scholarly journals Pharmacological Effects of Grifolin: Focusing on Anticancer Mechanisms

Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 284
Author(s):  
Abdelhakim Bouyahya ◽  
Aicha El Allam ◽  
Ikrame Zeouk ◽  
Douae Taha ◽  
Gokhan Zengin ◽  
...  
Keyword(s):  
Human Cancer ◽  
Human Cancer Cell Lines ◽  
Beneficial Effects ◽  
Human Cancer Cells ◽  
Pharmaceutical Application ◽  
Cycle Arrest ◽  
Ability To Act ◽  
Anti Cancer

Grifolin is a volatile compound contained in essential oils of several medicinal plants. Several studies show that this substance has been the subject of numerous pharmacological investigations, which have yielded interesting results. Grifolin demonstrated beneficial effects for health via its multiple pharmacological activities. It has anti-microbial properties against bacteria, fungi, and parasites. In addition, grifolin exhibited remarkable anti-cancer effects on different human cancer cells. The anticancer action of this molecule is related to its ability to act at cellular and molecular levels on different checkpoints controlling the signaling pathways of human cancer cell lines. Grifolin can induce apoptosis, cell cycle arrest, autophagy, and senescence in these cells. Despite its major pharmacological properties, grifolin has only been investigated in vitro and in vivo. Therefore, further investigations concerning pharmacodynamic and pharmacokinetic tests are required for any possible pharmaceutical application of this substance. Moreover, toxicological tests and other investigations involving humans as a study model are required to validate the safety and clinical applications of grifolin.

scholarly journals A New Smoothened Antagonist Bearing the Purine Scaffold Shows Antitumour Activity In Vitro and In Vivo

2021 ◽  
Vol 22 (16) ◽  
pp. 8372
Author(s):  
Ana María Zárate ◽  
Christian Espinosa-Bustos ◽  
Simón Guerrero ◽  
Angélica Fierro ◽  
Felipe Oyarzún-Ampuero ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Antitumour Activity ◽  
Anticancer Compounds ◽  
Human Cancer Cells ◽  
Cycle Arrest ◽  
Apoptosis Inducer ◽  
Purine Ring

The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised, and biologically tested to provide an insight to their mechanism of action. Compound 4s was the most active and the best inhibitor of cell growth and selectively cytotoxic to cancer cells. 4s induced cell cycle arrest, apoptosis, a reduction in colony formation and downregulation of PTCH and GLI1 expression. BODIPY-cyclopamine displacement assays confirmed 4s is a SMO antagonist. In vivo, 4s strongly inhibited tumour relapse and metastasis of melanoma cells in mice. In vitro, 4s was more efficient than vismodegib to induce apoptosis in human cancer cells and that might be attributed to its dual ability to function as a SMO antagonist and apoptosis inducer.

Flavonoid-Based Cancer Therapy: An Updated Review

2020 ◽  
Vol 20 (12) ◽  
pp. 1398-1414 ◽  
Author(s):  
Elham Hosseinzadeh ◽  
Ali Hassanzadeh ◽  
Faroogh Marofi ◽  
Mohammad Reza Alivand ◽  
Saeed Solali
Keyword(s):  
Cancer Therapy ◽  
Cancer Cells ◽  
Human Cancer ◽  
Human Cancer Cells ◽  
Anti Cancer ◽  
Phytochemical Compounds ◽  
Proliferation And Metastasis ◽  
The Relationship

: As cancers are one of the most important causes of human morbidity and mortality worldwide, researchers try to discover novel compounds and therapeutic approaches to decrease survival of cancer cells, angiogenesis, proliferation and metastasis. In the last decade, use of special phytochemical compounds and flavonoids was reported to be an interesting and hopeful tactic in the field of cancer therapy. Flavonoids are natural polyphenols found in plant, fruits, vegetables, teas and medicinal herbs. Based on reports, over 10,000 flavonoids have been detected and categorized into several subclasses, including flavonols, anthocyanins, flavanones, flavones, isoflavones and chalcones. It seems that the anticancer effect of flavonoids is mainly due to their antioxidant and anti inflammatory activities and their potential to modulate molecular targets and signaling pathways involved in cell survival, proliferation, differentiation, migration, angiogenesis and hormone activities. The main aim of this review is to evaluate the relationship between flavonoids consumption and cancer risk, and discuss the anti-cancer effects of these natural compounds in human cancer cells. Hence, we tried to collect and revise important recent in vivo and in vitro researches about the most effective flavonoids and their main mechanisms of action in various types of cancer cells.

