scholarly journals Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

2019 ◽  
Vol 20 (17) ◽  
pp. 4238 ◽  
Author(s):  
Yaqi Ren ◽  
Chunlan Wang ◽  
Jiakun Xu ◽  
Shuaiyu Wang

Cafestol and kahweol are natural diterpenes extracted from coffee beans. In addition to the effect of raising serum lipid, in vitro and in vivo experimental results have revealed that the two diterpenes demonstrate multiple potential pharmacological actions such as anti-inflammation, hepatoprotective, anti-cancer, anti-diabetic, and anti-osteoclastogenesis activities. The most relevant mechanisms involved are down-regulating inflammation mediators, increasing glutathione (GSH), inducing apoptosis of tumor cells and anti-angiogenesis. Cafestol and kahweol show similar biological activities but not exactly the same, which might due to the presence of one conjugated double bond on the furan ring of the latter. This review aims to summarize the pharmacological properties and the underlying mechanisms of cafestol-type diterpenoids, which show their potential as functional food and multi-target alternative medicine.

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.


2018 ◽  
Vol 18 (2) ◽  
pp. 156-165 ◽  
Author(s):  
Jiaqiang Wang ◽  
Chien-shan Cheng ◽  
Yan Lu ◽  
Xiaowei Ding ◽  
Minmin Zhu ◽  
...  

Background: Propofol, a widely used intravenous anesthetic agent, is traditionally applied for sedation and general anesthesia. Explanation: Recent attention has been drawn to explore the effect and mechanisms of propofol against cancer progression in vitro and in vivo. Specifically, the proliferation-inhibiting and apoptosis-inducing properties of propofol in cancer have been studied. However, the underlying mechanisms remain unclear. Conclusion: This review focused on the findings within the past ten years and aimed to provide a general overview of propofol's malignance-modulating properties and the potential molecular mechanisms.


Cancers ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 1550 ◽  
Author(s):  
Tomomi Sanomachi ◽  
Shuhei Suzuki ◽  
Keita Togashi ◽  
Asuka Sugai ◽  
Shizuka Seino ◽  
...  

Spironolactone, a classical diuretic drug, is used to treat tumor-associated complications in cancer patients. Spironolactone was recently reported to exert anti-cancer effects by suppressing DNA damage repair. However, it currently remains unclear whether spironolactone exerts combinational effects with non-DNA-damaging anti-cancer drugs, such as gemcitabine and epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs). Using the cancer cells of lung cancer, pancreatic cancer, and glioblastoma, the combinational effects of spironolactone with gemcitabine and osimertinib, a third-generation EGFR-TKI, were examined in vitro with cell viability assays. To elucidate the underlying mechanisms, we investigated alterations induced in survivin, an anti-apoptotic protein, by spironolactone as well as the chemosensitization effects of the suppression of survivin by YM155, an inhibitor of survivin, and siRNA. We also examined the combinational effects in a mouse xenograft model. The results obtained revealed that spironolactone augmented cell death and the suppression of cell growth by gemcitabine and osimertinib. Spironolactone also reduced the expression of survivin in these cells, and the pharmacological and genetic suppression of survivin sensitized cells to gemcitabine and osimertinib. This combination also significantly suppressed tumor growth without apparent adverse effects in vivo. In conclusion, spironolactone is a safe candidate drug that exerts anti-cancer effects in combination with non-DNA-damaging drugs, such as gemcitabine and osimertinib, most likely through the suppression of survivin.


2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Shaopeng Wang ◽  
Caihua Zhang ◽  
Guang Yang ◽  
Yanzong Yang

Numerous studies have revealed that regular consumption of certain fruits and vegetables can reduce the risk of many diseases. The rhizome of Zingiber officinale (ginger) is consumed worldwide as a spice and herbal medicine. It contains pungent phenolic substances collectively known as gingerols. 6-Gingerol is the major pharmacologically-active component of ginger. It is known to exhibit a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation. 6-Gingerol has been found to possess anticancer activities via its effect on a variety of biological pathways involved in apoptosis, cell cycle regulation, cytotoxic activity, and inhibition of angiogenesis. Thus, due to its efficacy and regulation of multiple targets, as well as its safety for human use, 6-gingerol has received considerable interest as a potential therapeutic agent for the prevention and/or treatment of various diseases. Taken together, this review summarizes the various in vitro and in vivo pharmacological aspects of 6-gingerol and the underlying mechanisms.


Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4941
Author(s):  
Abdelwahab Khalil ◽  
Basem H. Elesawy ◽  
Tarek M. Ali ◽  
Osama M. Ahmed

Insects of the order Hymenoptera have a defensive substance that contains many biologically active compounds. Specifically, venom from honeybees (Apis mellifera) contains many enzymes and peptides that are effective against various diseases. Different research papers stated the possibility of using bee venom (a direct bee sting or in an injectable form) in treating several complications; either in vivo or in vitro. Other reports used the active fractions of bee venom clinically or at labratory scale. Many reports and publications have stated that bee venom and its constituents have multiple biological activities including anti-microbial, anti-protozoan, anti-cancer, anti-inflammatory, and anti-arthritic properties. The present review aims to refer to the use of bee venom itself or its fractions in treating several diseases and counteracting drug toxicities as an alternative protocol of therapy. The updated molecular mechanisms of actions of bee venom and its components are discussed in light of the previous updated publications. The review also summarizes the potential of venom loaded on nanoparticles as a drug delivery vehicle and its molecular mechanisms. Finally, the products of bee venom available in markets are also demonstrated.


