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Three lycodine-type Lycopodium alkaloids ( 1 – 3 ) were isolated from Lycopodiastrum casuarinoides . Their structures were elucidated by spectroscopic analysis, single-crystal X-ray crystallography, and computational methods. Compound 1 possesses a rearranged five-membered ring D resulting from C-8/C-15 cleavage and a new C-7/C-15 linkage. Compound 2 is the first Lycopodium alkaloid found to bear an additional carbon (C-17) directly bonded to C-8, which is particularly unusual from a biogenetic point of view. Compounds 1 – 3 were evaluated for acetylcholinesterase inhibitory activities. [ABSTRACT FROM AUTHOR]

Eighteen polycyclic polyprenylated acylphloroglucinols were isolated from the whole plant of Hypericum scabrum Linn., including six new compounds (1 – 6). Their structures were elucidated by comprehensive spectroscopic analyses. The evaluation of their cytotoxic activities was carried out against SMMC-7721 and MGC-803 cell lines. We found that most tested compounds exhibited moderate cytotoxic activities against SMMC-7721 cell line except for 11 and 12 , while compounds 1 , 5 – 7 , 13 and 16 also showed cytotoxic activities on MGC-803 cells. Besides, Bacillus subtilis, MRSA and MDPRA were also used to test inhibitory activity of these compounds. Our results showed that only compounds 12 and 13 presented weak inhibitory activity against Bacillus subtilis , while compounds 7 , 13 and 14 also inhibited MRSA weakly. [Display omitted] • Six new polycyclic polyprenylated acylphloroglucinols and twelve known analogues were isolated. • The structure–activity relationship (SAR) of cytotoxicities of tested compounds against SMMC-7721 cell line was concluded. • Some compounds exhibited antibacterial activities. [ABSTRACT FROM AUTHOR]

Abstract: Six new polycyclic polyprenylated acylphloroglucinols, attenuatumiones A–F (1–6), together with twelve known analogs (7–18) were isolated from the whole plant of Hypericum attenuatum. Their structures were elucidated by spectroscopic methods, and the absolute configuration of C-13 in attenuatumione C (3) was deduced via the circular dichroism datum of the in situ formed [Rh2(OCOCF3)4] complexes. All isolates were evaluated for the cytotoxic activities on three human cancer cell lines. Compound 3 showed moderate cytotoxic activities with IC50 values of 10.12 and 10.56μM against SMMC7721 and U2OS, respectively. [Copyright &y& Elsevier]

A new polysaccharide fraction HLP-1 (2.55 × 105 Da) was obtained from the fruiting bodies of Helvella leucopus. Structural characterization of HLP-1 was elucidated by infrared spectroscopy, monosaccharide composition analysis, methylation analysis, nuclear magnetic resonance spectroscopy, scanning electron microscopy and Congo red assay. HLP-1 was a mannan with a backbone of →6)- α -D-Man p (1 → 4)- α -D-Man p (1 →6)- α -D-Man p (1 → 3)- α -D-Man p (1 → 4)- α -D-Man p (1 → 3)- α -D-Man p (1→, which branched at the O-6 position and terminated with T- β -D-Man p. Moreover, HLP-1 could significantly improve the proliferation and neutral red phagocytosis of RAW264.7. Besides, HLP-1 could stimulate the production of nitric oxide (NO), ROS, tumor necrosis factor- α (TNF- α), interleukin-1 beta (IL-1 β) and interleukin-6 (IL-6). HLP-1 induced macrophage activation via NF-κB signal pathway. These findings indicated that HLP-1 was a potential immune enhancement agent applied in functional foods. • A new mannan HLP-1 was obtained from the fruiting bodies of Helvella leucopus. • Structural characterization of HLP-1 was analyzed. • HLP-1 possessed significantly immunostimulatory activity in vitro. [ABSTRACT FROM AUTHOR]

• Three new Stemona alkaloids were isolated from Stemona tuberosa. • Atrop-tuberostemonone (1) is a diastereomeric atropisomer of tuberostemonone. • The reported structure of stemonatuberone B was revised. • Tuberostemonine and 2-oxostenine showed inhibitory activity against acetylcholinesterase. Three new Stemona alkaloids (1 – 3), along with five known compounds (4 – 8), were isolated from the roots of Stemona tuberosa. Their structures were unambiguously elucidated by spectroscopic analysis and single-crystal X-ray crystallography. Atrop-tuberostemonone (1) is a stable conformational isomer of tuberostemonone (4), which features a new type of atropisomerism in one-carbon bridged lactam with a [6.4.1] scaffold. The reported structure of stemonatuberone B was revised to 4. The inhibitory activities of all the isolates against acetylcholinesterase were evaluated. [ABSTRACT FROM AUTHOR]

Graph The antioxidant activity of compounds B 1-8 b was measured by DPPH and ABTS radical scavenging assays [[14], [16]]. Among them, compounds B 1 b , B 2 b , and B 7 b were obtained from the I Osmanthus i genus for the first time, and compounds B 1-8 b were also isolated from I O. fragrans i "Ziyingui" for the first time. As shown in Table 1, compounds B 1-4 b and B 6-8 b revealed weaker I i -glucosidase inhibitory activities at 0.16 mM than the positive control acarbose; compounds B 3 b , B 5 b , B 7 b , and B 8 b showed weaker I i -amylase inhibitory activities at 0.16 mM than the positive control acarbose. [Extracted from the article]

