Analysis of the anticancer activity of curcuminoids, thiotryptophan and 4-phenoxyphenol derivatives
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Curcumin, a non-nutritive yellow pigment derived from the rhizome of Curcuma longa (turmeric), is considered to be an established nutraceutical with anticancer activity. Turmeric contains three principal components, curcumin, demethoxycurcumin and bisdemethoxycurcumin, of which curcumin is most abundant and potent. The concurrence of a high consumption of turmeric and a low incidence of prostate cancer in Asian countries may suggest a role for curcumin in chemoprevention. Curcumin has been identified to exhibit anti-inflammatory, anti-oxidative and anticarcinogenic properties. Since the compound does not exhibit side effects, curcumin has been designated for several clinical trials as a treatment for human cancers. The pro-apototic, antioxidant and anti-inflammatory characteristics of curcumin are implicated in its anticancer activity, yet the mechanism of action of curcumin remains unknown. To achieve an effective pharmacological outcome, curcumin must reach and sustain appropriate levels at the site of action. However, the main disadvantage of curcumin is its high metabolic instability and poor aqueous solubility that limits its systemic bioavailability. To overcome this difficulty, the present study tested the anticancer activity of new curcumin-like compounds (E21cH and Q012095H). Also, the use of new medicaments requires an understanding of their pharmacokinetic profiles and targets. Thus, molecular modeling methods were used to identify the targets of curcumin and curcumin-like compounds compared with other anticancer drugs (Q012138 and Q012169AT), which were used as the controls. The present study identified several enzymes that are targeted by curcumin, aldo-keto reductase family 1 member B10 (AKR1B10), serine/threonine-protein kinase, protein kinase C, matrix metalloproteinase (MMP), cyclooxygenase and epidermal growth factor receptor, which were tested as targets for these anticancer chemicals. All the examined small compounds demonstrated anticancer activity in the in vitro experiments and may impact cancer cells by acting on AKR1B10, MMP-9 and their targets.Keywords:
Nutraceutical
Curcumin is the major constituent of turmeric ( Curcuma longa ). Turmeric has been widely used as a spice in foods and for therapeutic applications such as anti‐inflammatory, antihyperlipidemic, and antimicrobial activities. Turmeric and curcumin are nonmutagenic and nongenotoxic. Oral use of turmeric and curcumin did not have reproductive toxicity in animals at certain doses. Studies on human did not show toxic effects, and curcumin was safe at the dose of 6 g/day orally for 4–7 weeks. However, some adverse effects such as gastrointestinal upsets may occur. Moreover, oral bioavailable formulations of curcumin were safe for human at the dose of 500 mg two times in a day for 30 days, but there are still few trials and more studies are needed specially on nanoformulations and it should be discussed in a separate article. In addition, curcumin is known as a generally recognized as safe substance. This review discusses the safety and toxicity of turmeric and curcumin in medicine. Turmeric and curcumin are nontoxic for human especially in oral administration. Turmeric and curcumin are also safe in animals. They are nonmutagenic and are safe in pregnancy in animals but more studies in human are needed.
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Curcumin is a natural compound obtained from turmeric root with high antioxidant and anti-inflammatory activities. However, clinical application of curcumin has been limited due to its low solubility and bioavailability and rapid metabolism and degradation. This study was conducted to evaluate the effect of curcumin incorporation in zein nanoparticles on the pharmacokinetic parameters of systemic curcumin in plasma. Wistar rats were administered a single oral dose of 250 mg/kg of standard curcumin (control) or nanocurcumin (zein-based nanoparticles, Nucaps). The proposed new formulation was also compared with two commercially available curcumin complexes. Blood samples were collected at different times, and plasma levels were determined using HPLC-MS/MS. Overall, nanocurcumin (Nucaps) formulation was well tolerated and showed a 9-fold increase in oral bioavailability when compared to the standard curcumin natural extract. In addition, the nanoparticles prepared in this study demonstrated a bioavailability profile superior to that of other bioavailability-enhanced curcumin complexes currently available in the marketplace. Thus, our nanoparticle-based formulation has shown great potential as a nutraceutical for the oral administration of curcumin.
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Turmeric is the common name used for dried rhizome of Curcuma longa L., a monocotyledonous plant belonging to the family Zingiberaceae. Curcumin is responsible for the biological actions of turmeric and comprises of curcumin, demethoxy curcumin and bis demethoxy curcumin. Generally, the commercially produced curcumin is a mixture of the above with curcumin as the main constituent. Turmeric powder, curcumin and its derivatives and many other extracts from the rhizome were found to be bioactive. Tissue culture, an important area of biotechnology can be used to improve the productivity of planting material through enhanced availability of identified planting stock with desired traits.
Zingiberaceae
Curcuminoid
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Curcuma longa and its constituents, mainly curcumin, showed various of pharmacological effects in previous studies. This review article provides updated and comprehensive experimental and clinical evidence regarding the effects of C. longa and curcumin on respiratory, allergic, and immunologic disorders. Using appropriate keywords, databases including PubMed, Science Direct, and Scopus were searched until the end of October 2021. C. longa extracts and its constituent, curcumin, showed the relaxant effect on tracheal smooth muscle, which indicates their bronchodilatory effect in obstructive pulmonary diseases. The preventive effects of extracts of C. longa and curcumin were shown in experimental animal models of different respiratory diseases through antioxidant, immunomodulatory, and anti-inflammatory mechanisms. C. longa and curcumin also showed preventive effects on some lung disorders in the clinical studies. It was shown that the effects of C. longa on pulmonary diseases were mainly due to its constituent, curcumin. Pharmacological effects of C. longa extracts and curcumin on respiratory, allergic, and immunologic disorders indicate the possible therapeutic effect of the plant and curcumin on these diseases.