Author(s):  
Girum Tefera Belachew ◽  
Bitaniya Abera Tekelemariam ◽  
Paramesh Hanumanthaiah ◽  
Fekede Meshesha Namo

Utilization of crude extracts separated from herbal medicine is getting more worthy and ideal, conceivably because of the expense of production, accessibility and availability to bring down harmful effects as much as possible. Various researches have shown that the regular use of particular soil products like fruits and vegetables can minimize the risk of a number of infections. Ginger is among the most commonly and regularly devoured dietary sauces on the planet. One of the major impactful components of ginger, 6-gingerol is suggested for the avoidance of malignancy and different maladies. As a spice and home grown medicine, the rhizome of Zingiber officinale (ginger) is devoured worldwide and it contains sharp phenolic compounds known as gingerols aggregately. The main pharmacologically-dynamic segment of ginger is 6-Gingerol. It is recognized to show a variety of organic actions including anti-cancer, anti-inflammation, and anti-oxidation. 6-Gingerol has been found to have anticancer effects by means of its impact on an assortment of natural pathways associated with apoptosis, control of cell cycle, cytotoxic action and restraint of angiogenesis. Consequently, because of its adequacy and control of different targets, just as its security for human use, 6-gingerol has gained impressive enthusiasm as an expected helpful operator for the anticipation and additionally treatment for different maladies. Taken together, this review sums up the different in vitro and in vivo pharmacological aspects of 6-gingerol and their underlying mechanisms.


2020 ◽  
Author(s):  
Bing Wei ◽  
Shangli Yao ◽  
Ming Gao ◽  
Zujun Wang ◽  
Wenyan Wang ◽  
...  

Abstract Resveratrol (RES), a natural compound found in red wine, has previously reported to suppress ovarian cancer (OC) cell growth in vitro and in vivo; however, its potential molecular mechanisms are not fully elucidated. The aim of this study is to investigate the suppressive potential of RES in OC cell growth and invasion and reveal the underlying mechanisms. Herein, we found that RES treatment obviously suppressed the proliferative and invasive capacities of OC cells, and elevated cell apoptosis in vitro. Subsequent microarray and qRT-PCR analysis further showed that microRNA-34a (miR-34a) was significantly increased by RES treatment. Moreover, the inhibitory effects of RES on OC cells were enhanced by miR-34a overexpression, whereas weakened by miR-34a inhibition in OC cells. Of note, Bcl-2, an anti-apoptotic gene, was identified as a direct target of miR-34a. Then, we revealed that RES decreased the expression of Bcl-2 in OC cells in a dose dependent manner. Furthermore, the anti-tumor effects of RES were abolished by overexpression of Bcl-2 in OC cells. Overall, these results demonstrated that RES exerts the anti-cancer effects on OC cells through the miR-34a/Bcl-2 axis.


2020 ◽  
Vol 40 (7) ◽  
Author(s):  
Bei Yue ◽  
Junyu Ren ◽  
Zhilun Yu ◽  
Xiaoping Luo ◽  
Yijing Ren ◽  
...  

Abstract Pinocembrin, a plant-derived flavonoid, has a variety of pharmacological activities, including anti-infection, anti-cancer, anti-inflammation, cardiovascular protection, etc. However, the mechanism of pinocembrin on the anti-colitis efficacy remains elusive and needs further investigation. Here, we reported that pinocembrin eased the severity of dextran sulfate sodium (DSS)-induced colitis in mice by suppressing the abnormal activation of toll-like receptor 4 (TLR4)/nuclear factor-kappa B (NF-κB) signal pathway in vivo. In addition, the gut microbiota was disordered in DSS colitis mice, which was associated with a significant decrease in microbiota diversity and a great shift in bacteria profiles; however, pinocembrin treatment improved the imbalance of gut microbiota and made it similar to that in normal mice. On the other hand, in vitro, pinocembrin down-regulated the TLR4/NF-κB signaling cascades in lipopolysaccharide (LPS)-stimulated macrophages. At the upstream level, pinocembrin competitively inhibited the binding of LPS to myeloid differentiation protein 2 (MD2), thereby blocking the formation of receptor multimer TLR4/MD2·LPS. Furthermore, pinocembrin dose-dependently promoted the expression of tight junction proteins (ZO-1, Claudin-1, Occludin and JAM-A) in Caco-2 cells. In conclusion, our work presented evidence that pinocembrin attenuated DSS-induced colitis in mouse, at least in part, via regulating intestinal microbiota, inhibiting the over-activation of TLR4/MD2/NF-κB signaling pathway, and improving the barriers of intestine.


Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Lovekesh Mehta ◽  
Garima Kapoor ◽  
Pooja A. Chawla

: 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.


1970 ◽  
Vol 64 (4) ◽  
pp. 656-669 ◽  
Author(s):  
J. van der Vies

ABSTRACT Since the biological activities of long-acting hormonal preparations, containing steroids or esters of steroids dissolved in arachis oil, depend very much on the rate of absorption from the intramuscular depot, an in vitro model for the latter has been developed. In this model the solution of the drug in oil is applied to a strip of filter paper and the spot eluted with a stream of hog plasma. Using this model, results were obtained which correlated with the observed rates of resorption in vivo. This demonstrates that the physical process underlying parenteral resorption depends on the distribution of the steroid between oil and plasma. As far as these esters of steroids are concerned, the steroid moiety of which is the ultimate active component, the hydrolysis of the ester by the esterase of the transporting plasma is another important factor. This has been studied in an in vitro system. The results obtained with both models proved valuable in understanding the pharmacological properties of a number of anabolic, androgenic and progestational steroids and steroid esters and also in explaining the differences in biological activity between closely related preparations.


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