scholarly journals Liquiritin from Glycirrhyza Glabra L (Fabaceae) - a Natural Derived Drug, as a Potential Inhibitor for SARS-CoV-2

Author(s):  
Akash Vanzara ◽  
Ravi Patel ◽  
Amisha Patel ◽  
Nimisha Patel ◽  
Kapil Yadav ◽  
...  

<p>Novel Corona virus-2 (Covid-19) is spreading and causing major damage around the globe and constantly increasing daily. There is a prerequisite of expeditious development of safe and efficient drugs for such a contagious disease. In this regard, utilization of a computational approach with an aim to provide potential enzyme inhibitors derived from natural resources will give a providential therapy. The present study investigated one of the promising plants namely Glycyrrhiza glabra L. It has various medicinal properties viz. anti-inflammatory, anti-cancer, anti-demulcent, expectorant, etc. <i>In-Silico</i> Analysis of liquiritin against SARS-CoV-2 Mpro was carried out using Autodock 4.2.6 and results were compared with presently prescribed drugs i.e. dexamethasone, remdesivir, hydroxychloroquine, and azithromycin. The binding energy of liquiritin was found to be -6.62 kcal/mol. It shows presence of hydrogen bond, hydrophobic interaction and electrostatic interaction with six active residues THR26, GLY143, CYS145, HIS 164, GLU166, and GLN189. Comparative studies investigated that dexamethasone, remdesivir, hydroxychloroquine, and azithromycin have four (THR26, GLY143, CYS145, GLU166), three (CYS145, GLU166, GLN189), four (GLY143, CYS145, HIS 164, GLN189) and two (GLU166, GLN189) identical active residues, respectively. The present study recommended liquiritin as a potential candidate against SARS-CoV-2 as it is naturally derived and has tremendous traditional usage against various diseases. However, in-vitro and in-vivo studies are required to prove its efficacy.</p>

2021 ◽  
Author(s):  
Akash Vanzara ◽  
Ravi Patel ◽  
Amisha Patel ◽  
Nimisha Patel ◽  
Kapil Yadav ◽  
...  

<p>Novel Corona virus-2 (Covid-19) is spreading and causing major damage around the globe and constantly increasing daily. There is a prerequisite of expeditious development of safe and efficient drugs for such a contagious disease. In this regard, utilization of a computational approach with an aim to provide potential enzyme inhibitors derived from natural resources will give a providential therapy. The present study investigated one of the promising plants namely Glycyrrhiza glabra L. It has various medicinal properties viz. anti-inflammatory, anti-cancer, anti-demulcent, expectorant, etc. <i>In-Silico</i> Analysis of liquiritin against SARS-CoV-2 Mpro was carried out using Autodock 4.2.6 and results were compared with presently prescribed drugs i.e. dexamethasone, remdesivir, hydroxychloroquine, and azithromycin. The binding energy of liquiritin was found to be -6.62 kcal/mol. It shows presence of hydrogen bond, hydrophobic interaction and electrostatic interaction with six active residues THR26, GLY143, CYS145, HIS 164, GLU166, and GLN189. Comparative studies investigated that dexamethasone, remdesivir, hydroxychloroquine, and azithromycin have four (THR26, GLY143, CYS145, GLU166), three (CYS145, GLU166, GLN189), four (GLY143, CYS145, HIS 164, GLN189) and two (GLU166, GLN189) identical active residues, respectively. The present study recommended liquiritin as a potential candidate against SARS-CoV-2 as it is naturally derived and has tremendous traditional usage against various diseases. However, in-vitro and in-vivo studies are required to prove its efficacy.</p>


Biomolecules ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 831 ◽  
Author(s):  
Ching-Shu Lai ◽  
Chi-Tang Ho ◽  
Min-Hsiung Pan

In recent decades, cancer has been one of the leading causes of death worldwide. Despite advances in understanding the molecular basis of tumorigenesis, diagnosis, and clinical therapies, the discovery and development of effective drugs is an active and vital field in cancer research. Tetrahydrocurcumin is a major curcuminoid metabolite of curcumin, naturally occurring in turmeric. The interest in tetrahydrocurcumin research is increasing because it is superior to curcumin in its solubility in water, chemical stability, bioavailability, and anti-oxidative activity. Many in vitro and in vivo studies have revealed that tetrahydrocurcumin exerts anti-cancer effects through various mechanisms, including modulation of oxidative stress, xenobiotic detoxification, inflammation, proliferation, metastasis, programmed cell death, and immunity. Despite the pharmacological similarities between tetrahydrocurcumin and curcumin, the structure of tetrahydrocurcumin determines its distinct and specific molecular mechanism, thus making it a potential candidate for the prevention and treatment of cancers. However, the utility of tetrahydrocurcumin is yet to be evaluated as only limited pharmacokinetic and oral bioavailability studies have been performed. This review summarizes research on the anti-cancer properties of tetrahydrocurcumin and describes its mechanisms of action.


Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3797
Author(s):  
Marta Olech ◽  
Wojciech Ziemichód ◽  
Natalia Nowacka-Jechalke

This review focuses on the natural sources and pharmacological activity of tormentic acid (TA; 2α,3β,19α-trihydroxyurs-2-en-28-oic acid). The current knowledge of its occurrence in various plant species and families is summarized. Biological activity (e.g., anti-inflammatory, antidiabetic, antihyperlipidemic, hepatoprotective, cardioprotective, neuroprotective, anti-cancer, anti-osteoarthritic, antinociceptive, antioxidative, anti-melanogenic, cytotoxic, antimicrobial, and antiparasitic) confirmed in in vitro and in vivo studies is compiled and described. Biochemical mechanisms affected by TA are indicated. Moreover, issues related to the biotechnological methods of production, effective eluents, and TA derivatives are presented.


Author(s):  
Aloisio Cunha de Carvalho ◽  
Leoni Villano Bonamin

Background: Several reviews about phytotherapy and homeopathy have been published in the last years, including Viscum album (VA.L). VA is a parasite plant whose extract has anti-cancer proprieties and is used alone or in combination with conventional chemotherapy. Methods: We performed a systematic review about the in vivo and in vitro models described in the literature, including veterinary clinical trials. The literature was consulted from Pubmed database. Results: There are several kinds of pharmaceutical preparations about VA and their active principles used in experimental studies, lectin being frequently studied (alone or as an extract compound). More than 50% of available literature about VA is related to the lectin effects. On the other hand, the effects of viscotoxins are less studied. Among the in vivo experimental studies about VA and its compounds, the B16 murine melanoma is the most used model, followed by Ehrlich, Walker and Dalton tumors. The results point to the apoptotic effects, metastasis control and tumor regression. Some veterinary clinical studies about the use of VA in the treatment of sarcoid, fibrosarcoma and neuroblastoma are quoted in literature too, with interesting results. Considering the in vitro models, our review revealed that NALM6 leukemia cells, B16 melanoma and NC1-H460 lung carcinoma were the most studied tumor models, apoptosis signals being the most important findings. Only one study verified immunoglobulin and interleukin production. All consulted papers were related to phytotherapy preparations only. Conclusions: Although the literature about the anti-cancer activity of VA extract and its lectins is enough, there is a marked lack of information about viscotoxin activities and about the effects of homeopathic preparations of this plant on animal tumors and on in vitro cultivated tumor cells.


2016 ◽  
Vol 62 (3) ◽  
pp. 63-76
Author(s):  
Joanna Smolibowska ◽  
Marcin Szymański ◽  
Arkadiusz Szymański

Summary The article presents the chemical costituents and pharmacological properties of polyporoid fungi found on birch, namely Piptoporus betulinus, Inonotus obliquus, Lenzites betulina, Fomes fomentarius, and Trametes versicolor. The in vitro and in vivo studies on the effect of different extracts from above-mentioned fungi on the human organism shown anti-cancer, anti-inflammatory, antiviral, antibacterial and immunostimulant activity, conditioned by the presence of such compounds as polysaccharides, polyphenols or terpenes. These fungi are commonly found in Poland and may superbly compete with Ganoderma lucidum (Reishi) or Lentinula edodes (Shitake) used in Asia for medicinal purposes.


2021 ◽  
Vol 12 (6) ◽  
pp. 52-59
Author(s):  
Rajeev Sati ◽  
Monika Bisht

Holmskioldia sanguinea Retz. is a Sub-Himalayan plant that has been cultivated in the Americas, Europe, Indo-china, Asia-Pacific, and Southern Africa. It has been used traditionally to treat rheumatism and rheumatoid arthritis, dysentery, headaches, hypertension, boils, blain, ulcers, and gynaecological problems, as well as a blood purifying concoction. The botanical description of the plant, its phytochemical constituents, and its pharmacological activities are discussed, with an emphasis on antibacterial, antihepatotoxic, antifungal, anti-inflammatory, antioxidant, antimicrobial, analgesic, central nervous system depressant, diuretic, oestrogenic, anti-implantation, and anticancer properties. Most pharmacological effects are a result of plant constituents such as alkaloids, terpenoids, tannins, flavonoids, glycosides and phenols, to name a few. Conventional wisdom should be confirmed through in vitro and in vivo studies, as well as clinical trials. Herb's anti-tumor and anti-cancer properties have generated significant interest.


2021 ◽  
Vol 22 (21) ◽  
pp. 12018
Author(s):  
Julia K. Bar ◽  
Anna Lis-Nawara ◽  
Piotr Grzegorz Grelewski

The therapeutic potential of the dental pulp stem (DSC) cell-derived secretome, consisting of various biomolecules, is undergoing intense research. Despite promising in vitro and in vivo studies, most DSC secretome-based therapies have not been implemented in human medicine because the paracrine effect of the bioactive factors secreted by human dental pulp stem cells (hDPSCs) and human exfoliated deciduous teeth (SHEDs) is not completely understood. In this review, we outline the current data on the hDPSC- and SHED-derived secretome as a potential candidate in the regeneration of bone, cartilage, and nerve tissue. Published reports demonstrate that the dental MSC-derived secretome/conditional medium may be effective in treating neurodegenerative diseases, neural injuries, cartilage defects, and repairing bone by regulating neuroprotective, anti-inflammatory, antiapoptotic, and angiogenic processes through secretome paracrine mechanisms. Dental MSC-secretomes, similarly to the bone marrow MSC-secretome activate molecular and cellular mechanisms, which determine the effectiveness of cell-free therapy. Many reports emphasize that dental MSC-derived secretomes have potential application in tissue-regenerating therapy due to their multidirectional paracrine effect observed in the therapy of many different injured tissues.


