxing effect of the roots of Taverniera abyssinica A.Rich is essentially due the three isolated and purified the two isoflavones formononetin, afrormosin as well as the metoxyisoflavone tectorigenin, along with possibly other not yet purified bioactive substances, however with similar smooth muscle-relaxing properties.

Isolation of Betulinic Acid from Byttneria herbacea (Malvaceae)

During the phytochemical analysis, flavonoids, saponins, tannins, glycosides, alkaloids, and terpenoids were identified in Byttneria herbacea (Malvaceae) among other things. The goal of this research is to identify and characterize the plant's bioactive principle. It has a wide range of folk medicinal applications. The gradient fractionation method was used to isolate and characterize phytoconstituents from ethanol extract. Physical, chemical, and spectroscopic data were used to determine the structure of the isolated substance (IR, UV, 1HNMR, MS). The ethanol extract of the plant yielded a triterpenoid structure. Various spectroscopical approaches were used to identify the odorless, colorless chemical that solubilizes in ethyl acetate and has a melting point of 315°C - 318°C and an Rf value of 0.62 in the mobile phase toluene: ethyl acetate (85:15). As a result of this research, the isolated component has been identified as Betulinic acid, which is accountable for the plant's diverse pharmacological properties.

Prenylated Flavonoids of Genus Epimedium: Phytochemistry, Estimation and Synthesis

AbstractPrenylated flavonoids are the chemotaxonomic markers of genus Epimedium. Icariin, epimedin A, B and C are the main bioactive principles found in Epimedium spp. The chemical and pharmacological studies of a good number of prenylated flavonoids isolated from Epimedium species are reported in literature but their biosynthetic pathways have been explored to a limited extent only and remained ambiguous for a long time. In this review, an in‐depth and extensive coverage of Epimedium prenylated flavonoids is reported from 2012 to 2022 using SciFinder database for literature retreival. The review covers occurrence, synthesis, biosynthesis and quantification of prenylated flavonoids of genus Epimedium.

Curative potential of high-value phytochemicals on COVID-19 infection

Medicinal plants and their therapeutically promising chemical compounds belonging to the valued category of ‘traditional medicine’ are potential remedies for various health problems. Due to their complex structure and enormous health benefits, the high-value plant-derived metabolites collectively termed as ‘phytochemicals’ have emerged as a crucial source for novel drug discovery and development. Indeed, several medicinal plants from diverse habitats are still in the ‘underexplored’ category in terms of their bioactive principles and therapeutic potential. COVID-19, infection caused by the SARS-CoV-2, first reported in November 2019, resulted in the alarming number of deaths (6.61 million), was further declared ‘pandemic’, and spread of the disease has continued till today. Even though the well-established scientific world has successfully implemented vaccines against COVID-19 within the short period of time, the focus on alternative remedies for long-term symptom management and immunity boosting have been increased. At this point, interventions based on traditional medicine, which include medicinal plants, their bioactive metabolites, extracts and formulations, attracted a lot of attention as alternative solutions for COVID-19 management. Here, we reviewed the recent research findings related to the effectiveness of phytochemicals in treatment or prevention of COVID-19. Furthermore, the literature regarding the mechanisms behind the preventive or therapeutic effects of these natural phytochemicals were also discussed. In conclusion, we suggest that the active plant-derived components could be used alone or in combination as an alternative solution for the management of SARS-CoV-2 infection. Moreover, the structure of these natural productomes may lead to the emergence of new prophylactic strategies for SARS-CoV-2-caused infection.

In vivo studies on evaluation of endophytic fungi extract from Trichoderma viride against cervical cancer

