Characterization of binding interactions, gas-water interface properties and bioactivities in α-lactalbumin (αLa) with tea saponin (Ts), gynostemma saponin (Gyp) and tribulus saponin (Tr) were ...elucidated by using molecular docking, multi-spectroscopic techniques, polarization biomicroscopic and cryo-electron microscopic analysis. Specifically, the static quenching ability to intrinsic fluorescence of αLa decreased according to the order of Ts, Gyp and Tr. Among them, αLa interacted with Ts and Gyp through hydrogen bond and van der Waals force, while it combined with Tr via hydrophobic interaction force. Furthermore, Ts, Gyp and Tr made foaming ability of αLa increased by 164.54%, 136.73% and 63.95%, respectively. Under cryo-electron microscope, the descending order of foam integrity and liquid film thickness was αLa-Gyp, αLa-Tr, αLa-Ts. Moreover, the DPPH scavenging ability, ferrous reducing power, and α-glucosidase inhibition of αLa-saponins were higher than those of αLa, and αLa-Ts showed the maximum. Meanwhile, molecular docking indicated that there were different binding sites and numbers between αLa and three saponins. And αLa-Ts, αLa-Gyp and αLa-Tr had 12, 3 and 6 hydrogen bonds, respectively. Moreover, Ts did not significantly affect secondary structure of αLa, whereas Gyp and Tr decreased its α-helix and increased its random coil. The obtained results provided basic data supports for interaction mechanism between natural saponins and proteins, being beneficial to develop efficient and natural protein-saponin foaming agents for food industry.
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•αLa-Ts was the most stable and the least stable was αLa-Tr.•The addition of Ts had no significant effect on the secondary structure of αLa.•The addition of Gyp/Tr decreased the α-helix and increased the random curl of αLa.•The descending order to improve the foaming ability of αLa was Ts, Gyp, Tr.•αLa-Ts exhibited the best antioxidant activity and α-glucosidase inhibitory activity.
Diabetes mellitus (DM) is a long-term metabolic disorder that manifests as chronic hyperglycemia and impaired insulin, bringing a heavy load on the global health care system. Considering the ...inevitable side effects of conventional anti-diabetic drugs, saponins-rich natural products exert promising therapeutic properties to serve as safer and more cost-effective alternatives for DM management. Herein, this review systematically summarized the research progress on the anti-diabetic properties of dietary saponins and their underlying molecular mechanisms in the past 20 years. Dietary saponins possessed the multidirectional anti-diabetic capabilities by concurrent regulation of various signaling pathways, such as IRS-1/PI3K/Akt, AMPK, Nrf2/ARE, NF-κB-NLRP3, SREBP-1c, and PPARγ, in liver, pancreas, gut, and skeletal muscle. However, the industrialization and commercialization of dietary saponin-based drugs are confronted with a significant challenge due to the low bioavailability and lack of the standardization. Hence, in-depth evaluations in pharmacological profile, function-structure interaction, drug-signal pathway interrelation are essential for developing dietary saponins-based anti-diabetic treatments in the future.
•Universal colorimetric method for total quantification of saponins.•Quantification using only water-bath and spectrophotometer.•Bypassing all the interfering compounds through an optimised ...combination.•Similar accuracy compared to chromatographic method (LC-ELSD).
Saponins are heterosides widely distributed in the plant kingdom. Their properties are used in many industrial sectors, such as food, cosmetics, agriculture, and pharmaceuticals, and their use is increasing due to the market trend to use natural ingredients. Although many techniques exist to quantify saponins (e.g., gravimetric, foaming, spectrophotometric or chromatographic), none of these allow simultaneous accurate, rapid and inexpensive analysis of both triterpenoid and steroidal saponins. A new colorimetric method constituted of p-anisaldehyde and sulfuric acid was developed and avoids all of the above disadvantages. Parameters used in this method allow a similar molar absorptivity for steroidal and triterpenoid saponins with high specificity in complex matrices reducing the sample preparation step and allowing quantification of saponins blends.
Paris polyphylla, as a traditional Chinese herbal medicine, was often used to relieve inflammation and pain. Rhizoma Paridis saponins (RPS) as the main active components of Paris polyphylla have ...excellent analgesic effects.
Determine the analgesic material basis of RPS.
LC-MS/MS was used to analyze RPS, plasma after intravenous injection of RPS, and oral administration of RPS. H22 plantar pain model was established to explore the analgesic material basis of RPS. Moreover, correlation analysis, network pharmacology, RT-PCR and molecular docking were applied in this research.
RPS had dose-dependently analgesic effects in acetic acid- and formalin-induced pain models. LC-MS/MS detection indicated that diosgenin as the metabolite of RPS mainly distributed in brain tissues. The addition of antibiotics increased the anti-tumor effect of RPS, but reduced its analgesic effect. Network pharmacology, RT-PCR and molecular docking showed that diosgenin exerted its analgesic effect through SRC and Rap1 signaling pathway.
