A link between chemical structure and biological activity in triterpenoids

2021 ◽  
Vol 16 ◽  
Author(s):  
Zang Li ◽  
Hao Xu ◽  
Chao Huang ◽  
Cunqin Wang ◽  
Rongbin Wang ◽  
...  
Keyword(s):  
Chemical Structure ◽  
Biological Activities ◽  
Chemical Structures ◽  
Pentacyclic Triterpenoid ◽  
Medicinal Value ◽  
Anti Cancer ◽  
Cell Death Signaling ◽  
Cancer Activity ◽  
Novel Therapeutic ◽  
Skeleton Structure

Background: Plants with triterpenoid compounds in nature have various biological activities and are reported in many scientific works of literature. Triterpenoids are compounds that draw the attention of scientists because of their wide source, wide variety, high medicinal value, and anti-tumor properties. However, a lack of approach to understand their chemical structures has limited the fundamental comprehension of these compounds in cancer cell therapy. Objective: To seek anti-cancer activity of the structures of triterpenoid compounds and their derivatives, we summarized a number of plants and their derivatives that are a source of potential novel therapeutic anti-cancer agents. Methods: This work focuses on relevant 1036 patents and references that detail the structure of organic compounds and derivatives for the treatment of tumors. Result: Compared to tetracyclic triterpenoid, pentacyclic triterpenoid has contributed more to improve the autophagic signaling pathways of cancer cells. Conclusion: The heterogenous skeleton structure of triterpenoids impaired the programmed cell death signaling pathway in various cancers

ANTICANCER EFFECT OF UVARIA GENUS

2014 ◽  
pp. 98-101
Author(s):  
Thi Bich Hien Le ◽  
Viet Duc Ho ◽  
Thi Hoai Nguyen
Keyword(s):  
Biological Activities ◽  
Current Trend ◽  
Healthcare Systems ◽  
Chemical Compositions ◽  
Cancer Therapies ◽  
Pharmacological Effects ◽  
Anticancer Effect ◽  
Anti Cancer ◽  
Tropical Areas ◽  
Cancer Activity

Nowadays, cancer treatment has been a big challenge to healthcare systems. Most of clinical anti-cancer therapies are toxic and cause adverse effects to human body. Therefore, current trend in science is seeking and screening of natural compounds which possess antineoplastic activities to utilize in treatment. Uvaria L. - Annonaceae includes approximately 175 species spreading over tropical areas of Asia, Australia, Africa and America. Studies on chemical compositions and pharmacological effects of Uvaria showed that several compound classes in this genus such as alkaloid, flavonoid, cyclohexen derivaties, acetogenin, steroid, terpenoid, etc. indicate considerable biological activities, for example anti-tumor, anti-cancer, antibacterial, antifungal, antioxidant, etc. Specifically, anti-cancer activity of fractions of extract and pure isolated compounds stands out for cytotoxicity against many cancer cell lines. This study provides an overview of anti-cancer activity of Uvaria and suggests a potential for further studies on seeking and developing novel anti-cancer compounds. Key words: Anti-cancer, Uvaria.

scholarly journals A Further Comprehensive Review on the Phytoconstituents from the Genus Erythrina

2020 ◽  
Vol 23 (1) ◽  
pp. 65-77 ◽  
Author(s):  
Mohammad Musarraf Hussain
Keyword(s):  
Chemical Structure ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Pharmaceutical Journal ◽  
Significant Source ◽  
Comprehensive Review ◽  
Chemical Structures ◽  
Previous Review

Erythrina is a significant source of phytoconstituents. The aim of this review is to solicitude of classification, synthesis, and phytochemicals with biological activities of Erythrina. In our previous review on this genus (Hussain et. al., 2016a) fifteen species (Erythrina addisoniae, E. caribeae, E. indica, E. lattisima, E. melanacantha, E. mildbraedii, E. poeppigiama, E. stricta, E. subumbrans, E. veriagata, E. vespertilio, E. velutina, E. zeberi, E. zeyheri and E. americana) have been studied and 155 molecules with chemical structures were reported. A further comprehensive review was done upon continuation on the same genus and thirteen species (E. abyssinica, E. arborescens, E. berteroana, E. burttii, E. caffra, E. coralloids, E. crista-galli, E. fusca, E. herbaceae, E. lysistemon, E. mulungu, E. speciosa and E. tahitensis) of Erythrina have been studied and 127 compounds are reported as phytoconstituents with their chemical structure in this review. Erythrina crista-galli and E. lysistemon consist of highest number of chemical constituents. Bangladesh Pharmaceutical Journal 23(1): 65-77, 2020

scholarly journals Synergistic Action of Stilbenes in Muscadine Grape Berry Extract Shows Better Cytotoxic Potential Against Cancer Cells Than Resveratrol Alone