Potential Anti-Cancer Activities of Furanodiene, A Sesquiterpene from Curcuma wenyujin

2009 ◽  
Vol 37 (03) ◽  
pp. 589-596 ◽  
Author(s):  
Xiu-Yan Sun ◽  
Yan-Ping Zheng ◽  
Dong-Hai Lin ◽  
Hui Zhang ◽  
Feng Zhao ◽  
...  
Keyword(s):  
Essential Oil ◽  
Active Component ◽  
Human Cancer ◽  
Uterine Cervical Cancer ◽  
Primary Component ◽  
Inhibitory Effects ◽  
Human Cancer Cell Lines ◽  
Anti Cancer

Furanodiene is a sesquiterpene extracted from the essential oil of the rhizome of Curcuma wenyujin Y.H. Chen et C. Ling (Wen Ezhu). Furanodiene is the primary component in Wen Ezhu's essential oil, accounting for more than 20% by weight. In vitro, MTT assay was used to compare the inhibitory effects of furanodiene and Wen Ezhu's essential oil on 11 human cancer cell lines. Compared to the essential oil, furanodiene showed stronger growth inhibitions on Hela, Hep-2, HL-60, PC3, SGC-7901 and HT-1080 cells with IC50 between 0.6–4.8 μg/ml. In vivo, furanodiene was also found to exhibit inhibitory effects on the growth of uterine cervical (U14) and sarcoma 180 (Sl80) tumors in mice. Our data suggests that furanodiene, an active component from the essential oil of Wen Ezhu, possesses efficacy against uterine cervical cancer.

scholarly journals The Short-Term Effects of Pistacia Lentiscus Oil and Sesame Oil on Liver and Kidney Pathology of Rats and Human Cancer Cell Lines

2020 ◽  
Vol 9 ◽  
pp. 2001
Author(s):  
Maryam Ostovan ◽  
Mohammad Hossein Anbardar ◽  
Hajar Khazraei ◽  
Seyyed Mohammad bagher Fazljou ◽  
Zahra Khodabandeh ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Sesame Oil ◽  
Pistacia Lentiscus ◽  
Short Term ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Interstitial Inflammation

Background: Vegetable oils recently have been evaluated in many tissues. Pistacia lentiscus (mastic) of the Anacardiaceae family and Sesamum indicum (sesame) of the Pedaliaceae family are conventionally used in the management of gastrointestinal, lung, and skin illnesses. This assay attempts to determine if the oral usage of mastic and sesame oils has any short-term toxic effects in vivo on the rat and evaluate the human anticancer effect in vitro.  Materials and Methods: Twenty-one male Sprague-Dewley rats were assigned to three groups randomly: (A) control, (B) mastic oil (400 mg/kg), and (C) sesame oil (2cc/kg). The effects of these oils were investigated by determining histopathological and stereological parameters after six days, and the anticancer effects were evaluated on SW48, HepG2 human cell lines. Results: A mild chronic interstitial inflammation was seen in just one kidney of mastic oil group (B) and the other oneswere normal. In the sesame oil group (C), mild chronic interstitial inflammation was seen in six kidneys. In the liver samples of both groups, there were no specific pathological findings. Different concentrations of mastic oil (0.1%-5%) reduced the cell viability of SW48, HepG2, HEK293t, and human fat cells. Conclusion: Mastic and sesame oils have some side-effects on the kidney and might not be safe at high doses in rats. Sesame oil did not have any toxic effect on HepG2 and HEK293t human cancer cells. Mastic oil treatment has inhibited specific SW48 cells, so this oil seems to be a good adjuvant to chemotherapy in colon treatments.[GMJ.2020;9:e2001] 

Oleiferasaponin C6 from the seeds of Camellia oleifera Abel.: a novel compound inhibits proliferation through inducing cell-cycle arrest and apoptosis on human cancer cell lines in vitro

RSC Advances ◽  
2016 ◽  
Vol 6 (94) ◽  
pp. 91386-91393 ◽  
Author(s):  
Jianfa Zong ◽  
Dongxu Wang ◽  
Weiting Jiao ◽  
Liang Zhang ◽  
Guanhu Bao ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Camellia Oleifera ◽  
Human Cancer Cell Lines ◽  
Cycle Arrest

