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Currently available drugs for trypanosomiasis are few, and their use is limited by toxicity and growing resistance. This highlights the need for safer and more effective alternatives. In this study, the in vitro and in vivo antitrypanosomal activities of an 80% methanol root extract of Lobelia rhynchopetalum and its major constituent were evaluated against Trypanosoma congolense field isolates. Phytochemical separation of the extract yielded lobetyolin (a polyacetylene compound), confirmed through spectroscopic analysis. At 4 mg/mL, both the crude extract and lobetyolin inhibited parasite motility, with lobetyolin acting slightly faster (25 min) than the extract (30 min). The blood incubation assay demonstrated dose‐dependent protection, with 4 mg/mL of DA, the lobetyolin‐rich extract, or pure lobetyolin preventing infection, while lower doses only delayed parasitemia. In vivo testing showed that lobetyolin at 100 mg/kg exhibited stronger activity than the crude extract at 400 mg/kg. Molecular docking demonstrated that lobetyolin binds strongly to the homology‐modeled trypanothione reductase (TR) enzyme of T. congolense , achieving a Glide score of −8.002 kcal/mol, which is close to that of the native ligand (−8.307 kcal/mol). This suggests that lobetyolin may inhibit TR, thereby disrupting the parasite′s redox balance essential for survival. Overall, these findings provide the first evidence supporting the antitrypanosomal activity of L. rhynchopetalum root extract and lobetyolin, providing scientific support to the plant′s traditional use. Further studies are needed to fully validate its therapeutic potential.

Lobeline is an alkaloid derived from the leaves of an Indian tobacco plant (Lobelia inflata), which has been prepared by chemical synthesis. It is classified as a partial nicotinic agonist and has a long history of therapeutic usage ranging from emetic and respiratory stimulant to tobacco smoking cessation agent. The presence of both cis and trans isomers in lobeline is well known, and many studies on the relationship between the structure and pharmacological activity of lobeline and its analogs have been reported. However, it is a remarkable fact that no studies have reported the differences in pharmacological activities between the two isomers. In this article, we found that different degrees of isomerization of lobeline injection have significant differences in respiratory excitatory effects in pentobarbital sodium anesthetized rats. Compared with cis-lobeline injections, the respiratory excitatory effect was significantly reduced by 50.2% after administration of injections which contained 36.9% trans-lobeline. The study on the influencing factors of isomerization between two isomers shown that this isomerization was a one-way isomerism and only converted from cis to trans, where temperature was the catalytic factor and pH was the key factor. This study reports a new discovery. Despite the widespread use of ventilators, first-aid medicines such as nikethamide and lobeline has retired to second line, but as a nonselective antagonist with high affinity for a4b2 and a3b2 nicotinic acetylcholine receptors (nAChRs). In recent years, lobeline has shown great promise as a therapeutic drug for mental addiction and nervous system disorders, such as depression, Alzheimer disease and Parkinson disease. Therefore, we suggest that the differences between two isomers should be concerned in subsequent research papers and applications.

A neutral α-glucan, named BP1, with a molecular mass of approximately 9.45 kDa, was isolated from Lobelia chinensis by hot-water extraction, a Q-Sepharose Fast Flow column and Superdex-75 column chromatography. Its chemical structure was characterized by monosaccharide analysis, methylation analysis and analysis of its FT-IR, high performance gel permeation chromatography (HPGPC) and 1D/2D-NMR spectra data. The backbone of BP1 consists of →6α-d-Glcp1→6,3α-d-Glcp1→(6α-d-Glcp1)x-6,3α-d-Glcp1-(6α-d-Glcp1)y→. The side chains were terminal α-d-Glcp1→ and α-d-Glcp1→ (6α-d-Glcp1)z→4α-d-Glcp1→3α-d-Glcp1→4α-d-Glcp1→ (x + y + z = 5), which are attached to the backbone at O-3 of 3,6α-d-Glcp1. The results of the effect of BP1 on mouse macrophage cell line RAW 264.7 indicate that BP1 enhances the cell proliferation, phagocytosis, nitric oxide production and cytokine secretion in a dose-dependent manner. Because the inhibitor of Toll-like receptor 4 blocks the BP1-induced secretion of TNF-α and IL-6, we hypothesize that α-glucan BP1 activates TLR4, which mediates the above-mentioned immunomodulating effects.

