Properties Of Natural Compounds Research Articles

Synthesis of Gingerol-Metals Complex and in-vitro Cytotoxic Activity on Human Colon Cancer Cell Line.

Herbs are excellent sources of medicinal substances, and their curative abilities have been recognized to treat many ailments and are used for example as antioxidants, analgesics, anti-inflammatories, antipyretics, and many other medicinal uses. The properties of natural compounds and their health effects have been studied extensively, especially those that originate from plant sources such as ginger. The ginger plant contains many chemical compounds, such as 6-gingerol, which is characterized by containing active groups such as carbonyl and hydroxide, which can be attached to metal molecules. This is what was done in this study, where the formation of complexes with a group of metals was studied and their effect on cancer cells was investigated. These complexes will open new horizons for further study of medicinal uses. The synthesis of gingerol-metal complexes was carried out by conjugating gingerol molecules with Ag, Au, Cd, Co, Cu, Ni, and Zn metal ions. The extracted gingerol was transferred to culture tubes and deionized water-DMSO were added followed by sonication. The tubes were incubated at 90°C for two days as well as the control sample. The samples were then filtered and the complex solutions were transferred into new tubes for further studies. Different characterization techniques such as FT-IR, UV-visspectroscopy, FESEM, and EDX are used to confirm the formation of the complexes. The in vitro of the complexes was tested by the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay against the human colorectal cancer cell lines HCT116 and HT29 which exhibited strong cytotoxicity. The gingerol-metal complexes showed an enhancement as an anticancer agent compared to the control. The in vitro anticancer activity showed that the Ag-gingerol complex showed the most activity among the other complexes. Gingerol-metal complexes can inhibit cancer cells, noting that the potency of the complex depends on the type of metal used.

The Novel Drug Discovery to Combat COVID-19 by Repressing Important Virus Proteins Involved in Pathogenesis Using Medicinal Herbal Compounds.

Background:The cause of COVID-19 global pandemic is SARS-CoV-2. Given the outbreak of this disease, it is so important to find a treatment. One strategy to cope with COVID-19 is to use the active ingredients of medicinal plants. In this study, the effect of active substances was surveyed in inhibiting four important druggable targets, including S protein, 3CLpro, RdRp, and N protein. RdRp controls the replication of SARS-CoV-2 and is crucial for its life cycle. 3CLpro is the main protease of the virus and could be another therapeutic target. Moreover, N protein and S protein are responsible for SARS-CoV-2 assembly and attaching, respectively.Methods:The 3D structures of herbal active ingredients were prepared and docked with the mentioned SARS-CoV-2 proteins to obtain their affinity. Then, available antiviral drugs introduced in other investigations were docked using similar tools and compared with the results of this study. Finally, other properties of natural compounds were uncovered for drug designing.Results:The outcomes of the study revealed that Linarin, Amentoflavone, (−)-Catechin Gallate and Hypericin from Chrysanthemum morifolium, Hypericum perforatum, Humulus lupulus, and Hibiscus sabdariffa had the highest affinity for these basic proteins and in some cases, their affinity was much higher than antiviral medicines.Conclusion:In addition to having high affinity, these herb active ingredients have antioxidant, vasoprotective, anticarcinogenic, and antiviral properties. Therefore, they can be used as extremely safe therapeutic compounds in drug design studies to control COVID-19.

“Drug-likeness” properties of natural compounds

Abstract Our previous work was focused on the fundamental physical and chemical concepts behind “drug-likeness” and “natural product (NP)-likeness”. Herein, we discuss further details on the concepts of “drug-likeness”, “lead-likeness” and “NP-likeness”. The discussion will first focus on NPs as drugs, then a discussion of previous studies in which the complexities of the scaffolds and chemical space of naturally occurring compounds have been compared with synthetic, semisynthetic compounds and the Food and Drug Administration-approved drugs. This is followed by guiding principles for designing “drug-like” natural product libraries for lead compound discovery purposes. In addition, we present a tool for measuring “NP-likeness” of compounds and a brief presentation of machine-learning approaches. A binary quantitative structure–activity relationship for classifying drugs from nondrugs and natural compounds from nonnatural ones is also described. While the studies add to the plethora of recently published works on the “drug-likeness” of NPs, it no doubt increases our understanding of the physicochemical properties that make NPs fall within the ranges associated with “drug-like” molecules.