Biomedicines ◽  
2019 ◽  
Vol 7 (4) ◽  
pp. 96 ◽  
Author(s):  
Subramani Paranthaman Balasubramani ◽  
Mohammad Atikur Rahman ◽  
Sheikh Mehboob Basha
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Biological Activities ◽  
Grape Berry ◽  
Similar Response ◽  
Synergistic Activity ◽  
Anti Cancer ◽  
Muscadine Grape ◽  
Berry Extracts ◽  
Cancer Activity

Muscadine grape is rich in stilbenes, which include resveratrol, piceid, viniferin, pterostilbene, etc. Resveratrol has been extensively studied for its biological activities; however, the synergistic effect of stilbene compounds in berry extracts is poorly understood. The aim of this study was to evaluate the anti-cancer activity of stilbene-rich muscadine berry extract and pure resveratrol. Stilbenes were extracted from ripened berries of muscadine grape cultivars, Pineapple, and Southern Home. HPLC analysis was performed to determine quantity of stilbenes. The extracts were tested for their cytotoxic activity against A549 (lung carcinoma cells), triple negative breast cancer (HCC-1806) and HepG2 (human liver cancer) cells. The stilbene-rich extracts of the muscadine berry extracts showed cytotoxic activity against all of the cells tested. The extracts at 1 μg/mL induced death in 50–80% of cells by 72 h of treatment. About 50 μg/mL of resveratrol was required to induce a similar response in the cells. Further, modulation of genes involved in tumor progression and suppression was significantly (p < 0.0005) higher with the HepG2 cells treated with stilbene-rich berry extracts than the pure resveratrol. This shows that the synergistic activity of stilbenes present in muscadine grape berries have more potent anti-cancer activity than the resveratrol alone.

scholarly journals Anti-Cancer Potential of Synthetic Oleanolic Acid Derivatives and Their Conjugates with NSAIDs

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4957
Author(s):  
Wanda Baer-Dubowska ◽  
Maria Narożna ◽  
Violetta Krajka-Kuźniak
Keyword(s):  
Signaling Pathways ◽  
Oleanolic Acid ◽  
Short Review ◽  
Therapeutic Effects ◽  
Pentacyclic Triterpenoid ◽  
Anti Cancer ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Synthetic Derivatives ◽  
Cancer Activity

Naturally occurring pentacyclic triterpenoid oleanolic acid (OA) serves as a good scaffold for additional modifications to achieve synthetic derivatives. Therefore, a large number of triterpenoids have been synthetically modified in order to increase their bioactivity and their protective or therapeutic effects. Moreover, attempts were performed to conjugate synthetic triterpenoids with non-steroidal anti-inflammatory drugs (NSAIDs) or other functional groups. Among hundreds of synthesized triterpenoids, still the most promising is 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), which reached clinical trials level of investigations. The new group of synthetic triterpenoids are OA oximes. The most active among them is 3-hydroxyiminoolean-12-en-28-oic acid morpholide, which additionally improves the anti-cancer activity of standard NSAIDs. While targeting the Nrf2 and NF-κB signaling pathways is the main mechanism of synthetic OA derivatives′ anti-inflammatory and anti-cancer activity, most of these compounds exhibit multifunctional activity, and affect cross-talk within the cellular signaling network. This short review updates the earlier data and describes the new OA derivatives and their conjugates in the context of modification of signaling pathways involved in inflammation and cell survival and subsequently in cancer development.

