Discovery of myrsinane-type Euphorbia diterpene derivatives through a skeleton conversion strategy from lathyrane diterpene for the treatment of Alzheimer's disease.

A series of novel myrsinane-type Euphorbia diterpene derivatives (1-37) were synthesized from the abundant natural lathyrane-type Euphorbia factor L, using a multi-step chemical process guided by a bioinspired skeleton conversion strategy, with the aim of discovering potential anti-Alzheimer's disease (AD) bioactive lead compounds. The synthesis process involved a concise reductive olefin coupling reaction through an intramolecular Michael addition with a free radical, followed by a visible-light-triggered regioselective cyclopropane ring-opening. The cholinesterase inhibitory and neuroprotective activities of the synthesized myrsinane derivatives were evaluated.

Design, synthesis and anti-inflammatory activity of diterpenoid alkaloids and non-steroidal anti-inflammatory drug hybrids based on molecular hybridization strategy.

Molecular hybridization is a widely employed approach in pharmaceutical chemistry for modifying drugs with the aim of improving pharmacological efficacy and reducing adverse effects. A prime example of this is the case of benorylate, which was created by combining aspirin and acetaminophen, two non-steroidal anti-inflammatory drugs (NSAIDs). Diterpenoid alkaloids, which exhibit potent anti-inflammatory activity, have limitations in their application due to their toxicity and side effects.

Palladium-Catalyzed Synthesis, Acetylcholinesterase Inhibition, and Neuroprotective Activities of -Aryl Galantamine Analogues.

A series of new -aryl galantamine analogues (-) were designed and synthesized by modification of galantamine, using Pd-catalyzed Buchwald-Hartwig cross-coupling reaction in good to excellent yields. The cholinesterase inhibitory and neuroprotective activities of -aryl derivatives of galantamine were evaluated. Among the synthesized compounds, the 4-methoxylpyridine-galantamine derivative () (IC = 0.

Synthesis, antiproliferative and anti-MDR activities of lathyrane diterpene derivatives based on configuration inversion strategy.

A series of lathyrane-type Euphorbia diterpene derivatives featured 3R configuration (H-3β) were synthesized from natural rich Euphorbia factor Lvia modified Mitsunobu reaction based on configuration inversion strategy. The antiproliferation activity and MDR reversal ability of the lathyrane derivatives were evaluated, and the most synthesized compounds showed moderate or strong potencies. Among them, diterpenes 21 (IC values of 2.

Kusnezosines A-C, three C-diterpenoid alkaloids with a new skeleton from Aconitum kusnezoffii Reichb. var. gibbiferum.

Kusnezosines A-C (1-3), three C-diterpenoid alkaloids with a new skeleton which featured an undescribed lactone type D-ring, were isolated from the roots of Aconitum kusnezoffii Reichb. var. gibbiferum.

Antitumor activity of nervosine VII, and the crosstalk between apoptosis and autophagy in HCT116 human colorectal cancer cells.

Nervosine VII is one of the known saturated pyrrolizidine alkaloids isolated from the plant of Liparis nervosa. This is first study to investigate the antitumor activity of nervosine VII in vitro, and the results indicated that nervosine VII induced autophagy and apoptosis in HCT116 human colorectal cancer cells. Mechanistic studies showed that nervosine VII-induced apoptosis was associated with the intrinsic pathway by the activation of caspase-9, -3 and -7.

Four new C-diterpenoid alkaloids from .

Four new C-diterpenoid alkaloids, rotundifosines D-G (), along with eight known ones () were isolated from the whole plant of Kar. & Kir. The structures of the compounds were elucidated on the basis of spectroscopic analyses, including HR-ESI-MS and 1D, 2D NMR.

Diterpenoid Alkaloids from Two Aconitum Species with Antifeedant Activity against Spodoptera exigua.

Twenty-five diterpenoid alkaloids were isolated from the roots of two Aconitum species. The structures of seven new C-diterpenoid alkaloids, apetaldines A-G (1-7), and 10 known alkaloids (8-17) from Aconitum apetalum and eight known alkaloids (18-25) from Aconitum franchetii var. villosulum were elucidated via HRESIMS, IR, and NMR data.

Diterpenoid Alkaloids from Delphinium anthriscifolium var. majus.

Extensive phytochemical investigation on the whole herbs of Delphinium anthriscifolium var. majus led to the identification of fourteen diterpenoid alkaloids, including three new C-diterpenoid alkaloids (anthriscifolsines A-C, 1-3), six new C-diterpenoid alkaloids (anthriscifolrines A-F, 4-9), and five know compounds (10-14). Among them, anthriscifolsine A represents a novel C-diterpenoid alkaloid characterized by a seco C-ring.

C-Diterpenoid alkaloids from Delphinium anthriscifolium var. majus.

Five new C-diterpenoid alkaloids, anthriscifoltines C-G (1-5), along with four known diterpenoid alkaloids anthriscifolcines C-F (6-9), were isolated from the extract of Delphinium anthriscifolium var. majus. Their structures were elucidated by extensive spectroscopic analyses (including 1D-, 2D-NMR, and HR-ESI-MS).

Five New C -Diterpenoid Alkaloids from Delphinium tianshanicum W.T.Wang.

Five new diterpenoid alkaloids, tianshanitines A-E (1 - 5), along with ten known compounds (6 - 15), were isolated from the EtOH extracts of the whole plant of Delphinium tianshanicum W.T.Wang.

Pyrrolizidine alkaloids from Liparis nervosa with inhibitory activities against LPS-induced NO production in RAW264.7 macrophages.

Six pyrrolizidine alkaloids were isolated from the whole herb of Liparis nervosa together with two previously known ones. Their structures were elucidated by extensive spectroscopic analyses and chemical reactions. The cytotoxicity of the isolates was evaluated against A549, HepG2, and MCF-7 human cancer cell lines; however, no significant growth inhibition was observed.

New nervogenic acid derivatives from Liparis nervosa.

Ten new nervogenic acid derivatives (1-4, 6-11) and one known compound (5) have been isolated from Liparis nervosa. Their structures were determined using extensive spectroscopic analysis, including 1D and 2D NMR experiments. Compounds 3, 4, 9, 10, and 11 were evaluated for their cytotoxicity against A549, H460, Hela, MCF-7, Caco2, and HepG2 human cancer cell lines.

A novel steroidal alkaloid from Fritillaria shuchengensis.

A novel steroidal alkaloid, suchengbeisine (1), along with two known steroidal alkaloids, N-oxide of verticinone (2) and zhebeininoside (3), were isolated from the bulbs of Fritillaria shuchengensis S. C. Chen et S.