Unraveling the molecular mechanisms and the potential chemopreventive/therapeutic properties of natural compounds in melanoma.

Melanoma is the most fatal form of skin cancer. Current therapeutic approaches include surgical resection, chemotherapy, targeted therapy and immunotherapy. However, these treatment strategies are associated with development of drug resistance and severe side effects. In recent years, natural compounds have also been extensively studied for their anti-melanoma effects, including tumor growth inhibition, apoptosis induction, angiogenesis and metastasis suppression and cancer stem cell elimination. Moreover, a considerable number of studies reported the synergistic activity of phytochemicals and standard anti-melanoma agents, as well as the enhanced effectiveness of their synthetic derivatives and novel formulations. However, clinical data confirming these promising effects in patients are still scanty. This review emphasizes the anti-tumor mechanisms and potential application of the most studied natural products for melanoma prevention and treatment.

Curcuminoids from tumeric (Curcuma longa) target microRNA148 and microRNA146 in their anti‐inflammatory effects in non‐cancer colon cells

The anti‐inflammatory properties of tumeric have been investigated in multiple studies, however the involvement of microRNAs in anti‐inflammatory properties of natural compounds has not been much investigated yet. We studied the potential protective effects of a standardized curcuminoid extract against inflammation induced by lipopolysacharide (LPS) in CCD‐18Co colon cells and investigated underlying miRNA based mechanisms. We investigated miRNAs 146, which is regulated by NF‐kB and involved in the regulation of the TLR4 pathway and also microRNA148a which is a regulator of pregnane X receptor (PXR) a transcription factor involved in the regulation of drug‐metabolizing enzymes and drug transporters as well as in the suppression of NF‐kB. LPS significantly induced the expression of all inflammatory biomarkers by up to 2 fold. The extract significantly reduced the expression of inflammatory biomarkers including NF‐kB, IL‐6, IL‐8, TRAF6, TLR‐4 up to 0.9, 0.2, 0.4, 0.32, and 0.1 fold of control cells. The expression of microRNA146 and 148a were increased by LPS up to 30% and reduced by curcuminoids by 30 and 25% respectively. Overall, these data confirm the anti‐inflammatory effects of curcuminoids in colon and indicate the involvement of microRNAs 146 and 148a in the anti‐inflammatory effects of curcuminoids.Grant Funding Source: ASN

Turmeric curcuminoids (Curcuma longa L.) interacts with microRNAs in the regulation of inflammation on Human Umbilical Vein Endothelial Cells (HUVEC)

The anti‐inflammatory properties of turmeric have been well‐investigated; however, the involvement of miRNAs in anti‐inflammatory properties of natural compounds has not been much investigated yet. We studied the potential protective effects of standardized curcuminoid extract (SCE) against vascular inflammation induced by lipopolysacharide (LPS) in HUVEC and investigated underlying miRNA based mechanisms. We screened miRNAs widely express on endothelial cells (miRNA 146a, miRNA 130, miRNA 126a and miRNA 155). However, only miRNA 146 clearly responded to LPS and reversal of this effect by SCE (2.5 –20 mg/L) down to 0.4 fold. miRNA 146 might be in control of Toll‐like receptor through a negative loop feedback regulation of NFK‐B activation. We analyzed the effect of SCE on NFK‐B expression and depended genes within the TLR4‐pathway which are target of miRNA146. SCE decreased the expression of NFK‐B, TRAF, IRAK1 and TLR4 by 0.6, 3.5, 1.6, and 0.84‐fold respectively. When cells were transfected with the mimic of miRNA146, SCE reversed the mimic‐induced expression of miRNA146 by 3‐fold. This indicates that the anti‐inflammatory effects of SCE are at least in part be exerted through the decrease in miRNA 146. Overall, curcuminoids showed anti‐inflammatory properties in HUVEC where a decreased of miR‐146a expression was involved in the underlying anti‐inflammatory mechanism.Grant Funding Source: ASN

Natural compounds with antiatherosclerotic properties

This article reviews the chemistry and biological properties of natural compounds possessing antiatherosclerotic properties.