Thirteen previously undescribed lycodine-type Lycopodium alkaloids, namely, five alkaloids (lycocasuarines D–H) each possessing an uncommon five-membered C ring and eight Lycopodium alkaloid glycosides (casuarinosides A–H), together with a known analog, were isolated from the aerial parts of Lycopodiastrum casuarinoides (Spring) Holub ex R.D.Dixit (Lycopodiaceae). The structures of the compounds were elucidated by extensive spectroscopic analysis, single-crystal X-ray diffraction, and chemical methods. In addition, the acetylcholinesterase inhibitory activity of the isolated compounds was evaluated. [ABSTRACT FROM AUTHOR]

Quorum sensing (QS) plays an important role in the production of virulence factors and pathogenicity in pathogenic bacteria and is, therefore, a hopeful target to fight against bacterial infections. During our search for natural QS inhibitors, two new xanthonolignoids (1 and 2), each existing as a racemic mixture, one new simple oxygenated xanthone (7), and eight known analogs (3–6, 8–11) were isolated from Hypericum scabrum Linn. Chiral separation of 1 yielded a pair of enantiomers 1a and 1b. The structures of these compounds were elucidated by spectroscopic analysis and ECD (electrostatic circular dichroism) calculations. All isolates were evaluated for their QS inhibitory activity against Chromobacterium violaceum. Both 9 and 10 exhibited the most potent QS inhibitory effects with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 31.25 and 62.5 μM, respectively. Crystal violet staining was used to further evaluate the biofilm inhibition potential of compounds 7, 9 and 10, and the formation of biofilms increased with decreasing drug concentration in a classic dose-dependent manner. The results of a cytotoxicity assay revealed that compounds 7, 9 and 10 exhibited no cytotoxic activity on PC-12 cells at the tested concentration. [ABSTRACT FROM AUTHOR]

Phytochemical research on the roots and rhizomes of Strobilanthes cusia (Acanthaceae) resulted in the isolation of 22 compounds. These include eleven alkaloids (1 – 11), five organic acids or aldehydes (12 – 15 , 18), two phenols (16 , 17), three phenylpropanoids (19 – 21), and one terpenoid (22). Notably, compounds 3 , 10 , 11 , 13 , 14 , 16 , 17 , and 19 – 21 were isolated from Acanthaceae plants for the first time, with compounds 3 and 10 – 22 being reported from Strobilanthes cusia for the first time. The study also discussed the chemotaxonomic significance of these discoveries. • Fourteen compounds were first reported from Strobilanthes cusia. • Ten compounds were first reported from the family Acanthaceae. • The chemotaxonomic significance of these isolates was discussed. [ABSTRACT FROM AUTHOR]

The leaves of Ligustrum robustum have been applied as Ku-Ding-Cha, a functional tea to clear heat, remove toxins, and treat obesity and diabetes, in Southwest China. The phytochemical research on the leaves of L. robustum led to the isolation and identification of eight new monoterpenoid glycosides (1–8) and three known monoterpenoid glycosides (9–11). Compounds 1–11 were tested for the inhibitory activities on fatty acid synthase (FAS), α-glucosidase, α-amylase, and the antioxidant effects. Compound 2 showed stronger FAS inhibitory activity (IC50: 2.36 ± 0.10 μM) than the positive control orlistat (IC50: 4.46 ± 0.13 μM), while compounds 1, 2, 5 and 11 displayed more potent ABTS radical scavenging activity (IC50: 6.91 ± 0.10~9.41 ± 0.22 μM) than the positive control L-(+)-ascorbic acid (IC50: 10.06 ± 0.19 μM). This study provided a theoretical basis for the leaves of L. robustum as a functional tea to treat obesity. [ABSTRACT FROM AUTHOR]

Immunocytes‐involved inflammation is considered to modulate the damage in various diseases. Oxidative stress is initiated by oxidative agents such as LPS and ROS, which are strongly involved in chronic inflammation. Our previous study found that a polysaccharide fraction from Craterellus cornucopioides (CCPP‐1) showed good antioxidant activity. However, the anti‐inflammatory effect of CCPP‐1 was still elusive. The objective of this study was to evaluate the anti‐inflammatory activity of CCPP‐1 and its potential mechanism in LPS‐stimulated RAW264.7 macrophages. The results showed that CCPP‐1 could inhibit LPS‐induced ROS and NO accumulation. Additionally, CCPP‐1 could decrease pro‐inflammatory cytokines production (TNF‐α, IL‐1β, and IL‐18) and inflammatory mediator (iNOS) expression, which might be associated with its capacity to inhibit NF‐κB signaling pathway and NLRP3 inflammasome activation. Therefore, this study suggested that CCPP‐1 had an ameliorative effect on the inflammation response and was potential to develop into functional food for treating chronic inflammation. Practical applications: Craterellus cornucopioides is an edible fungus widely distributed in Southwestern China. It was reported that C. cornucopioides polysaccharide (CCPP‐1), as important active ingredient, showed good antioxidant activity. However, the anti‐inflammatory effect was still elusive. This study showed that CCPP‐1 possessed anti‐inflammatory activity. The molecular mechanism might be associated with its capacity to inhibit NF‐κB signaling pathway and NLRP3 inflammasome activation. Therefore, polysaccharides from C. cornucopioides have potential to develop into functional food to combat inflammatory condition and thus indirectly halt the progression of various inflammatory response‐related chronic diseases. [ABSTRACT FROM AUTHOR]

