scholarly journals Fungal Guttation, a Source of Bioactive Compounds and Its Ecological Role—A Review

Biomolecules ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 1270
Author(s):  
Adam Krain ◽  
Piotr Siupka
Keyword(s):  
Anticancer Agents ◽  
Incubation Temperature ◽  
Biological Activities ◽  
Culture Conditions ◽  
Medium Composition ◽  
Fungal Ecology ◽  
Bioactive Substances ◽  
Natural Products Discovery ◽  
Fungal Kingdom

Guttation is a common phenomenon in the fungal kingdom. Its occurrence and intensity depend largely on culture conditions, such as growth medium composition or incubation temperature. As filamentous fungi are a rich source of compounds, possessing various biological activities, guttation exudates could also contain bioactive substances. Among such molecules, researchers have already found numerous mycotoxins, antimicrobials, insecticides, bioherbicides, antiviral, and anticancer agents in exudate droplets. They belong to either secondary metabolites (SMs) or proteins and are secreted with different intensities. The background of guttation, in terms of its biological role, in vivo, and promoting factors, has been explored only partially. In this review, we describe the metabolites present in fungal exudates, their diversity, and bioactivities. Pointing to the significance of fungal ecology and natural products discovery, selected aspects of guttation in the fungi are discussed.

scholarly journals Influence of Culture Conditions and Medium Composition on the Production of Cellulose by Shiga Toxin-Producing Escherichia coli Cells

2009 ◽  
Vol 75 (13) ◽  
pp. 4630-4632 ◽  
Author(s):  
Byong Kwon Yoo ◽  
Jinru Chen
Keyword(s):  
Escherichia Coli ◽  
Water Activity ◽  
Shiga Toxin ◽  
Incubation Temperature ◽  
Culture Conditions ◽  
Luria Bertani ◽  
Medium Composition ◽  
Cellulose Production ◽  
Escherichia Coli Cells

ABSTRACT Culture conditions favoring cellulose production by Shiga toxin-producing Escherichia coli included a 28°C incubation temperature, an aerobic atmosphere, and the presence of 2% ethanol in Luria-Bertani no-salt agar with pH 6.0 and a water activity of 0.99. These findings will assist in formulating microbiological media useful for cellulose and biofilm research.

scholarly journals SEA CUCUMBER AS ANTICANCER AGENTS AND ITS DEVELOPMENT FOR FUNCTIONAL FOOD PRODUCTS

2014 ◽  
Vol 9 (2) ◽  
pp. 85 ◽  
Author(s):  
Sherly Ridhowati ◽  
Fransiska Rungkat Zakaria ◽  
Dahrul Syah ◽  
Ekowati Chasanah
Keyword(s):  
Enzymatic Hydrolysis ◽  
Anticancer Agents ◽  
Functional Food ◽  
Sea Cucumber ◽  
Biological Properties ◽  
Bioactive Substances ◽  
Potential Health ◽  
Sea Cucumbers ◽  
Antibacterial And Antifungal

Indonesia is popularly known as sea cucumber (teripang) exporter in the form of dried teripang. Commonly known as beche-de-mer or gamat, sea cucumber has long been used as medicine and food by Asian and Middle East people. Recent study  has shown that sea cucumbers contain active compounds that show potential health benefits and other biological properties such as antibacterial and antifungal products, anticoagulants, antihypertensives, immuno modulation, inhibitor of osteoclastogenesis. It was reported that sea cucumber posses aphrodisiacs, potentially improve immunity, anticancer and anticoagulation. Sea cucumber is also rich in collagen as a component of connective  tissue which can further be converted into smaller molecule and act as bioactive substances. This  review presents  the potential of sea cucumber as a functional food especially to prevent cancer and  strategy to develop sea cucumber-based functional food  by enzymatic hydrolysis and in vivo study.

Progress and development of C-3, C-6, and N-9 position substituted carbazole integrated molecular hybrid molecules as potential anticancer agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Pratibha Mehta Luthra ◽  
Nitin Kumar
Keyword(s):  
Biological Activity ◽  
Side Effects ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Structural Motif ◽  
Hybrid Compounds ◽  
Hybrid Molecules ◽  
Anticancer Mechanism ◽  
Pharmacologically Active

Abstract: The carbazole skeleton, a key structural motif occurring naturally or chemically synthesized, have shown various biological activities. Molecular hybridization based on the combination of two or more bioactive pharmacophores has been an important tool to convert the potent structural leads to form new hybrid compounds with improved biological activity. In recent years, modifications/substitutions of the carbazole motif at C3, C6, N9 position have been carried to develop novel carbazole based potential anticancer agents in the cancer therapy. In the last fifteen years, several compounds based on carbazole core integrated to pharmacologically active molecular hybrid having active pharmacophore such as 1,3,4-thiadiazole, thiazole, guanidine, sulfonamides, glyoxamides, imidazole, phenanthrene, rhodamine, chalcones, imidazopyridine, platinum 2H-chromen-2-one, hydrazones, piperazine, Isoxazole-thiadiazole, pyrazole etc. have been synthesized showing anticancer profile at sub-micromolar to nano-molar concentrations. We have thoroughly reviewed the design, progress and development of C-3, C-6, and N-9 position substituted carbazole derivatives integrated with various medicinally active pharmacophore as potential anticancer agents evaluated against various cancer cell lines. Additionally, the anticancer mechanism and in vivo activity of the reported compounds have been discussed. This study will support in designing of a new pharmacophore that can be linked to carbazole motif for development for new, potent and target specific anticancer drugs with improved pharmacokinetics and minimal side effects.