BackgroundThe crude ethyl acetate Trichoderma viride extract obtained from Ziziphus mauritiana was initially analyzed by HPLC for identification of major bioactive compounds, and then, it was subjected for in vivo acute and sub-acute toxicity, cervical cancer studies using Wistar albino rats.ResultDuring acute toxicity studies, animal groups treated with distinct dosage of 2000 mg/kg restrained toxicity signs in tested groups compared to controls for 14 days which established to be secure and non-toxic even at high dose. However, in terms of sub-acute toxicity studies, animals were given with repeated amount of (10 mg/kg, 20 mg/kg and 40 mg/kg) for a period of 28 days along with control group. Upon investigations of hematological, biochemical and histopathological studies repeated dose of 20 mg/kg and 40 mg/kg of T. viride extract found to be normal and no other major changes observed among treated groups. During in vivo studies, after treatment of T. viride extract (40 mg/kg) effectively inhibited the cervical cancer cell growth in DES-treated groups. Through HPLC analysis the major compound ursolic acid and 2,5-piperazinedione were mainly identified.ConclusionThe secondary metabolites of endophytes have been used substantially for the sustainable production of therapeutically important compounds. The limited availability of bioactive principles in plant sources could be surpassed by exploiting the chemical entities in the endophytes. In the present investigation, it has been accomplished that ethyl acetate extract of T. viride was safe at higher and lower dosage could be considered for pharmacological studies from plant may provide an excellent avenue for the discovery of drug candidates against deadly cancer diseases.

Ethnobotanical Survey, Physiochemical Composition and Preliminary Cytotoxic Evaluation of some Medicinal Plants with Anticancer Potential from Certain Areas in South-West Nigeria

Aims: Medicinal plants used by traditional medical practitioners (TMP) to treat cancers are considered safe when used alone or combined with conventional therapy to ensure their effectiveness and eliminate the toxic effects of orthodox medicines. Using cytotoxic and antioxidant studies, the study attempted to assess some of the commonly used medicinal plants used to cure cancer among Yoruba people in Ogun, Oyo, Osun, and Lagos (South-West, Nigeria).&#x0D; Study Design: Samples of commonly utilized anticancer plants obtained from the chosen areas using physical and virtual oral seminars were studied for physiochemical composition and a possible antioxidant and cytotoxic potential to validate the basis for the use of the selected anticancer plants.&#x0D; Methodology: Online academic literature searches were done on the cited plants to identify the already-exploited anticancer plants. The ethanolic extracts of the plant were examined for the presence of bioactive components and their total flavonoid content, with focusing on quercetin detection using thin layer bioautography (TLB) and brine shrimp lethality assay (BSLA) for cytotoxicity. In comparison to quercetin and ascorbic acid, the scavenging of superoxide radical (SOR), hydrogen peroxide, and 2, 2-Diphenyl-2-picrylhydrazyl (DPPH) radical activity by a model (most biologically active) of the anticancer plant was also evaluated.&#x0D; Results: There were only twelve anticancer species that were not used in related studies: Lannea egregia, Ficus exasperate, Croton zambesicus, Tetrapleurai tetraptera, Terminalia catappa, Zanthoxylum zanthoxyloides, Plumbago zelanica, Hilleria latifolia, Bryophyllum pinntum, Chromolena odorata, Brysocarpus coccineus and Spondias mombin. The anticancer plants contained bioactive and mineral substances like saponins, protein, lipids, magnesium, calcium, iron, zinc, and a decreased Na/K concentration. The plants had a fair amount of flavonoids and variable levels of cytotoxicity. L. egeregia was regarded as the prototype of the anticancer species due to its profound flavonoid concentration (85.40 µg/mL) and cytotoxicity (9.46 µg/mL) compared to other extracts. The TLB also demonstrated the presence of quercetin, with a dose-dependent antioxidant property. The anticancer model's overall antioxidant activity (34.72 µg/mL) was slightly lower than quercetin (30.44 µg/mL) but higher than ascorbic acid (41.68 µg/mL).&#x0D; Conclusion: The results support the traditional use of anticancer species as nutritional and dietary supplements, whose bioactive compounds are relevant in managing cancer patients. The plant’s bioactive principles need to be characterized in future research.

Metabolite profiling, in vitro and in silico assessment of antibacterial and anticancer activities of Alternaria alternata endophytic in Jatropha heynei.

