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A new peroxy fatty acid, tagetnoic acid (5) [4-((3S,6S)-6-((3E,8E)- octadeca-3,8-dien-1-yl)-3,6-dihydro-1,2-dioxin-3-yl)butanoic acid] and four known metabolites: ecliptal (5-formyl-a-terthiophene) (1), 5-(4-hydroxybut-1-ynyl)-2,20-bithiophene (2), 22,23-dihydrospinasterone (3), and stigmasterol (4) were separated from the n-hexane fraction of the aerial parts of Tagetes minuta L. (Asteraceae). Their chemical structures were verified using IR, UV, 2D and 1D NMR, and HRMS. Compounds 3-5 displayed potent lipoxygenase inhibitory potential with IC50s 2.26, 1.83, and 1.17 lM, respectively compared to indomethacin (IC50 0.89 lM). Moreover, molecular docking study revealed that the potent activity of 5 is due to H-bonding and hydrophobic interaction. The results of this study suggested that Tagetes minuta dietary consumption would be useful for the individuals at risk of acute and chronic inflammatory disorders. [ABSTRACT FROM AUTHOR]

Phytochemical investigation of the methanolic extract of Cucumis melo L. (Cucurbitaceae) seeds furnished a new triterpene benzoate derivative: cucumol B (1) and four known flavonoids: quercetin-3-O-β-D-glucopyranosyl-(1→6)-α-L-rhamnopyranoside (2), quercetin-3-O-β-D-glucopyranoside (3), quercetin (4), and luteolin (5). Their structures were identified by UV, IR, 1D (13C and 1H), 2D (HSQC, 1H-1H COSY, HMBC, and NOESY) NMR, and HRESIMS spectral as well as comparing with literature data. Compound 1 has been assessed for the in vitro cytotoxic effect against SKOV-3, MCF-7, and HCT-116 cell lines. It had selective and potent effect toward SKOV-3 and MCF-7 cell lines with IC50s 2.05 and 0.41 μM, respectively, in comparison to doxorubicin (IC50s 0.32 and 0.05 μM). However, it showed moderate activity toward HCT-116 cell line with IC50 8.27 μM. [ABSTRACT FROM AUTHOR]

A new prenylated xanthone, garcixanthone A (5), together with eight known compounds, mangostanaxanthones I (1) and II (2), garcinone E (3), β-mangostin (4), 8-hydroxycudraxanthone G (6), garcinone C (7), cudraxanthone G (8), and (-)-epicatechin (9) were isolated from the EtOAc-soluble fraction of the air-dried pericarps of Garcinia mangostana (family Clusiaceae). Their structures were verified on the basis of spectroscopic data interpretation as well as comparison with the literature. The cytotoxic and antimicrobial activities of the new compound were assessed using sulforhodamine B (SRB) and agar disk diffusion assays, respectively. Compound 5 showed significant cytotoxic potential against epithelial lung carcinoma (A549) and breast carcinoma (MCF7) cell lines with IC50s 3.0 and 4.2 μM, respectively, compared to doxorubicin (0.74 and 0.41 μM, respectively). [ABSTRACT FROM AUTHOR]

Background: Endophytic fungi attracted attention as a prolific source of bioactive natural products with a potent pharmaceutical activity and unique structure. Objective: The main goal of the study is to separate and identify the bioactive constituents from the endophytic fungus Fusarium sp. as well as to evaluate the antimicrobial of the new metabolites. Materials and Methods: The fungus was cultured on a rice medium, and then, the cultures were extracted with ethyl acetate (EtOAc). The EtOAc extract was chromatographed utilizing different chromatographic methods to give five metabolites. The structural determination of these metabolites was carried out by the analyses of various spectroscopic data, in addition to comparison with the formerly reported data. The antifungal and antibacterial potentials were evaluated toward various microbial strains using disc diffusion assay. Results: A new aminobenzamide derivative, namely fusaribenzamide A (2), and four known metabolites: (22E,24R)- stigmasta-5,7,22-trien-3-β-ol (1), adenosine (3), p-hydroxyacetophenone (4), and tyrosol (5) were isolated. Fusaribenzamide A (2) possessed significant antifungal activity toward Candida albicans with minimum inhibitory concentration (MIC) value 11.9 μg/disc compared to nystatin (MIC 4.9 μg/disc). Conclusion: The endophytic fungus Fusarium sp. could be considered as a wealthy pool for the isolation of aminobenzamide derivatives. Fusaribenzamide A may be a candidate for the discovery of a promising antifungal agent. [ABSTRACT FROM AUTHOR]