Advances on Quinazoline Based Congeners for Anticancer Potential

2021 ◽  
Vol 25 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Garima Kapoor ◽  
Lovekesh Mehta ◽  
Roma Ghai ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Anticancer Compounds ◽  
In Vivo Models ◽  
Appropriate Treatment

: The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop an appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogen-containing heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. The various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

scholarly journals Thiadiazole derivatives as anticancer agents

2020 ◽  
Vol 72 (5) ◽  
pp. 1079-1100 ◽  
Author(s):  
Monika Szeliga
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Cellular Membrane ◽  
Biological Targets ◽  
Cancer Pathogenesis ◽  
Thiadiazole Ring ◽  
Substantial Progress ◽  
Thiadiazole Derivatives

Abstract In spite of substantial progress made toward understanding cancer pathogenesis, this disease remains one of the leading causes of mortality. Thus, there is an urgent need to develop novel, more effective anticancer therapeutics. Thiadiazole ring is a versatile scaffold widely studied in medicinal chemistry. Mesoionic character of this ring allows thiadiazole-containing compounds to cross cellular membrane and interact strongly with biological targets. Consequently, these compounds exert a broad spectrum of biological activities. This review presents the current state of knowledge on thiadiazole derivatives that demonstrate in vitro and/or in vivo efficacy across the cancer models with an emphasis on targets of action. The influence of the substituent on the compounds’ activity is depicted. Furthermore, the results from clinical trials assessing thiadiazole-containing drugs in cancer patients are summarized.

scholarly journals Design, Synthesis and In-Vitro Biological Evaluation of Antofine and Tylophorine Prodrugs as Hypoxia-Targeted Anticancer Agents

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3327
Author(s):  
Ziad Omran ◽  
Chris P. Guise ◽  
Linwei Chen ◽  
Cyril Rauch ◽  
Ashraf N. Abdalla ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Multidrug Resistant ◽  
Biological Evaluation ◽  
High Chemical ◽  
Design Synthesis ◽  
Hypoxic Conditions ◽  
Cancerous Cell

Phenanthroindolizidines, such as antofine and tylophorine, are a family of natural alkaloids isolated from different species of Asclepiadaceas. They are characterized by interesting biological activities, such as pronounced cytotoxicity against different human cancerous cell lines, including multidrug-resistant examples. Nonetheless, these derivatives are associated with severe neurotoxicity and loss of in vivo activity due to the highly lipophilic nature of the alkaloids. Here, we describe the development of highly polar prodrugs of antofine and tylophorine as hypoxia-targeted prodrugs. The developed quaternary ammonium salts of phenanthroindolizidines showed high chemical and metabolic stability and are predicted to have no penetration through the blood–brain barrier. The designed prodrugs displayed decreased cytotoxicity when tested under normoxic conditions. However, their cytotoxic activity considerably increased when tested under hypoxic conditions.

Current developments in the Pyran-Based Analogues as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Lovekesh Mehta ◽  
Garima Kapoor ◽  
Pooja A. Chawla
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Anticancer Compounds ◽  
Appropriate Treatment ◽  
Anti Cancer ◽  
Privileged Structure ◽  
Different Types

: Heterocyclic compounds offer an enormous area for new lead molecules for drug discovery. Till today, efforts are being continuously made to find appropriate treatment for the management of the deadly disease of cancer. Amongst the large number of heterocycles that are found in nature, heterocycles having oxygen obtained noteworthy attention due to their distinctive and pharmacological activities.‘Pyran’ is one of the most significant non-aromatic, six-membered ring composed of one oxygen atom and five carbon atoms. It is considered a privileged structure since pyran and its related derivatives exhibit a wide spectrum of biological activities. Pyran derivatives are found to have excellent anti-cancer properties against various types of cancer. The present review focussed on the current advances in different types of pyran-based derivatives as anti-cancer agents. Various in-vitro (cell based testing), in-vivo (animal based testing) models as well as molecular docking along with results are also covered. A subsection describing briefly natural pyran containing anticancer compounds is also incorporated in the review.

scholarly journals Insight the Biological Activities of Selected Abietane Diterpenes Isolated from Plectranthus spp.