Diosgenin exhibited analgesic effects, while saponins had good anti-tumor effects in RPS. This discovery provided a better indication for the later application of RPS in anti-tumor and analgesic settings.
Steroidal and steroidal alkaloid glycosides, together with seven known compounds, were isolated from the aerial parts of
Solanum surattense Burm. f. Their structures were determined by spectroscopic ...methods.
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► Eleven saponins (
1–
11) were isolated from
Solanum surattense. ► Their structures were characterized on the basis of spectroscopic analysis. ► All compounds were evaluated for their cytotoxicities. ► Compounds
1 and
11 showed cytotoxicity against the A549.
A rare 16
β-H steroidal alkaloid saponin (
1), an avenacoside-type saponin (
2), two steroidal saponins (
4,
5), one revised-structure steroidal saponin (
3) and six known compounds (
6–
11) were isolated from aerial parts of
Solanum surattense Burm. f. Their structures were established on the basis of physical data, as well as by using spectroscopic (HRESIMS, 1D and 2D NMR), and chemical analysis methods. Compounds
1 and
11 showed cytotoxicity against A549 cell line with IC
50 values of 20.3 and 15.7
μM, respectively.
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Colorectal cancer (CRC) is one of the leading causes of cancer-related morbidity and mortality worldwide. Accumulating evidence suggests that mitochondrial dynamics are closely ...implicated in carcinogenesis including CRC. Paris Saponin II (PSII), a major steroidal saponin extracted from Rhizoma Paris polyphylla, has emerged as a potential anticancer agent. However, the effects of PSII on CRC and its underlying mechanisms remain unknown. In the present study, we found PSII induced apoptosis and inhibited colony formation in HT 29 and HCT 116 cells, and cell cycle arrest in G1 phase. PSII inhibited the phosphorylation of ERK1/2 and mitochondrial translocation of dynamin-related protein 1 (Drp1) by dephosphorylating Drp1 at Ser616, leading to the suppression of mitochondrial fission. PSII also suppressed NF-κB activation as a result of the inhibition of IKKβ and p65 translocation. Drp1 knockdown remarkably downregulated the nuclear expression of p65 and its target genes cyclin D1 and c-Myc in HCT 116 cell, confirming the link between mitochondrial fission and NF-κB pathway. Silencing of Drp 1 enhanced the inhibitory effects of PSII on p65 phosphorylation and the expressions of cyclin D1 and c-Myc, revealing that the inhibitory effects of PSII on cyclin D1 and c-Myc were relevant in the suppression of Drp1 and NF-κB activation. An in vivo study demonstrated PSII remarkably decreased the xenograft tumor size and suppressed the phosphorylation of ERK1/2 and Drp1 at Ser616. Taken together, our results suggested that PSII could inhibit colorectal carcinogenesis, at least in part, by regulating mitochondrial fission and NF-κB pathway.
Three spirostane saponins (1–3) and two furostane (4, 5) never described previously were isolated from Agave offoyana leaves. Their phytotoxic effect on Lactuca sativa indicated that may be ...considered as potential herbicides. Display omitted
•Five new steroidal saponins were isolated from Agave offoyana leaves.•Their structures were determined by NMR, mass spectrometry and chemical methods.•Saponins showed generally better phytotoxic effects than commercial herbicide used.
A bioassay-guided fractionation of Agave offoyana leaves led to the isolation of five steroidal saponins (1–5) along with six known saponins (6–11). The compounds were identified as (25R)-spirost-5-en-2α,3β-diol-12-one 3-O-{α-l-rhamnopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→2)-O-β-d-xylopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→4)-O-β-d-galactopyranoside} (1), (25R)-spirost-5-en-3β-ol-12-one 3-O-{α-l-rhamnopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→2)-O-β-d-xylopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→4)-O-β-d-galactopyranoside} (2), (25R)-spirost-5-en-3β-ol-12-one 3-O-{β-d-xylopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→2)-O-β-d-xylopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→4)-O-β-d-galactopyranoside} (3), (25R)-26-O-β-d-glucopyranosylfurost-5-en-3β,22α,26-triol-12-one 3-O-{α-l-rhamnopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→2)-O-β-d-xylopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→4)-O-β-d-galactopyranoside} (4) and (25R)-26-O-β-d-glucopyranosylfurost-5-en-3β,22α,26-triol-12-one 3-O-{β-d-xylopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→2)-O-β-d-xylopyranosyl-(1→3)-O-β-d-glucopyranosyl-(1→4)-O-β-d-galactopyranoside} (5) by comprehensive spectroscopic analysis, including one- and two-dimensional NMR techniques, mass spectrometry and chemical methods. The phytotoxicity of the isolated compounds on the standard target species Lactuca sativa was evaluated.