Fungal endophytes produce a range of structurally diverse metabolites with bioactive principles. In this study, an endophytic fungus Alternaria alternata was isolated from Jatropha heynei and cultured in potato dextrose liquid broth. Culture filtrate of A. alternata was extracted in ethyl acetate and metabolites were characterized by QTOF-HRLCMS. Among compounds detected, spectral compounds such as kigelinone, and levofuraltadone were reported with antibacterial property, while 2-hydroxychrasophanol, isoathyriol, glycophymoline, columbianetin and kaempferol 3-O-β-D- galactoside were reported with cytotoxic properties. Partially purified metabolites of A. alternata showed significant antibacterial activity against tested clinical bacterial strains by agar well diffusion method. High zone of inhibition was recorded against Enterococcus faecalis, Pseudomonas syringae and Klebsiella pneumoniae. In vitro anticancer activity of fungal extract by MTT assay displayed high cytotoxic effect on human lung carcinoma cancer cell line (A549) with IC50 value of 393.52µgml-1, and without any significant cytotoxic effect on human breast cancer cell line (MCF-7). Further, antibacterial and anticancer spectral compounds of A. alternata were subjected to molecular docking analysis with antibacterial target proteins such as tellurite resistance protein (2JXU), indole-3-acetaldehyde dehydrogenase (5IUU) and alkyl hydroperoxide reductase (5Y63), and anticancer target human apoptotic regulator protein (1G5M). The results of the study indicated that kigelinone, levofuraltadone, 2-hydroxychrasophanol and isoathyriolin the fungal extract have significant binding modes, with best binding energy scores with their respective antibacterial and anticancer target proteins. Alternaria alternata resident in J. heynei offers a promising source of broad-spectrum antibacterial and anticancer compounds.

Feature-Based Molecular Networking for the Exploration of the Metabolome Diversity of Common Egyptian Centaurea Species in Relation to Their Cytotoxic Activity

Centaurea is a genus compromising over 250 herbaceous flowering species and is used traditionally to treat several ailments. Among the Egyptian Centaurea species, C. lipii was reported to be cytotoxic against multidrug-resistant cancer cells. In this context, we aimed to explore the metabolome of C. lipii and compare it to other members of the genus in pursuance of identifying its bioactive principles. An LC-MS/MS analysis approach synchronized with feature-based molecular networks was adopted to offer a holistic overview of the metabolome diversity of the Egyptian Centaurea species. The studied plants included C. alexandrina, C. calcitrapa, C. eryngioides, C. glomerata, C. lipii, C. pallescens, C. pumilio, and C. scoparia. Their constitutive metabolome showed diverse chemical classes such as cinnamic acids, sesquiterpene lactones, flavonoids, and lignans. Linking the recorded metabolome to the previously reported cytotoxicity identified sesquiterpene lactones as the major contributors to this activity. To confirm our findings, bioassay-guided fractionation of C. lipii was adopted and led to the isolation of the sesquiterpene lactone cynaropicrin with an IC50 of 1.817 µM against the CCRF-CEM leukemia cell line. The adopted methodology highlighted the uniqueness of the constitutive metabolome of C. lipii and determined the sesquiterpene lactones to be the responsible cytotoxic metabolites.

Chemical Constituents and Bioactive Principles from the Mexican Truffle and Fermented Products of the Derived Fungus Ustilago maydis MZ496986.

To look in-depth into the traditional Mexican truffle, this study investigated the phytochemical and pharmacological properties of field-collected corn galls and the fermentate of its pathogen Ustilago maydis MZ496986. Here, we established the chemical profiles of both materials via the gradient HPLC-UV method and successfully identified six previously unreported chemical entities, ustilagols A-F (1-6), and 17 known components. Compounds 3, 5, and 9 exhibited potent nitric oxide production inhibitory activities in murine brain microglial BV-2 cells (IC50 = 6.7 ± 0.5, 5.8 ± 0.9, and 3.9 ± 0.1 μM) without cytotoxic effects. DIMBOA (9) also attenuates lipopolysaccharide (LPS)-stimulated NF-κB activation in RAW 264.7 macrophages (IC50 = 58.1 ± 7.2 μM). Ustilagol G (7) showed potent antiplatelet aggregation in U46619-stimulated human platelets (IC50 = 16.5 ± 5.3 μM). These findings highlighted the potential of corn galls and U. maydis MZ496986 fermentate as functional foods for improving inflammation-related discomforts and vascular obstruction.