Biomolecules ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 194 ◽  
Author(s):  
Przemysław Sitarek ◽  
Monika Toma ◽  
Epole Ntungwe ◽  
Tomasz Kowalczyk ◽  
Ewa Skała ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Glioma Cell Line ◽  
In Vivo Studies ◽  
Considerable Proportion ◽  
M Cell ◽  
Abietane Diterpenoids ◽  
Pure Compounds ◽  
Abietane Diterpenes

Natural compounds isolated from plants are excellent starting points in drug design and have been widely studied as anticancer agents; they hence find use in a considerable proportion of anticancer drugs. The genus Plectranthus (Lamiaceae) comprises a large and widespread group of species with various applications in traditional medicine. Therefore, the aim of the present study was to determine the effectiveness of treatment with four abietane diterpenoids isolated from P. madagascariensis and P. ecklonii, 6,7-dehydroroyleanone, 7β,6β-dihydroxyroyleanone, 7α-acetoxy-6β-hydroxyroyleanone and parvifloron D, in initiating apoptosis in a glioma cell line. The pure compounds were found to exhibit anticancer effects in primary H7PX glioma cells line by inducing apoptosis G2/M cell cycle arrest and double-strand breaks, indicated by increased levels of phosphorylated H2A.X and decreasing mitochondrial membrane potential; they also influenced the expression of pro- and anti-apoptotic genes (Bax, Bcl-2, TP53, or Cas-3). Our findings indicate that these compounds may offer potential as beneficial antitumor drugs but further in vivo studies are needed.

scholarly journals Optimized Protocol for In Vitro Pollen Germination in Yam (Dioscorea spp.)

Plants ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 795
Author(s):  
Jean M. Mondo ◽  
Paterne A. Agre ◽  
Robert Asiedu ◽  
Malachy O. Akoroda ◽  
Asrat Asfaw
Keyword(s):  
Pollen Germination ◽  
Incubation Temperature ◽  
Optimal Growth ◽  
Germination Percentage ◽  
Medium Composition ◽  
Assessment Protocol ◽  
Critical Problems ◽  
Growing Conditions

Yam (Dioscorea spp.) plants are mostly dioecious and sometimes monoecious. Low, irregular, and asynchronous flowering of the genotypes are critical problems in yam breeding. Selecting suitable pollen parents and preserving yam pollen for future use are potential means of controlling these constraints and optimizing hybridization practice in yam breeding programs. However, implementing such procedures requires a robust protocol for pollen collection and viability testing to monitor pollen quality in the field and in storage. This study, therefore, aimed at optimizing the pollen germination assessment protocol for yam. The standard medium composition was stepwisely modified, the optimal growth condition was tested, and in vivo predictions were made. This study showed that the differences in yam pollen germination percentage are primarily linked to the genotype and growing conditions (i.e., medium viscosity, incubation temperature, and time to use) rather than the medium composition. The inclusion of polyethylene glycol (PEG) in the culture medium caused 67–75% inhibition of germination in D. alata. Although the in vivo fertilization was dependent on female parents, the in vitro germination test predicted the percentage fruit set at 25.2–79.7% and 26.4–59.7% accuracy for D. rotundata and D. alata genotypes, respectively. This study provides a reliable in vitro yam pollen germination protocol to support pollen management and preservation efforts in yam breeding.

scholarly journals Optimization of the Biosynthesis of B-Ring Ortho-Hydroxy Lated Flavonoids Using the 4-Hydroxyphenylacetate 3-Hydroxylase Complex (HpaBC) of Escherichia coli

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2919
Author(s):  
Longji Wang ◽  
Xiubing Ma ◽  
Haixiang Ruan ◽  
Yang Chen ◽  
Liping Gao ◽  
...  
Keyword(s):  
Biological Activities ◽  
Expression System ◽  
Culture Conditions ◽  
Expression Vectors ◽  
Plant Metabolites ◽  
Iptg Induction ◽  
C Terminus ◽  
Wide Range ◽  
Conversion Efficiencies

Flavonoids are important plant metabolites that exhibit a wide range of physiological and pharmaceutical functions. Because of their wide biological activities, such as anti-inflammatory, antioxidant, antiaging and anticancer, they have been widely used in foods, nutraceutical and pharmaceuticals industries. Here, the hydroxylase complex HpaBC was selected for the efficient in vivo production of ortho-hydroxylated flavonoids. Several HpaBC expression vectors were constructed, and the corresponding products were successfully detected by feeding naringenin to vector-carrying strains. However, when HpaC was linked with an S-Tag on the C terminus, the enzyme activity was significantly affected. The optimal culture conditions were determined, including a substrate concentration of 80 mg·L−1, an induction temperature of 28 °C, an M9 medium, and a substrate delay time of 6 h after IPTG induction. Finally, the efficiency of eriodictyol conversion from P2&3-carrying strains fed naringin was up to 57.67 ± 3.36%. The same strategy was used to produce catechin and caffeic acid, and the highest conversion efficiencies were 35.2 ± 3.14 and 32.93 ± 2.01%, respectively. In this paper, the catalytic activity of HpaBC on dihydrokaempferol and kaempferol was demonstrated for the first time. This study demonstrates a feasible method for efficiently synthesizing in vivo B-ring dihydroxylated flavonoids, such as catechins, flavanols, dihydroflavonols and flavonols, in a bacterial expression system.

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