OSW-1 is a structurally unique steroidal saponin isolated from the bulbs of Ornithogalum saundersiae, and has exhibited highly potent and selective cytotoxicity in tumor cell lines. This study aimed ...to investigate the molecular mechanism for the membrane-permeabilizing activity of OSW-1 in comparison with those of other saponins by using various spectroscopic approaches. The membrane effects and hemolytic activity of OSW-1 were markedly enhanced in the presence of membrane cholesterol. Binding affinity measurements using fluorescent cholestatrienol and solid-state NMR spectroscopy of a 3-d-cholesterol probe suggested that OSW-1 interacts with membrane cholesterol without forming large aggregates while 3-O-glycosyl saponin, digitonin, forms cholesterol-containing aggregates. The results suggest that OSW-1/cholesterol interaction is likely to cause membrane permeabilization and pore formation without destroying the whole membrane integrity, which could partly be responsible for its highly potent cell toxicity.
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•OSW-1 has strong hemolytic and liposomal membrane activity owing to interactions with cholesterol in the membrane.•Cholesterol recognition by OSW-1 is essential for the subsequent membrane permeabilization.•OSW-1 induces membrane permeabilization via pore formation.
•Akebia saponin PA induces autophagy and apoptosis in AGS human gastric cancer cells.•PI3K/Akt/mTOR and AMPK/mTOR pathways are involved in akebia saponin PA-induced autophagy.•Autophagy plays the ...main role in akebia saponin PA-induced cell death.•Akebia saponin PA-induced autophagy activates JNK/p38 to promote caspase-3-dependent apoptosis.
In this study, we investigated the anticancer mechanism of akebia saponin PA (AS), a natural product isolated from Dipsacus asperoides in human gastric cancer cell lines. It was shown that AS-induced cell death is caused by autophagy and apoptosis in AGS cells. The apoptosis-inducing effect of AS was characterized by annexin V/propidium (PI) staining, increase of sub-G1 phase and caspase-3 activation, while the autophagy-inducing effect was indicated by the formation of cytoplasmic vacuoles and microtubule-associated protein 1 light chain-3 II (LC3-II) conversion. The autophagy inhibitor bafilomycin A1 (BaF1) decreased AS-induced cell death and caspase-3 activation, but caspase-3 inhibitor Ac-DEVD-CHO did not affect LC3-II accumulation or AS-induced cell viability, suggesting that AS induces autophagic cell death and autophagy contributes to caspase-3-dependent apoptosis. Furthermore, AS activated p38/c-Jun N-terminal kinase (JNK), which could be inhibited by BaF1, and caspase-3 activation was attenuated by both SB202190 and SP600125, indicating that AS-induced autophagy promotes mitogen-activated protein kinases (MAPKs)-mediated apoptosis. Taken together, these results demonstrate that AS induces autophagic and apoptotic cell death and autophagy plays the main role in akebia saponin PA-induced cell death.
Diabetes is a global disease that endangers human health. As reported, saponins are effective bioactive compounds for treating type 2 diabetes mellitus (T2DM) and have nontoxic side effects. This ...study aimed to examine the hypoglycemic effects of Polygonatum sibiricum saponin (PSS) on T2DM mice. We found that PSS could significantly decrease the levels of insulin secretion and fasting blood glucose (FBG) in T2DM mice. And the level of triacylglycerol (TG), total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C) in the blood was decreased. In contrast, the content of high-density lipoprotein cholesterol (HDL-C) was increased. 16S rDNA sequencing was used to evaluate the changes in the gut microbiota of T2DM mice, and metabolites were analyzed by metabolomic profiling. The results showed that PSS could decrease the abundance of Firmicutes in T2DM mice, increase the abundance of Bacteroidetes. It also increased the abundance of some bacterial genera (Lactobacillus, Lachnospiraceae_NK4A136_group and Intestinimonas). The phenotypes of the gut microbiome also changed accordingly. Metabolomics analysis showed that carbohydrate metabolism and amino acid metabolisms, such as L-alanine and L-glutamic acid, were greatly affected by PSS. In addition, the levels of inositol and chlorogenic acid in metabolites also increased significantly under PSS intervention. In general, PSS could exert its hypoglycemic effect, regulate the gut microbiota and affect the metabolism of T2DM mice.
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•Polygonatum sibiricum saponin improve glucose and lipid metabolism disorders in diabetic mice.•Polygonatum sibiricum saponin modulate the composition, structure and metabolism of gut microbiota.•Polygonatum sibiricum saponin affect the amino acid metabolism pathway of the gut microbiota.
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