China
Africa
Explore chapters and articles related to this topic
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
There is a number of plant-derived drugs are in the market, and some are in clinical trial phases such as Flavocoxid extract derived from Scutellaria baicalensis (Lamiaceae) and Acacia catechu (Mimosaceae) is in Phase I. This is developed by National Institute of Arthritis and Musculoskeletal and Skin Diseases, U.S.A. and Primus Pharmaceuticals. It is found to inhibit COX-1, COX-2, and 5-lipoxygenase. An intravenous chemotherapy agent Paxceed (micella Paclitaxel), developed by Agiotech pharmaceuticals is in Phase II. PMI-001 a botanical drug with multiple modes of mechanism and synergistic inhibition of IL-2, α-TNF, COX-2, and iNOS is in III phase of clinical. PMI-005 developed by phytomedicines for rheumatoid arthritis has completed Phase II in clinical trials. PMI-005 orally bioavailable and found to be active against pro-inflammatory cytokines including IL-2, α-TNF (Li and Li, 2011), COX-2 and iNOS. PMI-005 Phase II completed. It is an anti-inflammatory just finished with the II phase of clinical trials. A formulation PYN17 from European Chinese plants developed by Phynova to treat chronic hepatitis is in Phase IIa. IP-751 (Ajulemic acid, CT-3) appears to inhibit COX-2, and other inflammatory cytokines, particularly interleukin-1b, TNF-a, and also the peroxisomes proliferating activated receptor-g (PPAR-g) and is partial cannabinoid (CB) receptor agonist (Saklani and Kutty, 2008).
Asthma pharmacotherapy: an update on leukotriene treatments
Published in Expert Review of Respiratory Medicine, 2019
Hoang Kim Tu Trinh, So-Hee Lee, Thi Bich Tra Cao, Hae-Sim Park
Blockade of 5-LO enzymatic activity is beneficial for reducing LT synthesis, which induces vascular permeability and bronchoconstriction as well as LTB4-dependent pathway [33]. Nevertheless, it is unclear whether 5-LO inhibitors blocked the production of anti-inflammatory metabolites such as lipoxins. To date, among 5-LO inhibitors such as atreleuton (VIA-2291), MK-0633, PF-4,191,834, naproxen and flavocoxid, only zileuton is approved in clinical trials. Zileuton inhibits 5-hydroxyeicosatetranenoic acid synthesis, neutrophils and LTB4 biosynthesis, but it showed hepatic toxicity and adverse pharmacokinetic effects [34]. In patients with bronchial asthma, the robust effect of zileuton occurs 2 days after drug administration, but not immediately [11]. With increasing LTRA use, there is the need to develop novel 5-LO inhibitors.
Challenges with chromone as a privileged scaffold in drug discovery
Published in Expert Opinion on Drug Discovery, 2018
Carlos F. M. Silva, Vasco F. Batista, Diana C. G. A. Pinto, Artur M. S. Silva
This scaffold’s biological potential, allied to a low mammalian toxicity, prompted the development of several chromone-based drugs with distinct applications, particularly as anti-inflammatory agents (Figure 1) [5,6,8]. Disodium cromoglycate (1) is one such example, used as a mast cell stabilizer for the treatment of allergic rhinitis, asthma, and allergic conjunctivitis. Its commercialization faced some challenges, since the response of asthmatics to cromoglycate therapy is highly variable and it must be administrated by inhalation due to poor oral absorption. Likewise, nedocromil sodium (2) is marketed for the prevention of wheezing, shortness of breath, and other breathing problems caused by asthma. Also, flavocoxid, an extract containing the naturally occurring compound baicalin (3) as one of its major APIs, is an anti-inflammatory drug acting in the molecular pathways responsible for the production of both prostaglandins and leukotrienes, through the dual inhibition of COX and 5-LOX [9]. Finally, iguratimod (4) is a disease-modifying anti-rheumatic drug, accumulating its anti-inflammatory effects with the ability to inhibit immunoglobulin and cytokine production and even inducing an anabolic effect on bone metabolism [10].
The predictive utility of the plant phylogeny in identifying sources of cardiovascular drugs
Published in Pharmaceutical Biology, 2018
Emily Guzman, Jeanmaire Molina
The unrelated Lamiaceae family has also been shown to be TL for 7/9 species. Dracocephalum moldavica, traditionally used in Uyghur (Turkish) medicine, possessed polyphenolics, rosmarinic acid and tilianin, that inhibited platelet aggregation of plasma (Miernisha et al. 2016). Rosmarinic acid was first isolated from rosemary, Rosmarinus officinalis (Shekarchi et al. 2012), and may also be responsible for this species’ antithrombotic activity (Ulbricht et al. 2010). In traditional Chinese medicine, Salvia miltiorrhizae (danshen) is used to treat CVDs, and was also shown to inhibit platelet adhesion and aggregation, as well as protect against myocardial ischemia, effects attributable to its phenolic components, salvianolic acid A and B and danshensu (salianic acid A) (Liu and Huang 2016). Polyphenolic-rich aqueous extracts of basil, Ocimum basilicum, also inhibited platelet aggregation (Amrani et al. 2009). The flavonoid baicalin in the Chinese herb, Scutellaria baicalensis was also TL (Lee, Ku, et al. 2015) as well as anti-inflammatory, and in fact, used in flavocoxid, a medical food product prescribed for osteoarthritis (Levy et al. 2010). In Coleus forskohlii, the diterpene forskolin was responsible for its anticoagulant effect (Christenson et al. 1995). Though the specific phytochemical was not identified in motherwort, Leonurus cardiaca, it was also demonstrated to inhibit blood clotting. Presence of polyphenols, in general, seems to have inhibitory effect on platelet aggregation (Nardini et al. 2007). Though other species within Lamiaceae, such as Lavandula stoechas and Mentha spicata demonstrated other mechanisms of action (Table 1; Figure 1), it is highly likely that these species, as well as other members of Lamiaceae have TL effects given the pharmacological patterns observed.