Natural withanolides, an update

Using solution or solid-phase synthesis we prepared the cholecystokinin fragment Boc-CCK-7 (Boc-Tyr-(SO3-.Na+)-Met-Gly-Trp-Met-Asp-PheNH2) and its four analogues in which the methionine moiety (Met) in the carboxy-terminal part is replaced by tert-leucine (Tle) or neopentylglycine (Neo) residue or D-enantiomers of these non-coded amino acids. These structural modifications led to reduction of the studied biological activities (gall bladder contraction, anorectic activity, analgetic and sedation activity) of all prepared analogues except Boc[Neo5]-CCK-7 which, being less analgetically active, retains full gall bladder and sedation activity of CCK-8. Moreover, its anorectic activity is substantially higher (400%). This analogue is very interesting particularly for its selectively increased (4x) anorectic effect compared with that of CCK-8.

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Methodologies in the Analysis of Phenolic Compounds in Roselle (Hibiscus sabdariffa L.): Composition, Biological Activity, and Beneficial Effects on Human Health

Horticulturae ◽

10.3390/horticulturae7020035 ◽

2021 ◽

Vol 7 (2) ◽

pp. 35

Author(s):

Bety W. Hapsari ◽

Manikharda ◽

Widiastuti Setyaningsih

Keyword(s):

Biological Activity ◽

Phenolic Compounds ◽

Human Health ◽

Analytical Methods ◽

Environmental Influence ◽

Biological Activities ◽

Research Progress ◽

Hibiscus Sabdariffa ◽

Beneficial Effects ◽

Positive Effects

Roselle (Hibiscus sabdariffa L.), as an edible flower, has long provided an array of positive effects on human health. This benefit is a result of phenolic compounds that are naturally present mainly in the calyx. Plentiful medicinal remedies and functional foods based on this flower are available worldwide, as supported by the studies of phenolic compounds in recent decades. This paper aims to provide a comprehensive review of the composition, biological activity, and beneficial effects on human health of phenolic compounds in roselle. This review was performed in accordance with the Preferred Reporting Items for Systematic reviews and Meta-Analyses (PRISMA) guidelines. A structured search in the published literature for phenolics compositions in roselle was required prior to the evaluation on the validity of the reported analytical methods. Reliable identification and quantification of phenolic compounds in roselle can be achieved by employing the proper extraction and separation methods. With ample alternative analytical methods discussed here, this review provided an aid for comprehending and selecting the most appropriate method for a particular study. The applications of the analytical methods highlighted indicated that phenolic acids, flavonoids, and their derivatives have been identified and quantified in roselle with a range of biological activities and beneficial effects on human health. It was also disclosed that the composition and concentration of phenolic compounds in roselle vary due to the growth factors, cultivars, and environmental influence. Finally, apart from the research progress carried out with roselle during the last ten years, this review also proposed relevant future works.

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Tanshinone IIA: Pharmacology, total synthesis, and progress in structure-modifications

Current Medicinal Chemistry ◽

10.2174/0929867328666211108110025 ◽

2021 ◽

Vol 28 ◽

Author(s):

Xing Huang ◽

Hao Deng ◽

Qing-kun Shen ◽

Zhe-Shan Quan

Keyword(s):

Herbal Medicine ◽

Total Synthesis ◽

Chinese Herbal Medicine ◽

Biological Activities ◽

Structural Features ◽

Tanshinone Iia ◽

Structural Modifications ◽

Chinese Herbal ◽

Bioactive Constituent

: Tanshinone IIA, a major bioactive constituent of Danshen, a Chinese herbal medicine, has gained extensive exploration owing to its unique structural features and multiple promising biological activities. This review focuses on the pharmacology, total synthesis, and structural modifications of tanshinone IIA. We hope this review will contribute to a better understanding of the progress in the field and provide constructive suggestions for further study of tanshinone IIA.

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The Bioavailability and Biological Activities of Phytosterols as Modulators of Cholesterol Metabolism

Molecules ◽

10.3390/molecules27020523 ◽

2022 ◽

Vol 27 (2) ◽

pp. 523

Author(s):

Xiang Li ◽

Yan Xin ◽

Yuqian Mo ◽

Pavel Marozik ◽

Taiping He ◽

...