Malignant melanoma (MM) is the most dangerous type of skin cancer, killing more than 1,100 people each year in Canada. Prognosis for late stage and recurrent MM is extremely poor due to insensitivity to chemotherapy drugs, and thus many patients seek complementary and alternative medicines. In this study, we examined four commonly used anticancer herbs in traditional Chinese medicine, , , , and , for their in vitro antitumor effects toward human MM cell line A-375. The crude water extract of (1 g of dry herb in 100 mL water) and its 2-fold dilution caused 52.8%±13.0% and 17.3%±2.7% cytotoxicity in A-375 cells, respectively ( <0.01). The crude water extract of caused 11.1%±12.4% cytotoxicity in A-375 cells with no statistical significance ( >0.05). Higher concentrated formulation might be needed for to exert its cytotoxic effect against A-375 cells. No cytotoxicity was observed in A-375 cells treated with crude water extract of and . Further high performance liquid chromatography-tandem mass spectroscopy analysis of the herbal extracts implicated that and might have adopted the same bioactive components for their cytotoxic effects in spite of belonging to two different plant families. We also showed that the crude water extract of reduced intracellular reactive oxygen species generation in A-375 cells, which may lead to a cytostatic effect. Furthermore, synergistic effect was achieved when crude water extract of was coadministered with temozolomide, a chemotherapy drug for skin cancer.

Insects that feed on plants protected by latex canals often sever leaf veins or cut trenches across leaves before feeding distal to the cuts. The insects thereby depressurize the canals and reduce latex exudation at their prospective feeding site. How the cuts affect the distribution and concentration of latex chemicals was not known. We modified a microwave-assisted extraction technique to analyze the spatial distribution of alkaloids in leaves of Lobelia cardinalis (Campanulaceae) that have been trenched by a plusiine caterpillar, Enigmogramma basigera (Lepidoptera: Noctuidae). We produced sharp two dimensional maps of alkaloid distribution by microwaving leaves to transfer alkaloids to TLC plates that were then sprayed with Dragendorff's reagent to visualize the alkaloids. The leaf prints were photographed and analyzed with image processing software for quantifying alkaloid levels. A comparison of control and trenched leaves documented that trenching reduces alkaloid levels by approximately 50% both distal and proximal to the trench. The trench becomes greatly enriched in alkaloids due to latex draining from surrounding areas. Measurements of exudation from trenched leaves demonstrate that latex pressures are rapidly restored proximal, but not distal to the trench. Thus, the trench serves not only to drain latex with alkaloids from the caterpillar's prospective feeding site, but also to isolate this section, thereby preventing an influx of latex from an extensive area that likely extends beyond the leaf. Microwave-assisted extraction of leaves has potential for diverse applications that include visualizing the impact of pathogens, leaf miners, sap-sucking insects, and other herbivores on the distribution and abundance of alkaloids and other important defensive compounds.

Larvae of the cabbage looper, Trichoplusia ni (Lepidoptera: Noctuidae), often transect leaves with a narrow trench before eating the distal section. The trench reduces larval exposure to exudates, such as latex, during feeding. Plant species that do not emit exudate, such as Plantago lanceolata, are not trenched. However, if exudate is applied to a looper's mouth during feeding on P. lanceolata, the larva will often stop and cut a trench. Dissolved chemicals can be similarly applied and tested for effectiveness at triggering trenching. With this assay, I have documented that lactucin from lettuce latex (Lactuca sativa), myristicin from parsley oil (Petroselinum crispum), and lobeline from cardinal flower (Lobelia cardinalis) elicit trenching. These compounds are the first trenching stimulants reported. Several other constituents of lettuce and parsley, including some phenylpropanoids, monoterpenes, and furanocoumarins had little or no activity. Cucurbitacin E glycoside found in cucurbits, another plant family trenched by cabbage loopers, also was inactive. Lactucin, myristicin, and lobeline all affect the nervous system of mammals, with lobeline acting specifically as an antagonist of nicotinic acetylcholine receptors. To determine if cabbage loopers respond selectively to compounds active at acetylcholine synapses, I tested several neurotransmitters, insecticides, and drugs with known neurological activity, many of which triggered trenching. Active compounds included dopamine, serotonin, the insecticide imidacloprid, and various drugs such as ipratropium, apomorphine, buspirone, and metoclopramide. These results document that noxious plant chemicals trigger trenching, that loopers respond to different trenching stimulants in different plants, that diverse neuroactive chemicals elicit the behavior, and that feeding deterrents are not all trenching stimulants. The trenching assay offers a novel approach for identifying defensive plant compounds with potential uses in agriculture or medicine. Cabbage loopers in the lab and field routinely trench and feed on plants in the Asteraceae and Apiaceae. However, first and third instar larvae enclosed on Lobelia cardinalis (Campanulaceae) failed to develop, even though the third instar larvae attempted to trench. Trenching ability does not guarantee effective feeding on plants with canal-borne exudates. Cabbage loopers must not only recognize and respond to trenching stimulants, they must also tolerate exudates during the trenching procedure to disable canalicular defenses.