Background: Endophytic fungi are of a growing interest as prominent sources of structurally unique bioactive natural products. Objective: This study aims to isolate and characterize bio-metabolites from the endophytic fungus Fusarium sp. isolated from Mentha longifolia L. roots as well as to assess the antimicrobial and cytotoxic potential of these metabolites. Materials and Methods: The endophytic fungi Fusarium sp. was cultured on a rice medium. The rice cultures' ethyl acetate extract was separated using various chromatographic techniques (SiO2, RP-18, and sephadex LH-20) to afford four metabolites. Their structural characterization was achieved by various spectroscopic analyses, as well as comparing with the published data. Results: A new ergosterol derivative namely, fusaristerol A (22E,24R-5β,8β-epidioxyergosta-22-en-3β-yl decanoate) (1), along with ergosta-7,22-diene-3β,5α,6β-triol (2), ergosta-5,7,22-triene-3β-ol (3), and (22E,24R)-ergosta-7,22-dien-3β-ol (4), was separated. Fusaristerol A (1) possessed a significant antifungal activity toward Candida albicans with minimum inhibitory concentration (MIC) value of 8.3 μg/disc compared to clotrimazole (MIC 5.1 μg/disc). Moreover, it displayed a potent cytotoxic potential toward HCT-116 cell line with an half maximal inhibitory concentration (IC50) value of 0.21 μM, compared to doxorubicin (IC50 0.06 μM). Conclusion: This is the first report for separation of a 5,8-epidioxy ergostane derivative from Fusarium sp. Fusaristerol A may provide a new promising candidate for the development of a potential anti-candida and cytotoxic agent. Abbreviations used: BT-549: Ductal carcinoma; CC: Column chromatography; COSY: Correlations spectroscopy; CDCl3: Deuterated chloroform; EtOAc: Ethyl acetate; DMSO: Dimethyl sulfoxide; EIMS; Electron-impact mass spectrometry; EP: Ergosterol peroxide; GCMS; Gas chromatography mass spectrometry; HCl: Hydrochloric acid; H2O: Water; H2SO4: Sulfuric acid; HMBC: Heteronuclear multiple bond correlation experiment; HRMS: High-resolution mass spectrometry; HRESIMS: High-resolution electrospray ionization mass spectrometry; HCT-116: Colorectal adenocarcinoma; HSQC: Heteronuclear single-quantum correlation; IC50: Half maximal inhibitory concentration; IR: Infrared; KBr: Potassium bromide; KOH; Potassium hydroxide; LTQ: Linear trap quadruple; MeOH; Methanol; MIC: Minimum inhibitory concentration; MCF-7: Human breast adenocarcinoma; NMR: Nuclear magnetic resonance; PDA: Potato dextrose agar; RP: Reversed phase; SiO2: Silica gel; TLC: Thin-layer chromatography; VLC: Vacuum liquid chromatography. [ABSTRACT FROM AUTHOR]

Abstract: The genus Hylocereus (family Cactaceae) includes about 16 species. Now its reputation is spreading everywhere in the world due to its fruit (pitaya or pitahaya or dragon fruit), which is one of the most popular and widely used functional foods in the world. The fruit is a wealthy provenance of vitamins, minerals, antioxidants, and fiber. The ethno‐pharmacological history of this genus indicated that it possesses antioxidant, anticancer, antimicrobial, hepato‐protective, antihyperlipidemic, antidiabetic, and wound healing activities. Furthermore, it has been used for the treatment of cough, asthma, hyperactivity, tuberculosis, bronchitis, mumps, diabetes, and cervical lymph node tuberculosis. Different chemical constituents have been reported from this genus as betalains, flavonoids, phenolic acids, phenylpropanoids, triterpenes, sterols, fatty acids, etc. The current review focuses on the uses, botanical characterization, chemical constituents, nutritional importance, biological activities, and safety of Hylocereus species. Also, biosynthetic pathways of betalains have been discussed. Practical applications: Pitaya fruit is one of the most known fruit that is commercially grown in different countries of the world for its nutritional advantages. It has acquired a wide acceptance for its pharmacological actions against a variety of ailments. The present review revealed that pitaya contains various bioactive phytoconstituents which might participate directly or indirectly in their highlighted biological effects. Therefore, these compounds can be taken into account as favorable candidates for the development of effective and novel pharmaceutical leads. Deep phytochemical studies of pitaya fruit and its pharmacological effects, especially the mechanism of action of its constituents to clarify the relation between traditional uses and pharmacological activities will obviously be the focus of further research. [ABSTRACT FROM AUTHOR]

