Perylenequinones (PQs) are aromatic polyketides with an oxidized pentacyclic core that make up a family of natural compounds. Naturally occurring PQs mostly are produced by phytopathogenic fungi, ...with few aphides, crinoids, and plants. PQs, also known as photosensitizers, absorb light energy which empowers them to produce reactive oxygen species that damage host cells. Therefore, PQs gained a considerable interest in pharmaceutical application notably in photodynamic therapy. This review presents a comprehensive overview of fungal PQs. Their occurrence, categorization, biosynthesis, structures, and bioactivities are all discussed in detail. After that, an analysis outlines their distribution across the kingdom of fungi. A total of 66 fungal PQs have been described from 22 ascomycete genera (
Alternaria, Aspergillus
,
Bulgaria
,
Cenococcum
,
Cercospora
,
Cladosporium
,
Curvularia
,
Daldinia
,
Elsinoë
,
Hypocrella
,
Hypomyces
,
Parastagonospora
,
Phaeosphaeria
,
Phylacia
,
Pyrenochaeta
,
Rhopalostroma
,
Rubroshiraia, Setophoma, Shiraia
,
Stemphylium
,
Stagonospora
, and
Thamnomyces
).
Dothideomycetes
account for the majority of documented fungal PQs (82%), followed by
Sordariomycetes
(14%),
Leotiomycetes
(3%), and
Eurotiomycetes
(1%). Herein, five families
Pleosporaceae
,
Phaeosphaeriaceae
,
Cladosporiaceae
,
Shiraiaceae
, and
Hypoxylaceae
are highlighted as potential sources of novel PQs due to their diversity. The review intends to pique bioprospectors’ interest in fungal PQs. Indeed, the pharmaceutical and agrochemical industries might gain greatly by exploiting fungal perylenequinones.
Graphical abstract
(Roem. & Schult.) K. Schum (family Asclepiadaceae) is a creeping woody climber used to treat ailments in many traditional medicine systems. The present study aims to examine the antioxidant and ...enzyme inhibition activities of
leaf using different compositions of methanol-water mixture as an extraction solvent. The extracts were characterized by HPLC-ESI-MS
in terms of chemical compounds. The in silico results show that compound
(quercitrin) has the higher docking scores among the selected substances and the MD simulation revealed that the interactions with the enzymatic pocket are stable over the simulation time and strongly involve the tyrosinase catalytic Cu atoms. All together the results showed that both 80% and 100% methanolic extracts contained significantly (
< 0.05) the highest total phenolics content while the highest content of total flavonoids was significantly (
< 0.05) extracted by 100% methanol. About 26 compounds were tentatively identified by HPLC-ESI-MS
and 6 of them were quantified using standards. Results showed that the extracts were rich in flavonoids with a relatively high abundance of two kaempferol glycosides comprising 60% of quantified compounds. The 100% and 80% methanol extracts recorded significantly (
< 0.05) the highest total antioxidant, DPPH and ABTS activity as well as tyrosinase and ⍺-amylase inhibitory activities. The best significant (
< 0.05) cholinesterase inhibitory activity and reducing capacity of Fe
and Cu
was recorded from the 80% methanolic extract while 100% ethanolic extract gave the highest significant (
< 0.05) butyrylcholinesterase inhibitory activity. The best glucosidase activity was observed in the 50% and 80% methanolic extracts. Although the water extract displayed the least total phenolics and flavonoids content and consequently the lowest antioxidant and enzyme inhibition activity, it displayed significantly (
< 0.05) the highest chelating power. In conclusion, these results demonstrated the richness of
leaf as a potential source of bioactive compounds for the food industry, for the preparation of food supplements and functional foods.
