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theophylline (Unifyl / Uniphyllin / theophylline, Napp)

✓ Approved

Purdue Pharma L.P. · ADORA1 · 小分子

什么是 theophylline？

theophylline 是一种小分子，由Purdue Pharma L.P.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Unifyl, Uniphyllin, theophylline, Napp
公司Purdue Pharma L.P.
药物类别小分子
分子靶点ADORA1, ADORA2A
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Purdue Pharma L.P.

作用机制

分子靶点

theophylline 作用于 2 个分子靶点：

ADORA1adenosine A1 receptor (RDC7)
ADORA2Aadenosine A2a receptor (A2aR, RDC8)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

theophylline 针对 3 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Respiratory, thoracic and mediastinal disordersAsthma✓ Approved
Respiratory, thoracic and mediastinal disordersBronchitis chronic✓ Approved
Respiratory, thoracic and mediastinal disordersChronic obstructive pulmonary disease✓ Approved

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Ma Qianting Q, Yan Zhongjun Z, Yang Xiaolu X, Hou Aixiang A et al.

Zhuyecha (ZYC, Camellia sp.) is a newly discovered special wild tea plant resource in Cangwu County, Wuzhou City, Guangxi Province, China. However, there have been few scientific studies on it. This study investigated its morphological and chemical characteristics. The results revealed that ZYC is an arbor-type, upright plant with lanceolate leaves. The flower has five petals, five sepals, a trifid style, and a glabrous ovary. ZYC exhibited a unique chemical profile distinguished from common tea cultivars. Compared with the control cultivated varieties (Hongyan 12, Fuyun 6, and Yinghong 9), ZYC fresh leaves contained significantly higher contents of theobromine, theophylline, and gallic acid, but considerably lower caffeine and lower total catechins. The principal catechins were epi-form/galloylated catechins EGCG and ECG. Notably, theobromine was the most abundant alkaloid in ZYC, followed by caffeine and theophylline. In ZYC fresh leaves, 15 differential non-volatile metabolites were identified, and 22 key aroma compounds were screened, including linalool, (E)-2-hexenal, hexanal, heptan-2-ol, and β-myrcene, among others. The volatile components were primarily alcohols, aldehydes, and esters, contributing to floral, fruity, and green aroma attributes. This work enhances the understanding of the botanical and phytochemical properties of ZYC and provides scientific guidance for further research and efficient utilization of this natural low-caffeine/high-theobromine tea resource.

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PubMedNucleic acids research2026-06-11

Enhancing small-molecule-mediated translational control through multivalent RNA aptamers.

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The precise translational control of gene expression by small molecules through RNA-based switches holds considerable promise for both research and therapeutic developments. However, current high-performance RNA switches remain limited in adaptability, with strong responses typically constrained to a narrow set of specific ligand-aptamer pairs. To address this limitation, we introduce a robust and generalizable RNA platform based on a multivalent aptamer design, which significantly enhances ligand-responsive protein expression through alternative splicing regulation. We have demonstrated that the inherently weak aptamers, such as those for theophylline or tetracycline, can be dramatically improved through this multivalency circuit, elevating the induction levels from modest (<10-fold) to over 100-fold, an increase of more than an order of magnitude. Leveraging these improved switches, we achieve multiplex and orthogonal control over distinct protein outputs with these suboptimal aptamers. Furthermore, we implement precise manipulation of cellular phenotypes through the ligand-controlled expression of functional proteins, including the pro-apoptotic effector BAX and the adhesion protein E-cadherin. This work establishes a general and adaptable RNA platform for expanding the toolbox of small-molecule regulators of protein expression, with potential applications across synthetic biology and therapeutic applications.

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Phenotypic, physicochemical, sensory, and functional attributes of cocoa (Theobroma cacao L.) from Brazilian Amazonian floodplain and upland ecosystems.

Silva Danielle Amaral E DAE, de Lima Consuelo Lúcia Sousa CLS, Lima Giulia Victória Silva GVS, Silva Angela Maria Miranda AMM et al.

Cocoa (Theobroma cacao L.) from the Brazilian Amazon plays an important role in national production. While most cocoa is cultivated in upland systems, floodplain ecosystems represent a traditional and distinct production environment that may influence bean composition and quality. This study characterizes floodplain cocoa (FC) and compares it with upland cocoa (UC) from the eastern Amazon. FC fruits had an oval shape and thick husks, with smaller beans than UC, both well fermented. FC beans had higher fiber content (17.70 ± 0.7 g/100 g dry matter (DM)) and total polyphenols (27.04 ± 0.69 mg CE/g DM), but lower protein content (14.99 g/100 g DM) and antioxidant capacity (627.45 ± 30.99 μmol TE/g DM) compared to UC beans (fiber: 14.57 ± 0.40 g/100 g DM; protein: 16.44 g/100 g DM; polyphenols: 14.19 ± 4.19 mg CE/g DM; antioxidant capacity: 1112.58 ± 56.47 μmol TE/g DM). FC beans showed higher levels of caffeine and theophylline, and a theobromine/caffeine ratio typical of Criollo cocoa. Chocolates from both exhibited favorable attributes, including fine-flavor notes, and were similarly accepted by consumers. FC and UC beans exhibited distinct physicochemical profiles, both showing adequate fermentation and similar consumer acceptance, highlighting the potential of Amazonian cocoa for product differentiation and valorization of regionally distinct systems. © 2026 The Author(s). Journal of the Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