Chronic wounds present a major clinical challenge, often aggravated by infection and rising antimicrobial resistance. This study investigated the wound-healing efficacy of Lobelia alsinoides Lam., an ethnomedicinal herb, formulated as a topical ointment containing its ethanolic extract (LT). Phytochemical profiling identified high levels of phenolics, terpenoids, and tannins, while in vitro assays demonstrated strong antioxidant, broad-spectrum antimicrobial, and cytocompatible properties. Wound-healing potential was evaluated using excision and incision wound models in rats treated with 5% or 10% LT ointments, with Silverex™ as the reference standard. The 10% LT formulation significantly outperformed Silverex™, accelerating wound contraction (99.33 ± 0.55% by Day 16), shortening epithelialization time (16.1 ± 0.8 days), and enhancing tensile strength (837.36 ± 16.37 g; p < 0.001). Biochemical and histological analyses confirmed improved collagen deposition, extracellular matrix remodeling, and angiogenesis, without hepatic or renal toxicity. Overall, LT exhibited statistically superior wound-healing efficacy compared with Silverex™, supporting its potential as a safe, affordable, and sustainable phytotherapeutic alternative. These findings provide strong scientific validation for L. alsinoides as an evidence-based herbal candidate for integration into modern wound care, with future studies warranted to establish mechanistic and clinical efficacy in chronic and infected wounds.

The skin acts as a mechanical barrier that protects the body from the exterior environment, and skin barrier function is attributed to the stratum corneum (SC), which is composed of keratinocytes and skin lipids. Skin barrier homeostasis is maintained by a delicate balance between the differentiation and exfoliation of keratinocytes, and keratinocyte desquamation is regulated by members of the serine protease kalikrein (KLK) family and their endogenous inhibitor SPINK5/LEKTI (serine protease inhibitor Kazal type 5/lympho-epithelial Kazal-type-related inhibitor). Furthermore, SPINK5/LEKTI deficiency is involved in impaired skin barrier function caused by KLK over-activation. We sought to determine whether increased SPINK5/LEKTI expression ameliorates atopic dermatitis (AD) by strengthening skin barrier function using the ethanol extract of Lobelia chinensis (LCE) and its active compound, diosmetin, by treating human keratinocytes with UVB and using a DNCB-induced murine model of atopic dermatitis. LCE or diosmetin dose-dependently increased the transcriptional activation of SPINK5 promoter and prevented DNCB-induced skin barrier damage by modulating events downstream of SPINK5, that is, KLK, PAR2 (protease activated receptor 2), and TSLP (thymic stromal lymphopoietin). LCE or diosmetin normalized immune response in DNCB treated SKH-1 hairless mice as determined by reductions in serum immunoglobulin E and interleukin-4 levels and numbers of lesion-infiltrating mast cells. Our results suggest that LCE and diosmetin are good candidates for the treatment of skin barrier-disrupting diseases such as Netherton syndrome or AD, and that they do so by regulating SPINK5/LEKTI.

Lobelia chinensis is a kind of herbal medicine widely distributed and used in Asia. The chemical components of this herb, however, have not been well studied until now. Lobeline, as an essential and famous bioactive compound in Lobelia genus, has been assumed to be present in L. chinensis. In order to ascertain its presence and, more importantly, proper use of this herb, chemical profiling this herb with highly sensitive and high-resolution analytical mass spectrometry was applied. In this study, high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (HPLC/Q-TOF MS) method was employed to systematically profile the chemical constituents of L. chinensis for the first time. Comparative chemical profiling study of L. chinensis and Lobelia inflata was also conducted to provide evidence whether lobeline is present or not. Piperidine alkaloids except for lobeline, alkaloid-lignan hybrids, flavonoids, polyacetylenes, nonanedioic acid, and some new phytochemicals were successfully identified in L. chinensis simultaneously. Comparing to the chemical profiles of L. inflata, lobeline was found to be absent in L. chinensis. All of the secondary metabolites in L. chinensis were determined with the HPLC/Q-TOF MS method. The absence of lobeline in L. chinensis was confirmed after this extensive study.

High radial oxygen loss (ROL) from roots of aquatic plants to reduced sediments is thought to deplete the roots of oxygen and restrict the distribution of those species unable to form a barrier to oxygen loss. Metal precipitates with high iron content (Fe-plaques) frequently form on roots of aquatic plants and could create such a diffusion barrier, thereby diverting a larger proportion of downward oxygen transport to the root meristems. To investigate whether Fe-plaques form a barrier to oxygen loss, ROL and internal oxygen concentrations were measured along the length of roots of the freshwater plant Lobelia dortmanna using platinum sleeve electrodes and Clark-type microelectrodes. Measurements showed that ROL was indeed lower from roots with Fe-plaques than roots without plaques and that ROL declined gradually with thicker iron coating on roots. The low ROL was caused by low diffusion coefficients through root walls with Fe-plaques resulting in higher internal oxygen concentrations in the root lacunae. By diverting a larger proportion of downward oxygen transport to root meristems in L. dortmanna, the presence of Fe-plaques should diminish root anoxia and improve survival in reduced sediments.