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Curcumin is a phytochemical which is extracted from Turmeric root. It is used as Ayurvedic Medicine. Curcumin (diferuloylmethane) is a yellow pigment present in the turmeric ( Curcuma longa ) which gives the yellow color to turmeric that has been associated with antioxidant, anti-inflammatory, anticancer, antiviral, and antibacterial activities. Curcumin, these effects are mediated through the regulation of various transcription factors, growth factors, inflammatory cytokines, protein kinases, and other enzymes. Most westerners know turmeric as gold colored Indian spice. Turmeric and curcumin are not the same thing. The antioxidant and anti-inflammatory property of curcumin is much more potent in an extracted form. In the recent research findings of curcumin that it can also eliminate 3% of cancer stem cells present inside the malignant tumor and remaining 97% of cancer cells undergo gradual cell shrinkage which ultimately leads to cell death. Pharmacologically, curcumin has been found to be safe. Human clinical trials indicated no dose-limiting toxicity when administered at doses up to 10 g/day. All of these studies suggest that curcumin has enormous potential in the prevention and therapy of various diseases. KEYWORDS: Curcumin, phytochemical, Curcuma longa , Ayurvedic Medicine.
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Anti-inflammatory
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Turmeric, a dried powder derived from the rhizome of Curcuma longa , has been used for centuries in certain parts of the world and has been linked to numerous biological activities including antioxidant, anti‐inflammatory, anticancer, antigrowth, anti‐arthritic, anti‐atherosclerotic, antidepressant, anti‐aging, antidiabetic, antimicrobial, wound healing, and memory‐enhancing activities. One component of turmeric is curcumin, which has been extensively studied, as indicated by more than 5600 citations, most of which have appeared within the past decade. Recent research has identified numerous chemical entities from turmeric other than curcumin. It is unclear whether all of the activities ascribed to turmeric are due to curcumin or whether other compounds in turmeric can manifest these activities uniquely, additively, or synergistically with curcumin. However, studies have indicated that turmeric oil, present in turmeric, can enhance the bioavailability of curcumin. Studies over the past decade have indicated that curcumin‐free turmeric (CFT) components possess numerous biological activities including anti‐inflammatory, anticancer, and antidiabetic activities. Elemene derived from turmeric is approved in China for the treatment of cancer. The current review focuses on the anticancer and anti‐inflammatory activities exhibited by CFT and by some individual components of turmeric, including turmerin, turmerone, elemene, furanodiene, curdione, bisacurone, cyclocurcumin, calebin A, and germacrone.
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Zingiberaceae
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The plant Curcuma longa, a perennial herbaceous member of the Zingiberaceae (ginger family), produces turmeric. Protein, fat, minerals, carbs, and moisture are all included in turmeric. Curcumin (diferuloylmethane), a phenolic diketone that makes up 34 percent of curcumin and is made up of curcumin I, curcumin II, and curcumin III, is what gives turmeric its characteristic yellow colour. Curcumin have versatile pharmacotherapeutic potential and their biological functions have been thoroughly investigated in recent years. As the main bioactive component, curcumin has numerous pharmacological properties including antioxidant, antiinflammatory, anti-hypertensive, anti-diabetic, hepatoprotective, anti-rheumatoid arthritis and anti-cancer properties. In persons who are active, it improves recuperation and performance. It helps with viral infections and dental issues such as dental pain, gingivitis. Covid also benefits from curcumin. ar-turmerone also possesses antiinflammatory properties. Ar-turmerone is a potentially effective treatment for a number of neurologic conditions like schizophrenia. Multiple health advantages are provided by curcumin when mixed with boosting agents.
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In the modern world, where a person is exposed to daily stress, increased physical exertion, the toxic effect of various substances, including drugs. The task of modern science is to find antioxidants for the body. These can be additives obtained both synthetically and the active substances that we get daily from food. Such a striking example is turmeric, obtained from the plant Curcuma longa. Recently, it has been known that curcumin has an antioxidant, anti-inflammatory, anti-cancer effect and, thanks to these effects, plays an important role in the prevention and treatment of various diseases, in particular, from cancer to autoimmune, neurological, cardiovascular and diabetic diseases. In addition, much attention is paid to increasing the biological activity and physiological effects of curcumin on the body through the synthesis of curcumin analogues. This review discusses the chemical and physical characteristics, analogues, metabolites, the mechanisms of its physiological activity and the effect of curcumin on the body.
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Curcuma Longa L. has been considered as an excellent source of curcumin, having wide scale applications in pharmaceutical, food and cosmetic industry. However, widespread applications of this relatively efficacious agent have been limited due to the poor aqueous solubility, and consequently, minimal systemic bioavailability. In this research, ‘submicron curcumin’ suspension in aqueous media was prepared from Curcuma longa L. without the presence of any additive. The average diameter of the ‘submicron curcumin’ particles was 546 nm (DLS). It was found that the ‘submicron curcumin’ suspension could be used in conjunction with several common food ingredients with its stability remaining unaffected. As the system only contained ‘submicron curcumin’ and water, it would be highly promising to applications in functional food, cosmetic, and pharmaceutical industries.
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