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Ahmed Yousif Montasir Mohamedsaeed MM, Singanamala Rizwana R, Gari Poornima Manjulatha PM, Eranti Bhargav B

Chronic obstructive pulmonary disease (COPD) remains a major global healthcare burden, necessitating multimodal pharmacologic strategies optimized for effective drug delivery. Inhalation is the preferred route due to targeted pulmonary deposition, rapid onset, reduced systemic exposure, and lower dose requirements. Pressurized metered-dose inhalers, dry-powder inhalers, soft-mist inhalers, and nebulizers demonstrate proven efficacy; however, effectiveness is limited by patient technique, inspiratory capacity, and device-dependent variability. Oral agents, including corticosteroids, phosphodiesterase-4 inhibitors, and theophylline, provide systemic anti-inflammatory and bronchodilator effects but are constrained by adverse event profiles and narrow therapeutic windows. Parenteral therapy, such as intravenous corticosteroids and bronchodilators, remains primarily reserved for severe exacerbations; however, evidence suggests limited superiority over oral corticosteroids. Intravenous alpha-1 antitrypsin replacement offers a disease-modifying benefit in genetically deficient populations, slowing emphysema progression and improving survival. Transdermal nicotine replacement therapy contributes indirectly to COPD management via smoking cessation support. Collectively, inhalation continues to dominate COPD maintenance therapy, while systemic routes are reserved for specific indications. The optimal outcomes depend on individualized route selection based on disease severity, patient ability, and therapeutic goals.

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Interfacial Organization and Structural Changes in Model Lung Surfactants Induced by Methylxanthines.

Kołomyjska Wiktoria W, Zaborowska-Mazurkiewicz Michalina M, Fontaine Philippe P, Matyszewska Dorota D

This study investigates the interfacial interactions between the selected methylxanthines, theophylline (Theo) and its derivative theophylline-7-acetic acid (TheoAcid), and model pulmonary surfactants. Chronic obstructive pulmonary disease (COPD) and asthma treatments utilizing these drugs are often limited by a narrow therapeutic window and systemic toxicity. We explore the biophysical feasibility of localized inhalation delivery by analyzing physicochemical drug effects on two-dimensional (2D) monolayers of DPPC, DPPG, and their binary mixture (8:2 molar ratio) at the air-water interface. Structural reorganization was interrogated using Brewster angle microscopy (BAM), grazing incidence X-ray diffraction (GIXD), and polarization modulation infrared reflection absorption spectroscopy (PM-IRRAS). Results demonstrate that while theophylline exerts a mild influence, theophylline-7-acetic acid significantly disrupts the organization of the lipid models. The surface properties of phospholipid membranes probed by the Langmuir technique change significantly when exposed to theophylline-7-acetic acid. GIXD analysis reveals a drug-induced transition from rectangular to hexagonal molecular packing in the DPPG monolayers. Furthermore, PM-IRRAS identifies preferential interactions with phosphate head groups, leading to changes in hydration and interfacial fluidization. The increased effect of TheoAcid compared to that of theophylline is attributed to possible electrostatic interactions, especially with negatively charged DPPG layers. These findings were also bridged to three-dimensional (3D) systems using fluorescence microscopy of giant unilamellar vesicles (GUVs), which confirmed drug-induced phase separation and morphological changes. Together, these results provide information about the physicochemical mechanisms of methylxanthine-lung surfactant interactions, offering critical insights into the stability of pulmonary interfaces under drug exposure.

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Masters Chloe C, Ali Ajmol A, Badenhorst Claire C, Dickens Martin M et al.

This study examined the effects of caffeine consumption on endurance exercise performance, and the influence of CYP1A2 gene polymorphisms in caffeine pharmacokinetics and exercise performance. The data sets of two randomised, double blind, placebo-controlled crossover study design experiments have been merged. Thirty-eight recreationally active male participants provided saliva samples for CYP1A2 genotyping (AA homozygotes n = 19; AC heterozygotes n = 19) and completed either a 10-km run or 40-km cycling time trial of 60-min following a single dose of 6 mg·kg-1 caffeine (CAF) or placebo (maltodextrin; PLA) throughout which heart rate (HR) and time to completion (TTC) were measured. Caffeine ingestion improved TTC by 1.8% (p = 0.05; ηp 2 = 0.12). HR was higher in CAF trials compared to PLA (p = 0.02; ηp 2 = 0.15). Plasma caffeine concentrations were higher in AA allele carriers compared with AC allele carriers (p = 0.04; ηp 2 = 0.139). No caffeine-gene interaction effects were observed in TTC, HR or plasma concentrations of paraxanthine and theophylline. Total caffeine plasma concentrations in the area under the concentration-time curve (AUC) were significantly higher in AA allele carriers compared with AC allele carriers (p = 0.01). Ingesting a dose of 6 mg·kg-1 caffeine 60-min prior to exercise is likely to improve performance in endurance activities in recreationally trained males. Plasma caffeine concentrations were significantly higher in AA allele carriers compared to AC allele carriers, though no gene-caffeine interaction main effects were observed in TTC; so, the role of CYP1A2 gene polymorphisms in determining enhancements in exercise performance remains unclear.

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