Background: The coronavirus disease 2019 (COVID-19) is a novel coronavirus that causes severe infection in the respiratory system. Since the immune status plays an essential role in combating COVID-19, herbal medicines, which have an immunomodulatory effect, may help prevent and even treat COVID-19. Nigella is one of the herbal medicines with antiviral and immunomodulatory activities, and its therapeutic effectiveness makes it a promising add-on therapy for COVID-19. In addition, vitamin D3 has an immunomodulatory role, but the effect of therapeutic vitamin D3 supplementation in SARS-CoV-2 infection is still not well-known. sativa is one of the herbal medicines with antiviral and immunomodulatory activities, and its therapeutic effectiveness makes it a promising add-on therapy for COVID-19. In addition, vitamin D3 has an immunomodulatory role, but the effect of therapeutic vitamin D3 supplementation in SARS-CoV-2 infection is still not well-known. Objective: and vitamin D3 as single supplemental therapies and in combination on viral clearance indicated by a negative polymerase chain reaction and the alleviation of symptoms during the study follow-up duration of 14 days. Nigella sativa The study design was an open-label randomized controlled clinical trial conducted at the Respiratory Hospital at the Kobry El Qobba Armed Forces Medical Complex. In total, 120 COVID-19 patients with mild to moderate symptoms were randomly assigned to four groups, with thirty patients each, as follows: Group 1 received an oral dose of 900 mg Patients and Methods: The study design was an open-label randomized controlled clinical trial conducted at the Respiratory Hospital at the Kobry El Qobba Armed Forces Medical Complex. In total, 120 COVID-19 patients with mild to moderate symptoms were randomly assigned to four groups, with thirty patients each, as follows: Group 1 received an oral dose of 900 mg Nigella sativa through 450 mg soft gelatin capsules twice daily for two weeks; Group 2 received 2,000 IU of vitamin D3 through 1000-IU tablets given as two tablets, once daily; Group 3 received 900 mg of Nigella sativa and 2,000 IU of vitamin D3 in the same manner of dosing as in the previous groups; and Group 4 was the control group. All groups received standard therapy for COVID-19 infections and clinical management of COVID-19's clinical symptoms. Results: -vitamin D3 combination in addition to the standard therapy for COVID-19 infections significantly contributed to the alleviation of most COVID-19 symptoms: 50% of patients were free of cough after 7 days, 70% showed an absence of fatigue after 4 days, 80% had no headache after 5 days, 90% were free of rhinorrhea after 7 days, and 86.7% of the patients had no dyspnea after 7 days. Moreover, patients in the four studied groups showed a reduced median temperature after 3 days of treatment. Negative results of the polymerase chain reaction (PCR) test recorded on the 7th and 14th day of therapy were superior in the Nigella sativa -vitamin D3 combination in addition to the standard therapy for COVID-19 infections significantly contributed to the alleviation of most COVID-19 symptoms: 50% of patients were free of cough after 7 days, 70% showed an absence of fatigue after 4 days, 80% had no headache after 5 days, 90% were free of rhinorrhea after 7 days, and 86.7% of the patients had no dyspnea after 7 days. Moreover, patients in the four studied groups showed a reduced median temperature after 3 days of treatment. Negative results of the polymerase chain reaction (PCR) test recorded on the 7th and 14th day of therapy were superior in the Nigella sativa The results of this study showed a promising therapeutic benefit of the administration of Conclusion: and vitamin D3 combination in COVID-19 patients with mild to moderate symptoms. Additionally, the remarkable viral clearance in a short time interval and reduction in the severity and progression of symptoms recommended the use of this combination as an add-on therapy for the management of COVID-19 patients. Nigella sativa and vitamin D3 combination in COVID-19 patients with mild to moderate symptoms. Additionally, the remarkable viral clearance in a short time interval and reduction in the severity and progression of symptoms recommended the use of this combination as an add-on therapy for the management of COVID-19 patients. Clinical Trial Registration: ClinicalTrials.gov, Identifier: NCT04981743., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2022 Said, Abdulbaset, El-Kholy, Besckales and Sabri.)

Malaria is one of the major infectious diseases and foremost cause of mortality and morbidity in many subtropical and tropical regions. In the last years, the situation has become worst in many ways, due to increase in the parasites resistance to various available antimalarial agents. Furthermore, malaria`s control is beginning to be more sophisticated by the parallel spread of mosquito vector`s resistance to the available insecticides. Recently, there is a wide consensus to seek for target specific, safe, affordable, and effective new antimalarial agents, which can compete with synthetic ones. Endophytic fungi are of a growing interest as prominent sources of structurally unique bioactive natural products. The bio-metabolites isolated from endophytic fungi, possessing antimalarial potential may compose the base for the synthesis of novel drugs that might be utilized to withstand malaria and its resistance. For getting information on the various studies, PubMed, Google Scholar, ScienceDirect, SpringerLink, Scopus, and Wiley search was done using keywords (malaria, endophytic fungi, and antimalarial activity). The present review covers the literature published from 1996 to 2017 and highlights the metabolites for which antimalarial activities have been reported. Overall, 135 fungal metabolites and 72 references are cited. In addition, their structure, chemical class, fungal source, host, and activity have been presented. This review shows the significance of endophytic fungi as a wealthy pool of antimalarial agents., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)