Several species within the genera Cassia or Senna have a treasure of traditional medicines worldwide and can be a promising source of bioactive molecules. The objective of the present study was to ...evaluate the phenolic content and antioxidant and enzyme inhibition activities of leaf methanolic extracts of C. fistula L., C. grandis L., S. alexandrina Mill., and S. italica Mill. The two Cassia spp. contained higher total polyphenolic content (42.23–49.75 mg GAE/g) than the two Senna spp., and C. fistula had significantly (p ˂ 0.05) the highest concentration. On the other hand, the Senna spp. showed higher total flavonoid content (41.47–59.24 mg rutin equivalent per g of extract) than that found in the two Cassia spp., and S. alexandrina significantly (p ˂ 0.05) accumulated the highest amount. HPLC–MS/MS analysis of 38 selected bioactive compounds showed that the majority of compounds were identified in the four species, but with sharp variations in their concentrations. C. fistula was dominated by epicatechin (8928.75 µg/g), C. grandis by kaempferol-3-glucoside (47,360.04 µg/g), while rutin was the major compound in S. italica (17,285.02 µg/g) and S. alexandrina (6381.85). The methanolic extracts of the two Cassia species exerted significantly (p ˂ 0.05) higher antiradical activity, metal reducing capacity, and total antioxidant activity than that recorded from the two Senna species’ methanolic extracts, and C. fistula displayed significantly (p ˂ 0.05) the highest values. C. grandis significantly (p ˂ 0.05) exhibited the highest metal chelating power. The results of the enzyme inhibition activity showed that the four species possessed anti-AChE activity, and the highest value, but not significantly (p ≥ 0.05) different from those obtained by the two Cassia spp., was exerted by S. alexandrina. The Cassia spp. exhibited significantly (p ˂ 0.05) higher anti-BChE and anti-Tyr properties than the Senna spp., and C. grandise revealed significantly (p ˂ 0.05) the highest values. C. grandise revealed significantly (p ˂ 0.05) the highest α- amylase inhibition, while the four species had more or less the same effect against the α-glucosidase enzyme. Multivariate analysis and in silico studies showed that many of the identified phenols may play key roles as antioxidant and enzyme inhibitory properties. Thus, these Cassia and Senna species could be a promising source of natural bioactive agents with beneficial effects for human health.
The inhabitants of western Sudan use traditional medicine for the treatment of various ailments due to lack of medical doctors and unaffordable prices of pharmaceutical products. The present study is ...the first documentation of the traditional plant knowledge on medicinal uses of plants by healers in Algoz (South Kordofan), Sudan.
Ethnobotanical data were collected over a period from March to November 2015 using semi-structured interviews with 30 healers (24 male and 6 female) living in the investigated area. Quantitative indices such as use categories, use value (UV) and informant consensus factor (ICF) were intended to evaluate the importance of medicinal plant species.
A total of 94 medicinal plants, which belong to 45 families and 81 genera, were recorded in the study area. The most represented families are Leguminosae with 20 species followed by Combretaceae (6 species), Rubiaceae (5 species) and Asteraceae (4 species). The reported species were belonging to herbs (43%), trees (28%), shrubs (22%), climbers (4%) and parasites (3%). Root and stem (21% each) were the most plant parts used. A majority of remedies are administered orally (67%) where infusion (36%) and maceration (32%) are the most used methods. The highest ICF (0.87) was reported for poisonous animal bites followed by urinary system diseases (0.89), blood system disorders (0.88) and gynaecological diseases (0.87). Anastatica hierochuntica, Ctenolepis cerasiformis, Echinops longifolius, Cleome gynandra, Maerua pseudopetalosa, Martynia annua, Oldenlandia uniflora, Opuntia ficus-indica, Solanum dubium, Sonchus cornutus, Tribulus terrestris and Drimia maritima were reported for the first time in this study.
The number of medicinal plants reported in this paper reflects evidence that Algoz area had a high diversity of medicinal plants which will continue to play an important role in the healthcare system in the study area.
Cucurbitacin E (CuE) is an oxygenated tetracyclic triterpenoid isolated from the fruits of Citrullus colocynthis (L.) Schrad.
This study outlines CuE's cytotoxic activity against drug-resistant tumor ...cell lines. Three members of ABC transporters superfamily, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and ABCB5 were investigated, whose overexpression in tumors is tightly linked to multidrug resistance. Further factors of drug resistance studied were the tumor suppressor TP53 and the epidermal growth factor receptor (EGFR).
Cytotoxicity assays (resazurin assays) were used to investigate the activity of Citrullus colocynthis and CuE towards multidrug resistant cancer cells. Molecular docking (In silico) has been carried out to explore the CuE's mode of binding to ABC transporters (P-gp, BCRP and ABCB5). The visualization of doxorubicin uptake was done by a Spinning Disc Confocal Microscope. The assessment of proteins expression was done by western blotting analysis. COMPARE and hierarchical cluster analyses were applied to identify, which genes correlate with sensitivity or resistance to cucurbitacins (CuA, CuB, CuE, CuD, CuI, and CuK).