Lycocasuarines I–Q (1 – 9), nine new lycodine-type Lycopodium alkaloids were isolated from the aerial parts of Lycopodiastrum casuarinoides (Spring) Holub ex R.D.Dixit. Their structures were unambiguously determined via extensive spectroscopic analyses, including HRESIMS, NMR, and electronic circular dichroism (ECD). The new alkaloids were evaluated for their in vitro inhibitory activity against acetylcholinesterase (AChE). Compounds 3 , 5 – 8 exhibited marginal or weak activities with IC 50 values ranging from 97.2 to 171.9 μM. Unlabelled Image [ABSTRACT FROM AUTHOR]

A phytochemical investigation of the fruits of Citrullus colocynthis resulted in the isolation of 21 structurally diverse cucurbitane triterpenoids, including 9 previously undescribed ones, colocynins A-I (1–9). Their absolute configurations were elucidated by means of quantum chemical electronic circular dichroism (ECD) calculations, CD exciton chirality method, and single-crystal X-ray crystallography. Colocynins A-C (1–3) represent the first examples of nonanorcucurbitane-type triterpenoids. An anti-acetylcholinesterase activity assay showed that 6 , 10 , 13 , 18 , and 20 exhibited inhibitory activities, with IC 50 values ranging from 5.0 to 21.7 μM. In addition, 18 and 21 showed significant cytotoxicity against PACA, A431, and HepG2 cells, with IC 50 values ranging from 0.042 to 0.60 and 3.6–14.4 μM, respectively. [Display omitted] • Nine new cucurbitane-type triterpenoids and twelve known analogues were isolated from the fruits of Citrullus colocynthis. • Compounds 1–3 represent the first examples of nonanorcucurbitane-type triterpenoids. • The absolute configurations of the new compounds were established. • Compounds 6 , 10 , 13 , 18 , and 20 exhibited anti-acetylcholinesterase activities. • Cytotoxic activities of compounds 18 and 21 are related to α , β -unsaturated conjugated system of C 17 side chain. [ABSTRACT FROM AUTHOR]

Abstract: Ten new geranylated 2-arylbenzofuran derivatives, including two monoterpenoid 2-arylbenzofurans (1 and 2), two geranylated 2-arylbenzofuran enantiomers (3a and 3b), and six geranylated 2-arylbenzofurans (4–9), along with four known 2-arylbenzofurans (10–13) were isolated from the root bark of Morus alba var. tatarica. Their structures and relative configurations were established on the basis of spectroscopic data analysis. Compounds 3–7 with one asymmetric carbon at C-7″ were supposed to be enantiomeric mixtures confirmed by chiral HPLC analysis, and the absolute configurations of each enantiomer in 3–7 were determined by Rh2(OCOCF3)4-induced CD and Snatzke's method. The enantiomers with the substituting group at C-2′ exhibited better resolutions on a Chiralpak AD-H column than those with the substituting group at C-4′. Compounds 1–7, 10, 11 and 13, showed α-glucosidase inhibitory activities with IC50 values of 11.9–131.9 μM, and compounds 1 and 9–13 inhibited protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 7.9–38.1 μM. [ABSTRACT FROM AUTHOR]

Abstract: Ten new geranylated 2-arylbenzofuran derivatives, including two monoterpenoid 2-arylbenzofurans (1 and 2), two geranylated 2-arylbenzofuran enantiomers (3a and 3b), and six geranylated 2-arylbenzofurans (4–9), along with four known 2-arylbenzofurans (10–13) were isolated from the root bark of Morus alba var. tatarica. Their structures and relative configurations were established on the basis of spectroscopic data analysis. Compounds 3–7 with one asymmetric carbon at C-7″ were supposed to be enantiomeric mixtures confirmed by chiral HPLC analysis, and the absolute configurations of each enantiomer in 3–7 were determined by Rh2(OCOCF3)4-induced CD and Snatzke's method. The enantiomers with the substituting group at C-2′ exhibited better resolutions on a Chiralpak AD-H column than those with the substituting group at C-4′. Compounds 1–7, 10, 11 and 13, showed α-glucosidase inhibitory activities with IC50 values of 11.9–131.9 μM, and compounds 1 and 9–13 inhibited protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 7.9–38.1 μM. [Copyright &y& Elsevier]

Among the four new flavonoids, mortatarins A-D, mortatarin D (IV) exhibits a significant degree of inhibition against the α-glucosidase. [ABSTRACT FROM AUTHOR]