A biphosphinic ruthenium complex with potent anti-bacterial and anti-cancer activity

2017 ◽  
Vol 41 (21) ◽  
pp. 13085-13095 ◽  
Author(s):  
José Marcos da Silveira Carvalho ◽  
Andressa Hellen de Morais Batista ◽  
Nádia Accioly Pinto Nogueira ◽  
Alda Karine Medeiros Holanda ◽  
Jackson Rodrigues de Sousa ◽  
...  
Keyword(s):  
Ruthenium Complex ◽  
Biological Activities ◽  
Anti Cancer ◽  
Cancer Activity

Photorelease of CO and moderate binding to DNA did not seem to be essential features for potent biological activities.

scholarly journals A Review: Underutilized plant of Sabah and Its Potential Value

2021 ◽  
Vol 22 ◽  
Author(s):  
Nor Amirah Shamsudin ◽  
Lucky Poh Wah Goh ◽  
Mohd Khalizan Sabullah ◽  
Suraya Abdul Sani ◽  
Rahmath Abdulla ◽  
...  
Keyword(s):  
Additional Data ◽  
Biological Activities ◽  
Local Area ◽  
Pharmacological Properties ◽  
Health Product ◽  
Sustainable Resources ◽  
Potential Value ◽  
Medicinal Value ◽  
Anti Cancer ◽  
Pharmacological Studies

Abstract: Underutilized plants are referred to a plant species which their potential is not fully utilized yet and they are usually found abundantly in certain local area but globally rare. Sabah is known for a high biodiversity and contains many underutilized plants. To our knowledge, this is the first review is to provide an overview information of medicinal value and pharmacological properties of underutilized plant in Sabah. Extract and metabolites in different part of several underutilized plant contains multiple beneficial bioactive compounds and exploitation of these compounds was supported by additional data which plays various biological activities including anti-atherosclerotic, anti-cancer, antihypercholesterolemic and anti-ulcerogenic. A handful of pharmacological studies on the natural product these underutilized plants have conclusively outlined the mode of action in treatment of several diseases and in other health aspects. This paper limits its scope to reviewe and highlight the potential of using underutilized plants in Sabah only which could serve as reliable resource for health product development in pharmaceutical and nutraceutical through continuous discovering of more active and sustainable resources as well as ingredients for food and medicine.

scholarly journals Ursolic Acid-Based Derivatives as Potential Anti-Cancer Agents: An Update

2020 ◽  
Vol 21 (16) ◽  
pp. 5920 ◽  
Author(s):  
Vuyolwethu Khwaza ◽  
Opeoluwa O. Oyedeji ◽  
Blessing A. Aderibigbe
Keyword(s):  
Ursolic Acid ◽  
Clinical Medicine ◽  
Biological Activities ◽  
Therapeutic Effects ◽  
Pharmacological Activities ◽  
Pentacyclic Triterpenoid ◽  
Anti Cancer ◽  
Pharmacologically Active ◽  
Derivatives Of ◽  
Cell Signaling Pathways

Ursolic acid is a pharmacologically active pentacyclic triterpenoid derived from medicinal plants, fruit, and vegetables. The pharmacological activities of ursolic acid have been extensively studied over the past few years and various reports have revealed that ursolic acid has multiple biological activities, which include anti-inflammatory, antioxidant, anti-cancer, etc. In terms of cancer treatment, ursolic acid interacts with a number of molecular targets that play an essential role in many cell signaling pathways. It suppresses transformation, inhibits proliferation, and induces apoptosis of tumor cells. Although ursolic acid has many benefits, its therapeutic applications in clinical medicine are limited by its poor bioavailability and absorption. To overcome such disadvantages, researchers around the globe have designed and developed synthetic ursolic acid derivatives with enhanced therapeutic effects by structurally modifying the parent skeleton of ursolic acid. These structurally modified compounds display enhanced therapeutic effects when compared to ursolic acid. This present review summarizes various synthesized derivatives of ursolic acid with anti-cancer activity which were reported from 2015 to date.

scholarly journals Coumarin sulfonamide derivatives: An emerging class of therapeutic agents

2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Review Article ◽  
Structural Motif ◽  
Structure Activity ◽  
Anti Cancer ◽  
Novel Therapeutic

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.

scholarly journals Computing Vertex Degree-Based Multiplicative Version of Topological Indices for Tungsten Trioxide Nano Multilayer Structure in Nanotherapeutic Anti-Cancer Activity

