Flavonoids and their glycosides, including anthocyanins

The calcitonin/calcitonin gene-related peptide (CGRP) family of peptides includes calcitonin, α and β CGRP, amylin, adrenomedullin (AM) and adrenomedullin 2/intermedin (AM2/IMD). Their receptors consist of one of two G protein-coupled receptors (GPCRs), the calcitonin receptor (CTR) or the calcitonin receptor-like receptor (CLR). Further diversity arises from heterodimerisation of these GPCRs with one of three receptor activity-modifying proteins (RAMPs). This gives the CGRP receptor (CLR/RAMP1), the AM1 and AM2 receptors (CLR/RAMP2 or RAMP3) and the AMY1, AMY2 and AMY3 receptors (CTR/RAMPs1-3 complexes, respectively). Apart from the CGRP receptor, there are only peptide antagonists widely available for these receptors and these have limited selectivity, thus defining the function of each receptor in vivo remains challenging. Further challenges arise from the probable co-expression of CTR with the CTR/RAMP complexes and species-dependent splice variants of the CTR (CT(a) and CT(b)). Furthermore, the AMY1(a) receptor is activated equally well by both amylin and CGRP and the preferred receptor for AM2/IMD has been unclear. However, there are clear therapeutic rationales for developing agents against the various receptors for these peptides. For example many agents targeting the CGRP system are in clinical trials and pramlintide, an amylin analogue, is an approved therapy for insulin-requiring diabetes. This review provides an update on the pharmacology of the calcitonin family of peptides by members of the corresponding subcommittee of the International Union of Basic and Clinical Pharmacology and colleagues.

https://bpspubs.onlinelibrary.wiley.com/doi/epdf/10.1111/bph.14075

Update on the pharmacology of calcitonin/CGRP family of peptides: IUPHAR Review 25

The antitumor agents

The naphthoquinone shikonin is the main active principle of Zicao, a
 traditional Chinese herbal medicine made from the dried root of
 Lithospermum erythrorhizon. Studies carried out over the past 30
 years have provided a scientific basis for the use of Zicao which has
 been long employed in folk medicine to treat a variety of inflammatory and
 infectious diseases. In particular, shikonin has been shown to possess many
 diverse properties, including antioxidant, anti-inflammatory,
 antithrombotic, antimicrobial, and wound healing effects. The fact that
 shikonin shows so many beneficial properties has increased the interest in
 this molecule dramatically, especially in the past few years. The aim of
 this review is to provide an update of the new data published on shikonin,
 whose wide spectrum of pharmacological effects as well as pharmacokinetic
 properties and toxicity make it a highly interesting target molecule.

https://www.thieme-connect.com/products/ejournals/pdf/10.1055/s-0033-1350934.pdf

Pharmacological properties of shikonin - a review of literature since 2002

An update on lignans: natural products and synthesis.

Three new hydroquinone terpenoids with benzogeijerene skeletons, euchroquinols A-C (1- 3), and a new monoterpenylbenzenoid, 9,17-epoxyarnebinol (4), along with five known compounds were isolated from the stem bark of ARNEBIA EUCHROMA. Shikonin (6) exhibited potent anti-HCV activity with a selective index of 43.56, and compounds 1, 6, and des-O-methyllasiodiplodin (7) showed anti-Staphylococcus aureus activity with MICs of 0.5, 0.125, and 0.125 mg/mL, respectively.

Compounds from Arnebia euchroma and their related anti-HCV and antibacterial activities

Phytochemical studies on the branches and leaves of Lyonia ovalifolia yielded a new grayanane diterpenoid, lyonin A (1), together with two known compounds, secorhodomollolides A and D (2 and 3, resp.). The structure of 1 was elucidated by combination of 1D- and 2D-NMR, and MS analyses. Compound 1 turned out to be a new, highly O-acylated grayanane diterpenoid, of which ring B has undergone an oxidative cleavage between C(9) and C(10), yielding a system differing from the previously reported grayanane type with a 5/7/6/5 ring system. Results of the cAMP regulation activity assay showed that compounds 2 and 3 at 50 mu m induced a significantly decreased cAMP level in N1E-115 neuroblastoma cells (p < 0.001), indicating neuropharmacological potential.

Lyonin A, a new 9,10-Secograyanotoxin from Lyonia ovalifolia.

Three new iridoids, jatamanins N–P (1–3), along with the seven known iridiods 4–10, were isolated from the roots of Valeriana jatamansi. Compound 1 is an unusual iridoid bearing two epoxy bridges between C(3) and C(6) and between C(1) and C(10), forming a unique cage-like rigid skeleton. The structures of the new compounds were assigned on the basis of spectroscopic methods.

Iridoids from the Roots of Valeriana jatamansi

A new dibenzocyclooctadiene lignan, intermedin A (1), and a new natural bisabolane sesquiterpenoid, intermedin B (2), were isolated from the aerial parts of Schisandra propinqua var. intermedia. Their structures were elucidated on the basis of extensive spectroscopical analysis.

Hong-Mei Li

Papers

Compounds from Arnebia euchroma and their related anti-HCV and antibacterial activities

Lyonin A, a new 9,10-Secograyanotoxin from Lyonia ovalifolia.

Iridoids from the Roots of Valeriana jatamansi

Intermedins A and B; New metabolites from Schisandra propinqua var. intermedia

New grayanol diterpenoid and new phenolic glucoside from the flowers of Pieris formosa.