Keyword(s):

Cholesterol Metabolism ◽

Biological Activities ◽

Low Density Lipoprotein ◽

Density Lipoprotein ◽

Cholesterol Absorption ◽

The Body ◽

Research Progress ◽

Intestinal Lumen ◽

Dose Response Relationship ◽

Liver X Receptor Α

Phytosterols are natural sterols widely found in plants that have a variety of physiological functions, and their role in reducing cholesterol absorption has garnered much attention. Although the bioavailability of phytosterols is only 0.5–2%, they can still promote cholesterol balance in the body. A mechanism of phytosterols for lowering cholesterol has now been proposed. They not only reduce the uptake of cholesterol in the intestinal lumen and affect its transport, but also regulate the metabolism of cholesterol in the liver. In addition, phytosterols can significantly reduce the plasma concentration of total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C), with a dose-response relationship. Ingestion of 3 g of phytosterols per day can reach the platform period, and this dose can reduce LDL-C by about 10.7%. On the other hand, phytosterols can also activate the liver X receptor α-CPY7A1 mediated bile acids excretion pathway and accelerate the transformation and metabolism of cholesterol. This article reviews the research progress of phytosterols as a molecular regulator of cholesterol and the mechanism of action for this pharmacological effect.

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The Natural Compound Hydrophobic Usnic Acid and Hydrophilic Potassium Usnate Derivative: Applications and Comparisons

Molecules ◽

10.3390/molecules26195995 ◽

2021 ◽

Vol 26 (19) ◽

pp. 5995

Author(s):

Hallysson Douglas Andrade de Araújo ◽

Hianna Arely Milca Fagundes Silva ◽

José Guedes da Silva Júnior ◽

Mônica Camelo Pessoa de Azevedo Albuquerque ◽

Luana Cassandra Breitenbach Barroso Coelho ◽

...

Keyword(s):

Biological Activities ◽

Structural Characteristics ◽

Usnic Acid ◽

Raw Material ◽

Structural Modifications ◽

Hydrophobic Molecule ◽

Antiparasitic Agents ◽

Toxic Molecule

Usnic acid is the best-studied lichen metabolite, presenting several biological activities, such as antibacterial, immunostimulating, antiviral, antifungal, anti-inflammatory, and antiparasitic agents; despite these relevant properties, it is a hydrophobic and toxic molecule. In this context, scientific research has driven the development of innovative alternatives, considering usnic acid as a source of raw material in obtaining new molecules, allowing structural modifications (syntheses) from it. The purpose is to optimize biological activities and toxicity, with less concentration and/or response time. This work presents a literature review with an analogy of the hydrophobic molecule of usnic acid with its hydrophilic derivative of potassium usnate, emphasizing the elucidation and structural characteristics, biological activities, and toxicological aspects of both molecules, and the advantages of using the promising derivative hydrophilic in different in vitro and in vivo assays when compared to usnic acid.

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Nonclassical Biological Activities of Quinolone Derivatives

Journal of Pharmacy & Pharmaceutical Sciences ◽

10.18433/j3302n ◽

2011 ◽

Vol 15 (1) ◽

pp. 52 ◽

Cited By ~ 19

Author(s):

Mohsen Daneshtalab ◽

Abeer Ahmed

Keyword(s):

Mammalian Cells ◽

Antibacterial Agents ◽

Biological Activities ◽

Antiviral Agent ◽

Bioactive Molecules ◽

Structural Modifications ◽

Further Development ◽

Derivatives Of ◽

Ns5b Polymerase

Quinolones are considered as a big family of multi-faceted drugs; their chemical synthesis is flexible and can be easily adapted to prepare new congeners with rationally devised structures. This is shown by the description of many thousands of derivatives in the literature. Scientists could accurately describe their QSAR, which is essential for effective drug design. This also gave them the chance to discover new and unprecedented activities, which makes quinolones an endless source of hope and enables further development of new clinically useful drugs. Quinolones are among the most common frameworks present in the bioactive molecules that have dominated the market for more than four decades. Since 1962, 4(1H)-quinolone-3-carboxylic acid derivatives are widely used as antibacterial agents. Quinolones have a broad and potent spectrum of activity and are also used as second-line drugs to treat tuberculosis (TB). Recently, quinolones have been reported to display “nonclassical” biological activities, such as antitumor, anti-HIV-1 integrase, anti- HCV-NS3 helicase and -NS5B-polymerase activities. The present review focuses on the structural modifications responsible for the transformation of an antibacterial into an anticancer agent and/or an antiviral agent. Indeed, quinolones’ antimicrobial action is distinguishable among antibacterial agents, because they target different type II topoisomerase enzymes. Many derivatives of this family show high activity against bacterial topoisomerases and eukaryotic topoisomerases, and are also toxic to cultured mammalian cells and in vivo tumor models. Moreover, quinolones have shown antiviral activity against HIV and HCV viruses. In this context the quinolones family of drugs seem to link three different biological activities (antibacterial, anticancer, and the antiviral profiles) and the review will also provide an insight into the different mechanisms responsible for these activities among different species. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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Alkaloids Produced by Endophytic Fungi: A Review

Natural Product Communications ◽

10.1177/1934578x1200700742 ◽

2012 ◽

Vol 7 (7) ◽

pp. 1934578X1200700 ◽

Cited By ~ 11

Author(s):

Yanyan Zhang ◽

Ting Han ◽

Qianliang Ming ◽

Lingshang Wu ◽

Khalid Rahman ◽

...