2021 ◽  
Vol 12 (2) ◽  
pp. 2275-2284
Keyword(s):  
Chemical Structure ◽  
Chemical Compounds ◽  
Topological Indices ◽  
Vertex Degree ◽  
Anti Cancer ◽  
Cancerous Cells ◽  
Insight Into ◽  
Cancer Activity ◽  
Mcf 7 ◽  
Chemical Materials

Several research reports suggest that there is a strong interdependence among the molecular structure of chemical compounds and their physicochemical properties. The computation of the topological index of such a chemical structure facilitates researchers to gain more insight into the physical and bio-activity of chemical materials. In this article, we focus on WO3, which is a widely studied nanomaterial and is recently employed as an excellent cytotoxic agent towards the liver (Hep–2) and the breast (MCF–7) cancerous cells. Various vertex degree-based multiplicative versions of topological indices for WO3 nano multilayer were computed using the edge partition technique. We also compared all of the indices graphically. The obtained results redress the lack of medical and chemical experiments, thus constructing the theoretical framework for the pharmacological field.

scholarly journals Phytochemical Profiling, In Vitro and In Silico Anti-Microbial and Anti-Cancer Activity Evaluations and Staph GyraseB and h-TOP-IIβ Receptor-Docking Studies of Major Constituents of Zygophyllum coccineum L. Aqueous-Ethanolic Extract and Its Subsequent Fractions: An Approach to Validate Traditional Phytomedicinal Knowledge

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 577
Author(s):  
Hamdoon A. Mohammed ◽  
Riaz A. Khan ◽  
Atef A. Abdel-Hafez ◽  
Marwa Abdel-Aziz ◽  
Eman Ahmed ◽  
...  
Keyword(s):  
In Silico ◽  
Biological Activities ◽  
Symptomatic Relief ◽  
Ethanolic Extract ◽  
Spectrometric Analysis ◽  
Chloroform Fraction ◽  
Anti Cancer ◽  
Aqueous Ethanolic Extract ◽  
Cancer Activity

Zygophyllum coccineum, an edible halophytic plant, is part of the traditional medicine chest in the Mediterranean region for symptomatic relief of diabetes, hypertension, wound healing, burns, infections, and rheumatoid arthritis pain. The current study aimed to characterize Z. coccineum phytoconstituents, and the evaluations of the anti-microbial-biofilm, and anti-cancers bioactivities of the plant’s mother liquor, i.e., aqueous-ethanolic extract, and its subsequent fractions. The in silico receptors interaction feasibility of Z. coccineum major constituents with Staph GyraseB, and human topoisomerase-IIβ (h-TOP-IIβ) were conducted to confirm the plant’s anti-microbial and anti-cancer biological activities. Thirty-eight secondary metabolites of flavonoids, stilbene, phenolic acids, alkaloids, and coumarin classes identified by LC-ESI-TOF-MS spectrometric analysis, and tiliroside (kaempferol-3-O-(6′′′′-p-coumaroyl)-glucoside, 19.8%), zygophyloside-F (12.78%), zygophyloside-G (9.67%), and isorhamnetin-3-O-glucoside (4.75%) were identified as the major constituents. A superior biofilm obliteration activity established the minimum biofilm eradication concentration (MBEC) for the chloroform fraction at 3.9–15.63 µg/mL, as compared to the positive controls (15.63–31.25 µg/mL) against all the microbial strains that produced the biofilm under study, except the Aspergillus fumigatus. The aqueous-ethanolic extract showed cytotoxic effects with IC50 values at 3.47, 3.19, and 2.27 µg/mL against MCF-7, HCT-116, and HepG2 cell-lines, respectively, together with the inhibition of h-TOP-IIβ with IC50 value at 45.05 ng/mL in comparison to its standard referral inhibitor (staurosporine, IC50, 135.33 ng/mL). This conclusively established the anti-cancer activity of the aqueous-ethanolic extract that also validated by in silico receptor-binding predicted energy levels and receptor-site docking feasibility of the major constituents of the plant’s extract. The study helped to authenticate some of the traditional phytomedicinal properties of the anti-infectious nature of the plant.

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