Multidrug-resistant cells overexpressing P-gp or BCRP were cross-resistant to CuE. By contrast, TP53 knock-out cells were sensitive to CuE. Remarkably, resistant cells transfected with oncogenic ΔEGFR or ABCB5 were hypersensitive (collateral sensitive) to CuE. In silico analyses demonstrated that CuE is a substrate for P-gp and BCRP. Immunoblot analyses highlighted that CuE targeted EGFR and silenced its downstream signaling cascades. The most striking result that emerged from the doxorubicin uptake by ABCB5 overexpressing cells is that CuE is an effective inhibitor for ABCB5 transporter when compared with verapamil. The COMPARE analyses of transcriptome-wide expression profiles of tumor cell lines of the NCI identified common genes involved in cell cycle regulation, cellular adhesion and intracellular communication for different cucurbitacins.
CuE represents a potential therapeutic candidate for the treatment of certain types of refractory tumors. To best of our knowledge, this is the first time to identify CuE and verapamil as inhibitors for ABCB5 transporter.
Display omitted
Soil microorganisms play crucial roles in soil fertility, e.g., through decomposing organic matter, cycling nutrients or through beneficial interactions with plants. Actinomycetes are a major ...component of soil inhabitants; they are prolific producers of specialized metabolites, among which many antibiotics. Here we report the isolation and characterization of 175 Actinomycetes from rhizosphere and bulk soil samples collected in 18 locations in Sudan. We evaluated the strains’ metabolic potential for plant protection by testing their ability to inhibit the mycelial growth of the oomycete
Phytophthora infestans
, which is one of the most devastating plant pathogens worldwide. Most strains significantly reduced the oomycete’s growth in direct confrontational
in vitro
assays. A significant proportion of the tested strains (15%) were able to inhibit
P. infestans
to more than 80%, 23% to 50%–80%, while the remaining 62% had inhibition percentages lesser than 50%. Different morphologies of
P. infestans
mycelial growth and sporangia formation were observed upon co-inoculation with some of the Actinomycetes isolates, such as the production of fewer, thinner hyphae without sporangia leading to a faint growth morphology, or on the contrary, of clusters of thick-walled hyphae leading to a bushy, or “frozen” morphology. These morphologies were caused by strains differing in activity levels but phylogenetically closely related with each other. To evaluate whether the isolated Actinomycetes could also inhibit the pathogen’s growth
in planta,
the most active strains were tested for their ability to restrict disease progress in leaf disc and full plant assays. Five of the active strains showed highly significant protection of potato leaves against the pathogen in leaf disc assays, as well as substantial reduction of disease progress in full plants assays. Using cell-free filtrates instead of the bacterial spores also led to full protection against disease on leaf discs, which highlights the strong crop protective potential of the secreted metabolites that could be applied as leaf spray. This study demonstrates the strong anti-oomycete activity of soil- and rhizosphere-borne Actinomycetes and highlights their significant potential for the development of sustainable solutions based on either cell suspensions or cell-free filtrates to safeguard potatoes from their most damaging pathogen.
Patients suffering from inflammatory chronic diseases are classically treated with anti-inflammatory drugs but unfortunately are highly susceptible to becoming resistant to their treatment. Finding ...new drugs is therefore crucial and urgent and research on endophytic fungi is a promising way forward. Endophytic fungi are microorganisms that colonize healthy plants and live within their intercellular tissues. They are able to produce a large variety of secondary metabolites while allowing their host to stay healthy. A number of these molecules are endowed with antioxidant or antimicrobial as well as cytotoxic properties, making them very interesting/promising in the field of human therapy. The aim of our study was to investigate whether extracts from five endophytic fungi isolated from plants are endowed with anti-inflammatory activity. Extracts of the endophytic fungi Alternaria alternata from Calotropis procera leaves and Aspergillus terreus from Trigonella foenum-graecum seeds were able to counteract the lipopolysaccharide (LPS) pro-inflammatory effect on THP-1 cells differentiated into macrophages. Moreover, they were able to induce an anti-inflammatory state, rendering them less sensitive to the LPS pro-inflammatory stimulus. Taken together, these results show that these both endophytic fungi could be interesting alternatives to conventional anti-inflammatory drugs. To gain more detailed knowledge of their chemical richness, phytochemical analysis of the ethyl acetate extracts of the five endophytic fungi studied was performed using HPTLC, GC-MS and LC-MS with the Global Natural Products Social (GNPS) platform and the MolNetEnhancer tool. A large family of metabolites (carboxylic acids and derivatives, steroid derivatives, alkaloids, hydroxyanthraquinones, valerolactones and perylenequinones) were detected. The purification of endophytic fungus extract of Alternaria alternate, which diminished TNF-α production of 66% at 20 µg/mL, incubated one hour before LPS addition, led to the characterization of eight pure compounds. These molecules are altertoxins I, II, III, tricycloalternarenes 3a, 1b, 2b, anthranilic acid, and o-acetamidobenzoic acid. In the future, all these pure compounds will be evaluated for their anti-inflammatory activity, while altertoxin II has been shown in the literature as the most active mycotoxin in terms of anti-inflammatory activity.
