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Herbal Drug Discovery Against Inflammation: From Traditional Wisdom to Modern Therapeutics
Published in Amit Baran Sharangi, K. V. Peter, Medicinal Plants, 2023
Shalini Dixit, Karuna Shanker, Madhumita Srivastava, Priyanka Maurya, Nupur Srivastava, Jyotshna, Dnyaneshwar U. Bawankule
Parthenolide are isolated from Tanacetum parthenium L and are major sesquiterpenes lactones. Commonly occurs in leaves and flower heads of feverfew. Tanacetum parthenium is locally used by Mexican Indians for infectious diseases for a long time. Its methylene γ-lactone ring epoxide group has neuclophillic nature which enables its fast interaction with the receptor. The interaction between these sites and the receptors can induce oxidative stress and also shows anticancer properties (Mathema et al., 2012; Jain and Kulkarni, 1999; Li et al., 2002).
Biotransformation of Sesquiterpenoids, Ionones, Damascones, Adamantanes, and Aromatic Compounds by Green Algae, Fungi, and Mammals
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Yoshinori Asakawa, Yoshiaki Noma
Parthenolide (240), a germacrane-type lactone, isolated from the European feverfew (Tanacetum parthenium) as a major constituent, shows cytotoxic, antimicrobial, antifungal, anti-inflammatory, antirheumatic activity, apoptosis inducing, and NF-βB and DNA binding inhibitory activity. This substrate was incubated with A. niger in Czapek-peptone medium for 2 days to give six metabolites (241, 12.3%; 242, 11.3%; 243, 13.7%; 244, 5.0%; 245, 9.6%; 246, 5.1%) (Hashimoto et al., 2005) (Figure 23.71). Compound 244 was a naturally occurring lactone from Michelia champaca (Jacobsson et al., 1995). The stereostructure of compound 243 was established by x-ray crystallographic analysis.
Potential of Herbal Extracts and Bioactive Compounds for Human Healthcare
Published in Megh R. Goyal, Hafiz Ansar Rasul Suleria, Ramasamy Harikrishnan, The Role of Phytoconstitutents in Health Care, 2020
Ramasamy Harikrishnan, Chellam Balasundaram
Recently much interest has been focused on herbal bioactive compounds because of their ability to promote our health, with reference to the amelioration and better management of deleterious cancer, diabetes, and cardiovascular disorders, etc. [188, 420, 466]. The associations of free radicals by tumor or proto-oncogenes are involved in the progress of cancers [328, 329, 587]. Phenolics plant compounds have recently gained great popularity due to their significant bioactives and positive effects on human health [46, 63]. It is import ant to emphasize the need to increase the consumption of foods rich in Phenolic compounds aimed at preventive action [63]. The chlorophyll compound has a significant antioxidant effect [804]. Parthenolide and some other metabolites have been determined as an inhibitor of human blood platelet function [359].
Neuronal and non-neuronal TRPA1 as therapeutic targets for pain and headache relief
Published in Temperature, 2023
Luigi F. Iannone, Romina Nassini, Riccardo Patacchini, Pierangelo Geppetti, Francesco De Logu
Regarding herbal products, Tanacetum parthenium (feverfew) and Petasites hybridus Gaertn (butterbur) have been used for centuries to treat migraine and other pain conditions. Some preparations containing parthenolide (a feverfew constituent) and butterbur (in particular, its components, petasin and isopetasin) are or have been used for migraine prophylaxis [116]. In rodents, parthenolide and isopetasin behave as TRPA1 partial agonists [61,117] with an initial activation followed by prolonged concentration- and dose-dependent specific TRPA1 desensitization and nonspecific desensitization of peptidergic nociceptors, which express the channel [61]. In this manner, nociceptor nerve fibers became unresponsive to any stimulus, and unable to release CGRP from their terminals, including those present in the trigeminovascular system. Finally, a compound contained in plants largely used in traditional medicine, ligustilide, has been identified as a TRPA1 partial agonist, with a certain degree of inhibitory activity on mustard oil activated currents in the dural [118].
Lessons learned from the discovery and development of the sesquiterpene lactones in cancer therapy and prevention
Published in Expert Opinion on Drug Discovery, 2022
Israa A. Cheikh, Chirine El-Baba, Ali Youssef, Najat A. Saliba, Akram Ghantous, Nadine Darwiche
Curry et al. conducted the only phase 1 clinical trial based on parthenolide administration as a component of feverfew to cancer patients [221]. The daily administration of parthenolide as oral capsules for doses up to 4 mg did not successfully provide detectable plasma concentrations. As a result, pharmacokinetics studies of parthenolide could not be completed. The authors emphasized on their inability to enrich and reach the desired levels of parthenolide with the feverfew formulation. Furthermore, even though parthenolide led to reversible fever, gastrointestinal side effects, chills, fatigue, and blurred vision, no dose limiting toxicities were reached [221]. The chemically modified parthenolide analogue, DMAPT, entered phase 1 clinical trials for the treatment of leukemia and other blood cancers [7]. However, the study was suspended for unknown reasons. There is not enough evidence, to our knowledge, indicating that DMAPT was evaluated in a phase 2 clinical trial in AML patients [222].
Targeting Major Signaling Pathways of Bladder Cancer with Phytochemicals: A Review
Published in Nutrition and Cancer, 2021
Connor Chestnut, Dharmalingam Subramaniam, Prasad Dandawate, Subhash Padhye, John Taylor, Scott Weir, Shrikant Anant
Parthenolide occurs naturally in the feverfew herb (Tanacetum parthenium), which has been used in European folk medicine to treat ailments ranging from migraine headaches to dysmenorrhea (208). Parthenolide is an esquiterpene lactone and has been investigated in pre-clinical trials for treatment of both solid and hematogenous tumors (186). Shanmugam showed In Vivo that the water-soluble parthenolide analogue dimethylaminoparthenolide (DMAPT) inhibits BC cell proliferation through induction of oxidative stress, inhibition of NF-κB signaling, and induction of JNK (209). Cheng et al. showed In Vitro that parthenolide inhibits proliferation, induces apoptosis, and causes G1-phase arrest in BC cell lines (210). Western-blot analysis revealed that parthenolide achieved these effects through PARP activation and downregulation of Bcl-2 (210).