Oleiferasaponin C6 was isolated from Camellia oleifera Abel. and inhibits proliferation through inducing cell-cycle arrest and apoptosis on cancer cell lines in vitro.

scholarly journals Induction of apoptosis by in vitro and in vivo plant extracts derived from Menyanthes trifoliata L. in human cancer cells

2019 ◽  
Vol 71 (1) ◽  
pp. 165-180 ◽  
Author(s):  
Tomasz Kowalczyk ◽  
Przemysław Sitarek ◽  
Ewa Skała ◽  
Monika Toma ◽  
Marzena Wielanek ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Plant Extracts ◽  
Human Cancer ◽  
Human Cancer Cells ◽  
Induction Of Apoptosis ◽  
Menyanthes Trifoliata

The Design and Synthesis of Novel Phenothiazine Derivatives as Potential Cytotoxic Agents

2019 ◽  
Vol 17 (1) ◽  
pp. 57-67
Author(s):  
Yepeng Luan ◽  
Jinyi Liu ◽  
Jianjun Gao ◽  
Jinhua Wang
Keyword(s):  
Cell Lines ◽  
High Efficiency ◽  
Human Cancer ◽  
Human Tumor ◽  
Cytotoxic Agents ◽  
Cancer Drug ◽  
Human Cancer Cell Lines ◽  
Incidence And Mortality ◽  
Anti Cancer

Background: Cancer incidence and mortality have been increasing and cancer is still the leading cause of death all over the world. Despite the enormous progress in cancer treatment, many patients died of ineffective chemotherapy and drug resistance. Therefore, the design and development of anti-cancer drugs with high efficiency and low toxicity is still one of the most challenging tasks. Tricyclic heterocycles, such as phenothiazine, are always important sources of scaffolds for anti-cancer drug discovery. Methods: In this work, ten new urea-containing derivatives of phenothiazine coupled with different kinds of amine motifs at the endpoint through a three carbon long spacer were designed and synthesized. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR and HRMS. All the synthesized compounds were tested for their antitumor activity in vitro against the proliferation of PC-3 cells, and the compounds with best potency entered further cytotoxicity evaluations against other 22 human tumor cell lines. Mechanism was also studied. Results: From all data, it showed that among all 10 target compounds, TTi-2 showed the best effect in inhibiting the proliferation of 23 human cancer cell lines while TTi-2 without obvious inhibitory effect on normal cell. Furthermore, our results also showed that TTi-2 could inhibit migration, invasion and colony formation of MDA-MB-231 cells. Finally, TTi-2 can induce arrest of cell cycle at G0/G1 phase and cell apoptosis by activating the caspase 3 activity. Conclusion: All these results suggested that TTi-2 might be used as a promising lead compound for anticancer drug development.

scholarly journals New Oleoyl Hybrids of Natural Antioxidants: Synthesis and In Vitro Evaluation as Inducers of Apoptosis in Colorectal Cancer Cells

Antioxidants ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 1077
Author(s):  
Gabriele Carullo ◽  
Sarah Mazzotta ◽  
Adrian Koch ◽  
Kristin M. Hartmann ◽  
Oliver Friedrich ◽  
...  
Keyword(s):  
Healthy Lifestyle ◽  
Apoptotic Cell ◽  
Human Cancer ◽  
Natural Antioxidants ◽  
In Vitro Assays ◽  
Human Cancer Cell Lines ◽  
Cancer Management ◽  
Anti Cancer ◽  
Colorectal Cancer Cells

Nowadays, the beneficial role of a healthy lifestyle, particularly emphasizing the quality of foods and cancer management, is accepted worldwide. Polyphenols and oleic acid play a key role in this context, but are still scarcely used as anti-cancer agents due to their bio-accessibility limits. Therefore, we aimed to synthesize a set of new oleoyl-hybrids of quercetin, morin, pinocembrin, and catechin to overcome the low bioavailability of polyphenols, throughout a bio-catalytic approach using pancreatic porcine lipase as a catalyst. The in vitro assays, using a wide panel of human cancer cell lines showed, mainly for two novel regioisomer oleoyl-hybrids of quercetin, a remarkable increase in apoptotic cell populations. We suggested that the DNA damage shown as ɣH2AX signals might be the major cause of apoptotic cell death. Finally, we demonstrated convincing data about two novel polyphenol-based hybrids displaying a highly selective anti-cancer cytotoxicity and being superior compared to their reference/parental compounds.

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