The documentation of ethnobotanical knowledge in Sudan is restricted to specific regions, and there is a far-reaching lack of written information on the traditional use of medicinal plants in other ...places like Darfur State, in western Sudan. The present study was designed to document the medicinal plants used in traditional medicine of Melit area in North Darfur State.
Ethnomedicinal information was collected from 135 local informants through semi-structured questionnaires. Data were analysed for use value (UV), informant consensus factor (ICF) and fidelity level.
A total of 59 medicinal plants, belonging to 32 families and 55 genera, were recorded for their traditional uses in Melit area. Fabaceae were represented by highest number of species (13) followed by Asteraceae and Malvaceae (4 each) and Poaceae (3). Herbs comprise the main sources (50.8%) of traditional remedies. Fruits and stem bark (17.9% each) were the major plant parts used. Decoction (36.5%) is the most mode of preparation used. Geigeria alata was most commonly used species with UV of 2.37. The highest ICF values were recorded for swellings (ICF = 1.00) and respiratory system (ICF = 0.95) categories. Ten plants, namely Carica papaya, Corchorus trilocularis, Eragrostis cilianensis, Heliotropium sudanicum, Mollugo cerviana, Psiadia punctulate, Rhynchosia minima, Solanum coagulans, Solanum forskalii and Tephrosia purpurea, were cited for the first time as medicinal plants used in Sudan traditional medicine. Resins of Boswellia papyrifera, seeds of Nigella sativa, pods of Vachellia nilotica (syn. Acacia nilotica) and clove of Syzygium aromticum were used to make different preparations for the treatment of the corona virus.
This is the first ethnobotanical survey conducted in this region which is always suffering from security issues, and results indicated that Melit area harbours high diversity of plants used traditionally to cure different health conditions. The present study aids in conserving such rich heritage, and it is recommended that the newly reported species worth further studying over their phytochemical and biological properties.
This study was aimed to perform the mechanistic investigations of chalcone scaffold as inhibitors of acetylcholinesterase (AChE) enzyme using molecular docking and molecular dynamics simulation ...tools. Basic chalcones (
-
) were synthesized and their in vitro AChE inhibition was tested. Binding interactions were studied using AutoDock and Surflex-Dock programs, whereas the molecular dynamics simulation studies were performed to check the stability of the ligand-protein complex. Good AChE inhibition (IC
= 22 ± 2.8 to 37.6 ± 0.75 μM) in correlation with the in silico results (binding energies = -8.55 to -8.14 Kcal/mol) were obtained. The mechanistic studies showed that all of the functionalities present in the chalcone scaffold were involved in binding with the amino acid residues at the binding site through hydrogen bonding, π-π, π-cation, π-sigma, and hydrophobic interactions. Molecular dynamics simulation studies showed the formation of stable complex between the AChE enzyme and
ligand.
Objective: To investigate the traditional antidiabetic uses of some indigenous Sudanese plants on streptozotocin-induced diabetes rats. Methods: Diabetic rats were treated with a 400 mg/kg dose of ...aqueous extracts of five plant species orally for 2 h(acute) or 14 days(chronic). In acute model blood glucose levels were monitored at specific intervals. In the chronic model blood samples were collected from overnight fasted diabetic rats on day 15 to estimate blood glucose level. And the body weight, serum lipid profile and activities of liver and kidney enzymes were measured. Histopathological observations of liver sections were also studied.Results: In the case of acute treatment, aqueous extracts of Tinospora bakis(T. bakis), Nauclea latifolia(N. latifolia) and Randia nilotica(R. nilotica) at 400 mg/kg significantly lowered(P < 0.05) blood glucose levels in diabetic rats whereas, chronic treatment of diabetic rats with 400 mg/kg of T. bakis, N. latifolia, R. nilotica and Mitragyna inremis proved to have significant(P < 0.05) antihyperglycemic effect and have the capacity to correct the metabolic disturbances associated with diabetes. Histopathological studies showed that the aqueous extracts of these four plants reinforced the healing of liver. However, Striga hermonthica aqueous extract did not exert any antihyperglycemic effect to diabetic rats. Conclusions: This study demonstrated that T. bakis, N. latifolia, R. nilotica and Mitragyna inremis have therapeutic value in diabetes and related complications and thus supporting the traditional uses of these plants in Sudanese traditional medicine.
PDF