2018 ◽  
Vol 24 (24) ◽  
pp. 2760-2764 ◽  
Author(s):  
Chenxing Fu ◽  
Guiping Guan ◽  
Hongbing Wang

In vitro and in vivo studies have revealed that Sanguinarine has antioxidant, anti-inflammatory, proapoptotic, and growth inhibitory effects on tumor cells of a variety of cancers. Previous research showed that sanguinarine induced apoptosis (cell death) and/or antiproliferative while reducing tumor cell antiangiogenic and anti-invasive properties. This paper describes various sanguinarine anti-cancer mechanisms, including inhibition of erroneously-activated signal transduction pathways, apoptosis, and tumor cell proliferation inhibition.


2018 ◽  
Vol 16 (1) ◽  
pp. 78-91 ◽  
Author(s):  
Mateusz Pięt ◽  
Roman Paduch

Background:Cancer is one of the main causes of death worldwide. Contemporary therapies, including chemo- and radiotherapy, are burdened with severe side effects. Thus, there exists an urgent need to develop therapies that would be less devastating to the patient’s body. Such novel approaches can be based on the anti-tumorigenic activity of particular compounds or may involve sensitizing cells to chemotherapy and radiotherapy or reducing the side-effects of regular treatment.Objective:Natural-derived compounds are becoming more and more popular in cancer research. Examples of such substances are Ursolic Acid (UA) and Oleanolic Acid (OA), plant-derived pentacyclic triterpenoids which possess numerous beneficial properties, including anti-tumorigenic activity.Results:In recent years, ursolic and oleanolic acids have been demonstrated to exert a range of anticancer effects on various types of tumors. These compounds inhibit the viability and proliferation of cancer cells, prevent their migration and metastasis and induce their apoptosis. Both in vitro and in vivo studies indicate that UA and OA are promising anti-cancer agents that can prevent carcinogenesis at each step. Furthermore, cancers at all stages are susceptible to the activity of these compounds. </P><P> Neoplasms that are formed in the gastrointestinal tract, i.e. gastric, colorectal, pancreatic, and liver cancers, are among the most common and most lethal malignancies. Their localization in the digestive system, however, facilitates the action of orally-administered (potential) anti-cancer agents, making chemopreventive drugs more accessible.In this paper, the anti-tumorigenic effect of ursolic and oleanolic acids on gastric, colon, pancreatic, and liver cancers, as well as the mechanisms underlying this process, are presented.


2018 ◽  
Vol 36 (4_suppl) ◽  
pp. 323-323
Author(s):  
Khac Cuong Bui ◽  
Mai Ly Thi Nguyen ◽  
Samarpita Barat ◽  
Xi Chen ◽  
Vikas Bhuria ◽  
...  

323 Background: Adiponectin is the key adipokine, which plays an important role in health and disease such as obesity, diabetes, and cancer. Adiponectin is reduced in different tumor types, especially in obesity-related cancer, and recent studies showed that Adiponectin had a potential anti-cancer effect. Obesity is a risk factor for various tumor diseases including cholangiocarcinoma (CC), the second most common primary hepatic cancer. The aim of this study is to investigate for the first time the anti-cancer effect of AdipoR agonist in CC cell lines and a CC engineered mouse model. Methods: Human CC cell lines (TFK-1 and SZ-1) and CC engineered mice (Alb-Cre/KRASG12D/p53L/L) were used to investigate the anti-cancer effects of an AdipoR agonist (2-(4-Benzoylphenoxy)-N-[1-(phenylmethyl)-4-piperidinyl]-acetamide). Cell proliferation, migration, invasion, colony formation, apoptosis assay were applied to evaluate the effect of AdipoR agonist in vitro. In addition, important cancer signalling pathways and targets were analysed by Western Blot. Mice (n = 12) were treated with AdipoR or verhicle and tumor burden and survival were monitored. Results: AdipoR agonist suppressed proliferation, migration, invasion, colony formation and apoptosis in CC cells. AdipoR agonist regulated the expression of different proteins such as EMT markers, pAMPK, pSTAT3, and PARP, which have pivotal functions in cholangiocarcinogenesis. AdipoR agonist also prolonged survival time in a CC engineered mouse model. Conclusions: Our data revealed that AdipoR agonist inhibited successfully cell proliferation, migration, invasion, colony formation and apoptosis in vitro, and prolonged mice survival in vivo through regulation of crucial signaling pathways in cholangiocarcinogenesis. These results suggested that AdipoR agonist might become a new potential candidate for CC treatment in the future.


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