Keyword(s):

Endophytic Fungi ◽

Host Plants ◽

Biological Activities ◽

Biological Properties ◽

Research Progress ◽

Indole Derivatives ◽

Anticancer Activities ◽

Action Mechanisms ◽

The Future ◽

Potential Applications

In recent years, a number of alkaloids have been discovered from endophytic fungi in plants, which exhibited excellent biological properties such as antimicrobial, insecticidal, cytotoxic, and anticancer activities. This review mainly deals with the research progress on endophytic fungi for producing bioactive alkaloids such as quinoline and isoquinoline, amines and amides, indole derivatives, pyridines, and quinazolines. The biological activities and action mechanisms of these alkaloids from endophytic fungi are also introduced. Furthermore, the relationships between alkaloid-producing endophytes and their host plants, as well as their potential applications in the future are discussed.

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Current Research Progress on Long Noncoding RNAs Associated with Hepatocellular Carcinoma

Analytical Cellular Pathology ◽

10.1155/2019/1534607 ◽

2019 ◽

Vol 2019 ◽

pp. 1-8 ◽

Cited By ~ 3

Author(s):

Haihong Shi ◽

Yuxin Xu ◽

Xin Yi ◽

Dandan Fang ◽

Xia Hou

Keyword(s):

Hepatocellular Carcinoma ◽

Cell Proliferation ◽

Liver Cancer ◽

Biological Activities ◽

Noncoding Rnas ◽

Long Noncoding Rnas ◽

Research Progress ◽

Invasion And Metastasis ◽

Complex Processes ◽

And Function

Hepatocellular carcinoma (HCC) is the second leading cause of mortality among cancers. It has been found that long noncoding RNAs (lncRNAs) are involved in many human cancers, including liver cancer. It has been identified that carcinogenic and tumor-suppressing lncRNAs are associated with complex processes in liver cancer. These lncRNAs may participate in a variety of pathological and biological activities, such as cell proliferation, apoptosis, invasion, and metastasis. Here, we review the regulation and function of lncRNA in liver cancer and evaluate the potential of lncRNA as a new goal for liver cancer.

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Research progress on biological activities of Olea europaea leaf extract

China Journal of Chinese Materia Medica ◽

10.4268/cjcmm20160411 ◽

2016 ◽

Keyword(s):

Olea Europaea ◽

Leaf Extract ◽

Biological Activities ◽

Research Progress ◽

Olea Europaéa

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New Potential Inhibitors of Pheromonal Attractionin the Oriental Fruit Moth, Cydia molesta

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19981031 ◽

1998 ◽

Vol 63 (7) ◽

pp. 1031-1044 ◽

Cited By ~ 2

Author(s):

Michal Hoskovec ◽

Oldřich Hovorka ◽

Blanka Kalinová ◽

Bohumír Koutek ◽

Aleš Svatoš ◽

...

Keyword(s):

Biological Activities ◽

Inhibitory Effect ◽

Oriental Fruit Moth ◽

Single Sensillum Recording ◽

Wind Tunnel Experiments ◽

Structural Modifications ◽

Cydia Molesta ◽

Single Sensillum ◽

Behavioural Experiments ◽

Potential Inhibitors

New analogues of (Z)-dodec-8-en-1-yl acetate (Z8-12:OAc, 1), the main sex pheromone component of the Oriental fruit moth, Cydia molesta, were designed by formally transferring the terminal propyl group from the C-9 to the C-7 position to form vinyl-branched (2, 3) or, after isomerization, ethylidene-branched (4) structures and by replacing the -CH=CH- grouping by the -S-CH2- moiety (5, 6). Their biological activities were studied both electrophysiologically and behaviourally (laboratory mating and wind tunnel experiments). All the structural modifications resulted in analogues whose electroantennographic activities were lower than that of 1 following the order 1 >> 6 ≈ 5 >> 2 ≈ 4 ≈ 3. The single sensillum recording activities indicated that all the analogues stimulate the same Z8-12:OAc receptor neurone. In behavioural experiments, the analogues were generally found to reduce the ability of males to find a pheromone source, however, to different degrees. The highest inhibitory effect (90%) was observed for the thia analogues 5 and 6. The results support the view that the inhibitory properties of the analogues should not be entirely associated with their pheromone-mimicking capabilities.

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